Hallucinogens and Serotonin 5-HT2A Receptor-Mediated Signaling Pathways

EVIDENCE FOR THE EXISTENCE OF MONOAMINE-CONTAINING NEURONS IN THE CENTRAL NERVOUS SYSTEM. I. DEMONSTRATION OF MONOAMINES IN THE CELL BODIES OF BRAIN STEM NEURONS.

Dahlstroem, A., & Fuxé, K. (1964) · PubMed · Cited by 5,133

How many drug targets are there?

Overington, J. P., Al-Lazikani, B., & Hopkins, A. L. (2006) · Nature Reviews Drug Discovery · doi:10.1038/nrd2199 · Cited by 3,505

A review of central 5-HT receptors and their function

Barnes, N. M., & Sharp, T. (1999) · Neuropharmacology · doi:10.1016/s0028-3908(99)00010-6 · Cited by 3,161

International Union of Pharmacology classification of receptors for 5-hydroxytryptamine (Serotonin).

Hoyer, D., Clarke, D. E., Fozard, J. R., Hartig, P. R., Martin, G. R., Mylecharane, E. J., Saxena, P. R., & Humphrey, P. P. (1994) · Pharmacological Reviews · doi:10.1016/s0031-6997(25)06783-3 · Cited by 3,003

Seven-transmembrane receptors

Pierce, K. L., Premont, R. T., & Lefkowitz, R. J. (2002) · Nature Reviews Molecular Cell Biology · doi:10.1038/nrm908 · Cited by 2,701

The structure and function of G-protein-coupled receptors

Rosenbaum, D. M., Rasmussen, S. G. F., & Kobilka, B. K. (2009) · Nature · doi:10.1038/nature08144 · Cited by 2,534

The expanded biology of serotonin

Berger, M., Gray, J. A., & Roth, B. L. (2009) · Annual Review of Medicine · doi:10.1146/annurev.med.60.042307.110802 · Cited by 2,100

Domain Interaction Between NMDA Receptor Subunits and the Postsynaptic Density Protein PSD-95

Kornau, H.-C., Schenker, L. T., Kennedy, M. B., & Seeburg, P. H. (1995) · Science · doi:10.1126/science.7569905 · Cited by 1,904

Molecular, pharmacological and functional diversity of 5-HT receptors

Hoyer, D., Hannon, J. P., & Martin, G. R. (2002) · Pharmacology Biochemistry and Behavior · doi:10.1016/s0091-3057(01)00746-8 · Cited by 1,865

Quantitative autoradiographic mapping of serotonin receptors in the rat brain. I. Serotonin-1 receptors

Pazos, A., & Palacios, J. M. (1985) · Brain Research · doi:10.1016/0006-8993(85)90856-x · Cited by 1,855

Evolving Concepts in G Protein-Coupled Receptor Endocytosis: The Role in Receptor Desensitization and Signaling

Ferguson, S. S. G. (2001) · Pharmacological Reviews · doi:10.1016/s0031-6997(24)01478-9 · Cited by 1,826

Structures of the CXCR4 Chemokine GPCR with Small-Molecule and Cyclic Peptide Antagonists

Wu, B., Chien, E. Y. T., Mol, C. D., Fenalti, G., Liu, W., Katritch, V., Abagyan, R., Brooun, A., Wells, P., Bi, F. C., et al. (2010) · Science · doi:10.1126/science.1194396 · Cited by 1,782

A ternary complex model explains the agonist-specific binding properties of the adenylate cyclase-coupled beta-adrenergic receptor.

De Lean, A., Stadel, J. M., & Lefkowitz, R. J. (1980) · Journal of Biological Chemistry · doi:10.1016/s0021-9258(20)79672-9 · Cited by 1,612

Neurotransmitters and neuromodulators in the basal ganglia

Graybiel, A. M. (1990) · Trends in Neurosciences · doi:10.1016/0166-2236(90)90104-i · Cited by 1,576

The neostriatal mosaic: multiple levels of compartmental organization

Gerfen, C. R. (1992) · Trends in Neurosciences · doi:10.1016/0166-2236(92)90355-c · Cited by 1,467

Multiple Serotonin Receptors: Differential Binding of [3H]5-Hydroxytryptamine, [3H]Lysergic Acid Diethylamide and [3H]Spiroperidol

PEROUTKA, S. J., & SNYDER, S. H. (1979) · Molecular Pharmacology · doi:10.1016/s0026-895x(25)13812-1 · Cited by 1,360

Crystal structure of the µ-opioid receptor bound to a morphinan antagonist

Manglik, A., Kruse, A. C., Kobilka, T. S., Thian, F. S., Mathiesen, J. M., Sunahara, R. K., Pardo, L., Weis, W. I., Kobilka, B. K., & Granier, S. (2012) · Nature · doi:10.1038/nature10954 · Cited by 1,356

Hallucinogens

Nichols, D. E. (2004) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2003.11.002 · Cited by 1,211

Heterotrimeric G protein activation by G-protein-coupled receptors

Oldham, W. M., & Hamm, H. E. (2008) · Nature Reviews Molecular Cell Biology · doi:10.1038/nrm2299 · Cited by 1,184

The role of β-arrestins in the termination and transduction of G-protein-coupled receptor signals

Luttrell, L. M., & Lefkowitz, R. J. (2002) · Journal of Cell Science · doi:10.1242/jcs.115.3.455 · Cited by 1,122

Functional Selectivity and Classical Concepts of Quantitative Pharmacology

Urban, J. D., Clarke, W. P., von Zastrow, M., Nichols, D. E., Kobilka, B., Weinstein, H., Javitch, J. A., Roth, B. L., Christopoulos, A., Sexton, P. M., et al. (2007) · The Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.106.104463 · Cited by 1,116

Structure-Function of the G Protein–Coupled Receptor Superfamily

Katritch, V., Cherezov, V., & Stevens, R. C. (2013) · Annual Review of Pharmacology and Toxicology · doi:10.1146/annurev-pharmtox-032112-135923 · Cited by 1,054

Psilocybin induces schizophrenia-like psychosis in humans via a serotonin-2 agonist action

Vollenweider, F. X., Vollenweider-Scherpenhuyzen, M. F. I., Bäbler, A., Vogel, H., & Hell, D. (1998) · NeuroReport · doi:10.1097/00001756-199812010-00024 · Cited by 1,018

Hallucinogens Recruit Specific Cortical 5-HT2A Receptor-Mediated Signaling Pathways to Affect Behavior

González-Maeso, J., Weisstaub, N. V., Zhou, M., Chan, P., Ivic, L., Ang, R., Lira, A., Bradley-Moore, M., Ge, Y., Zhou, Q., et al. (2007) · Neuron · doi:10.1016/j.neuron.2007.01.008 · Cited by 925

Serotonin Receptors

Nichols, D. E., & Nichols, C. D. (2008) · Chemical Reviews · doi:10.1021/cr078224o · Cited by 895 · cited 4×

Structure of the human κ-opioid receptor in complex with JDTic

Wu, H., Wacker, D., Mileni, M., Katritch, V., Han, G. W., Vardy, E., Liu, W., Thompson, A. A., Huang, X.-P., Carroll, F. I., et al. (2012) · Nature · doi:10.1038/nature10939 · Cited by 879

TWO KINDS OF TRYPTAMINE RECEPTOR

GADDUM, J. H., & PICARELLI, Z. P. (1957) · British Journal of Pharmacology and Chemotherapy · doi:10.1111/j.1476-5381.1957.tb00142.x · Cited by 847

Quantitative autoradiographic mapping of serotonin receptors in the rat brain. II. Serotonin-2 receptors

Pazos, A., Cortés, R., & Palacios, J. M. (1985) · Brain Research · doi:10.1016/0006-8993(85)90857-1 · Cited by 824

Conformational biosensors reveal GPCR signalling from endosomes

Irannejad, R., Tomshine, J. C., Tomshine, J. R., Chevalier, M., Mahoney, J. P., Steyaert, J., Rasmussen, S. G. F., Sunahara, R. K., El-Samad, H., Huang, B., et al. (2013) · Nature · doi:10.1038/nature12000 · Cited by 819

Molecular biology of 5-HT receptors

Hannon, J., & Hoyer, D. (2008) · Behavioural Brain Research · doi:10.1016/j.bbr.2008.03.020 · Cited by 815

Identification of a serotonin/glutamate receptor complex implicated in psychosis

González-Maeso, J., Ang, R. L., Yuen, T., Chan, P., Weisstaub, N. V., López-Giménez, J. F., Zhou, M., Okawa, Y., Callado, L. F., Milligan, G., et al. (2008) · Nature · doi:10.1038/nature06612 · Cited by 803

Constitutive activity of receptors coupled to guanine nucleotide regulatory proteins

Lefkowitz, R. J., Cotecchia, S., Samama, P., & Costa, T. (1993) · Trends in Pharmacological Sciences · doi:10.1016/0165-6147(93)90048-o · Cited by 792

Safety, tolerability, and efficacy of psilocybin in 9 patients with obsessive-compulsive disorder

Moreno, F. A., Wiegand, C. B., Taitano, E. K., & Delgado, P. L. (2006) · The Journal of Clinical Psychiatry · doi:10.4088/jcp.v67n1110 · Cited by 789

DARPP-32: An Integrator of Neurotransmission

Svenningsson, P., Nishi, A., Fisone, G., Girault, J.-A., Nairn, A. C., & Greengard, P. (2004) · Annual Review of Pharmacology and Toxicology · doi:10.1146/annurev.pharmtox.44.101802.121415 · Cited by 720

A monomeric G protein-coupled receptor isolated in a high-density lipoprotein particle efficiently activates its G protein

Whorton, M. R., Bokoch, M. P., Rasmussen, S. G. F., Huang, B., Zare, R. N., Kobilka, B., & Sunahara, R. K. (2007) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0611448104 · Cited by 675

Agonist-receptor efficacy II: agonist trafficking of receptor signals

Kenakin, T. (1995) · Trends in Pharmacological Sciences · doi:10.1016/s0165-6147(00)89032-x · Cited by 657

Evidence for 5-HT2 involvement in the mechanism of action of hallucinogenic agents

Glennon, R. A., Titeler, M., & McKenney, J. D. (1984) · Life Sciences · doi:10.1016/0024-3205(84)90436-3 · Cited by 631

Regulation of GPCRs by Endocytic Membrane Trafficking and Its Potential Implications

Hanyaloglu, A. C., & Zastrow, M. V. (2008) · Annual Review of Pharmacology and Toxicology · doi:10.1146/annurev.pharmtox.48.113006.094830 · Cited by 609

Lysergic acid diethylamide (LSD) for alcoholism: meta-analysis of randomized controlled trials

Krebs, T. S., & Johansen, P.-Ø. (2012) · Journal of Psychopharmacology · doi:10.1177/0269881112439253 · Cited by 583

G Protein–Coupled Receptor Oligomerization Revisited: Functional and Pharmacological Perspectives

Ferré, S., Casadó, V., Devi, L. A., Filizola, M., Jockers, R., Lohse, M. J., Milligan, G., Pin, J.-P., & Guitart, X. (2014) · Pharmacological Reviews · doi:10.1124/pr.113.008052 · Cited by 570

Anatomy of the Serotonergic Systema

TÖRK, I. (1990) · Annals of the New York Academy of Sciences · doi:10.1111/j.1749-6632.1990.tb16870.x · Cited by 557

SERUM VASOCONSTRICTOR (SEROTONIN)

Rapport, M. M., Green, A. A., & Page, I. H. (1948) · Journal of Biological Chemistry · doi:10.1016/s0021-9258(18)57137-4 · Cited by 552

Serotonin model of schizophrenia: emerging role of glutamate mechanisms

Aghajanian, G. (2000) · Brain Research Reviews · doi:10.1016/s0165-0173(99)00046-6 · Cited by 529

Serotonin: a review

MOHAMMAD‐ZADEH, L. F., MOSES, L., & GWALTNEY‐BRANT, S. M. (2008) · Journal of Veterinary Pharmacology and Therapeutics · doi:10.1111/j.1365-2885.2008.00944.x · Cited by 522

Effector Pathway-Dependent Relative Efficacy at Serotonin Type 2A and 2C Receptors: Evidence for Agonist-Directed Trafficking of Receptor Stimulus

Berg, K. A., Maayani, S., Goldfarb, J., Scaramellini, C., Leff, P., & Clarke, W. P. (1998) · Molecular Pharmacology · doi:10.1124/mol.54.1.94 · Cited by 510

5-HT2AReceptor-Mediated Regulation of Brain-Derived Neurotrophic Factor mRNA in the Hippocampus and the Neocortex

Vaidya, V. A., Marek, G. J., Aghajanian, G. K., & Duman, R. S. (1997) · The Journal of Neuroscience · doi:10.1523/jneurosci.17-08-02785.1997 · Cited by 479

Biology and significance of the JAK/STAT signalling pathways

Kiu, H., & Nicholson, S. E. (2012) · Growth Factors · doi:10.3109/08977194.2012.660936 · Cited by 470

Structure of active β-arrestin-1 bound to a G-protein-coupled receptor phosphopeptide

Shukla, A. K., Manglik, A., Kruse, A. C., Xiao, K., Reis, R. I., Tseng, W.-C., Staus, D. P., Hilger, D., Uysal, S., Huang, L.-Y., et al. (2013) · Nature · doi:10.1038/nature12120 · Cited by 469

Multiplicity of mechanisms of serotonin receptor signal transduction

Raymond, J. R., Mukhin, Y. V., Gelasco, A., Turner, J., Collinsworth, G., Gettys, T. W., Grewal, J. S., & Garnovskaya, M. N. (2001) · Pharmacology & Therapeutics · doi:10.1016/s0163-7258(01)00169-3 · Cited by 466

Serotonin receptors in the human brain—III. Autoradiographic mapping of serotonin-1 receptors

Pazos, A., Probst, A., & Palacios, J. M. (1987) · Neuroscience · doi:10.1016/0306-4522(87)90326-5 · Cited by 436

Acute Effects of Lysergic Acid Diethylamide in Healthy Subjects

Schmid, Y., Enzler, F., Gasser, P., Grouzmann, E., Preller, K. H., Vollenweider, F. X., Brenneisen, R., Müller, F., Borgwardt, S., & Liechti, M. E. (2015) · Biological Psychiatry · doi:10.1016/j.biopsych.2014.11.015 · Cited by 411

Lysergic acid diethylamide: Sensitive neuronal units in the midbrain raphe

Aghajanian, G. K., Foote, W. E., & Sheard, M. H. (1968) · Science · doi:10.1126/science.161.3842.706 · Cited by 404

The Fabric of Meaning and Subjective Effects in LSD-Induced States Depend on Serotonin 2A Receptor Activation

Preller, K. H., Herdener, M., Pokorny, T., Planzer, A., Kraehenmann, R., Stämpfli, P., Liechti, M. E., Seifritz, E., & Vollenweider, F. X. (2017) · Current Biology · doi:10.1016/j.cub.2016.12.030 · Cited by 402

Serotonin and hallucinogens

Aghajanian, G. (1999) · Neuropsychopharmacology · doi:10.1016/s0893-133x(98)00135-3 · Cited by 371

Functional characterization of agonists at recombinant human 5‐HT2A, 5‐HT2B and 5‐HT2C receptors in CHO‐K1 cells

Porter, R. H. P., Benwell, K. R., Lamb, H., Malcolm, C. S., Allen, N. H., Revell, D. F., Adams, D. R., & Sheardown, M. J. (1999) · British Journal of Pharmacology · doi:10.1038/sj.bjp.0702751 · Cited by 358

Serotonin receptors in the human brain—IV. Autoradiographic mapping of serotonin-2 receptors

Pazos, A., Probst, A., & Palacios, J. M. (1987) · Neuroscience · doi:10.1016/0306-4522(87)90327-7 · Cited by 355

Control of Serotonergic Function in Medial Prefrontal Cortex by Serotonin-2A Receptors through a Glutamate-Dependent Mechanism

Martı́n-Ruiz, R., Puig, M. V., Celada, P., Shapiro, D. A., Roth, B. L., Mengod, G., & Artigas, F. (2001) · The Journal of Neuroscience · doi:10.1523/jneurosci.21-24-09856.2001 · Cited by 339

Effects of Schedule I drug laws on neuroscience research and treatment innovation

Nutt, D. J., King, L. A., & Nichols, D. E. (2013) · Nature Reviews Neuroscience · doi:10.1038/nrn3530 · Cited by 337

Signaling at G-protein-coupled serotonin receptors: recent advances and future research directions

MILLAN, M., MARIN, P., BOCKAERT, J., & MANNOURYLACOUR, C. (2008) · Trends in Pharmacological Sciences · doi:10.1016/j.tips.2008.06.007 · Cited by 320

Drug Efficacy at G Protein–Coupled Receptors

Kenakin, T. (2002) · Annual Review of Pharmacology and Toxicology · doi:10.1146/annurev.pharmtox.42.091401.113012 · Cited by 316

The Rate of Action of Drugs on Cells

Clark, A. J. (1937) · General Pharmacology · doi:10.1007/978-3-642-80555-4_13 · Cited by 315

Diverse Psychotomimetics Act Through a Common Signaling Pathway

Svenningsson, P., Tzavara, E. T., Carruthers, R., Rachleff, I., Wattler, S., Nehls, M., McKinzie, D. L., Fienberg, A. A., Nomikos, G. G., & Greengard, P. (2003) · Science · doi:10.1126/science.1089681 · Cited by 314

Recent advances in the neuropsychopharmacology of serotonergic hallucinogens

Halberstadt, A. L. (2015) · Behavioural Brain Research · doi:10.1016/j.bbr.2014.07.016 · Cited by 312 · cited 3×

Decoding the signaling of a GPCR heteromeric complex reveals a unifying mechanism of action of antipsychotic drugs

Fribourg, M., Moreno, J. L., Holloway, T., Provasi, D., Baki, L., Mahajan, R., Park, G., Adney, S. K., Hatcher, C., Eltit, J. M., et al. (2011) · Cell · doi:10.1016/j.cell.2011.09.055 · Cited by 311

Transcriptome fingerprints distinguish hallucinogenic and nonhallucinogenic 5-hydroxytryptamine 2A receptor agonist effects in mouse somatosensory cortex

González-Maeso, J., Yuen, T., Ebersole, B. J., Wurmbach, E., Lira, A., Zhou, M., Weisstaub, N., Hen, R., Gingrich, J. A., & Sealfon, S. C. (2003) · The Journal of Neuroscience · doi:10.1523/jneurosci.23-26-08836.2003 · Cited by 297

Physiological Antagonism between 5-Hydroxytryptamine2A and Group II Metabotropic Glutamate Receptors in Prefrontal Cortex

Marek, G. J., Wright, R. A., Schoepp, D. D., Monn, J. A., & Aghajanian, G. K. (2000) · The Journal of Pharmacology and Experimental Therapeutics · doi:10.1016/s0022-3565(24)35262-0 · Cited by 280

Efficient Coupling of Transducin to Monomeric Rhodopsin in a Phospholipid Bilayer

Whorton, M. R., Jastrzebska, B., Park, P. S.-H., Fotiadis, D., Engel, A., Palczewski, K., & Sunahara, R. K. (2008) · Journal of Biological Chemistry · doi:10.1074/jbc.m703346200 · Cited by 266

Restructuring G-Protein- Coupled Receptor Activation

Audet, M., & Bouvier, M. (2012) · Cell · doi:10.1016/j.cell.2012.09.003 · Cited by 262

Crystal structure of oligomeric β1-adrenergic G protein–coupled receptors in ligand-free basal state

Huang, J., Chen, S., Zhang, J. J., & Huang, X.-Y. (2013) · Nature Structural & Molecular Biology · doi:10.1038/nsmb.2504 · Cited by 261

Response of cluster headache to psilocybin and LSD

Sewell, R. A., Halpern, J. H., & Pope, H. G. (2006) · Neurology · doi:10.1212/01.wnl.0000219761.05466.43 · Cited by 259

Metabotropic glutamate mGlu2 receptor is necessary for the pharmacological and behavioral effects induced by hallucinogenic 5-HT2A receptor agonists

Moreno, J. L., Holloway, T., Albizu, L., Sealfon, S. C., & González-Maeso, J. (2011) · Neuroscience Letters · doi:10.1016/j.neulet.2011.01.046 · Cited by 234

The neostriatal mosaic: multiple levels of compartmental organization

Gerfen, C. R. (1992) · Advances in Neuroscience and Schizophrenia · doi:10.1007/978-3-7091-9211-5_4 · Cited by 232

PANCREATITIS INDUCED BY 5-AMINOSALICYLIC ACID

Deprez, P., Descamps, C., & Fiasse, R. (1989) · The Lancet · doi:10.1016/s0140-6736(89)90620-x · Cited by 230

Mechanism of the 5-hydroxytryptamine 2A receptor-mediated facilitation of synaptic activity in prefrontal cortex

Béïque, J.-C., Imad, M., Mladenovic, L., Gingrich, J. A., & Andrade, R. (2007) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0700436104 · Cited by 229

Agonist-directed signaling of the serotonin 2A receptor depends on β-arrestin-2 interactions in vivo

Schmid, C. L., Raehal, K. M., & Bohn, L. M. (2008) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0708862105 · Cited by 229

The behavioral pharmacology of hallucinogens

Fantegrossi, W. E., Murnane, K. S., & Reissig, C. J. (2008) · Biochemical Pharmacology · doi:10.1016/j.bcp.2007.07.018 · Cited by 225

SERUM VASOCONSTRICTOR (SEROTONIN)

Rapport, M. M., Green, A. A., & Page, I. H. (1948) · Journal of Biological Chemistry · doi:10.1016/s0021-9258(18)57136-2 · Cited by 225

In Vivo Modulation of the Activity of Pyramidal Neurons in the Rat Medial Prefrontal Cortex by 5-HT2A Receptors: Relationship to Thalamocortical Afferents

Puig, M. V. (2003) · Cerebral Cortex · doi:10.1093/cercor/13.8.870 · Cited by 222

Head‐twitch response in rodents induced by the hallucinogen 2,5‐dimethoxy‐4‐iodoamphetamine: a comprehensive history, a re‐evaluation of mechanisms, and its utility as a model

Canal, C. E., & Morgan, D. (2012) · Drug Testing and Analysis · doi:10.1002/dta.1333 · Cited by 221

Rhodopsin-family receptors associate with small G proteins to activate phospholipase D

Mitchell, R., McCulloch, D., Lutz, E., Johnson, M., MacKenzie, C., Fennell, M., Fink, G., Zhou, W., & Sealfon, S. C. (1998) · Nature · doi:10.1038/32937 · Cited by 209

Selective visualization of rat brain 5-HT2A receptors by autoradiography with [3H]MDL 100,907

López-Giménez, J. F., Mengod, G., Palacios, J. M., & Vilaró, M. T. (1997) · Naunyn-Schmiedeberg's Archives of Pharmacology · doi:10.1007/pl00005075 · Cited by 205

Neuropeptide receptor ligands as drugs for psychiatric diseases: the end of the beginning?

Griebel, G., & Holsboer, F. (2012) · Nature Reviews Drug Discovery · doi:10.1038/nrd3702 · Cited by 194

Gonadotropin-releasing Hormone Receptor-coupled Gene Network Organization

Wurmbach, E., Yuen, T., Ebersole, B. J., & Sealfon, S. C. (2001) · Journal of Biological Chemistry · doi:10.1074/jbc.m108716200 · Cited by 187

A Direct Interaction of PSD-95 with 5-HT2A Serotonin Receptors Regulates Receptor Trafficking and Signal Transduction

Xia, Z., Gray, J. A., Compton-Toth, B. A., & Roth, B. L. (2003) · Journal of Biological Chemistry · doi:10.1074/jbc.m301905200 · Cited by 179

Purification and Functional Reconstitution of Monomeric μ-Opioid Receptors

Kuszak, A. J., Pitchiaya, S., Anand, J. P., Mosberg, H. I., Walter, N. G., & Sunahara, R. K. (2009) · Journal of Biological Chemistry · doi:10.1074/jbc.m109.026922 · Cited by 176

Autoradiographic characterization of (+-)-1-(2,5-dimethoxy-4-[125I] iodophenyl)-2-aminopropane ([125I]DOI) binding to 5-HT2 and 5-HT1c receptors in rat brain.

Appel, N. M., Mitchell, W. M., Garlick, R. K., Glennon, R. A., Teitler, M., & De Souza, E. B. (1990) · The Journal of Pharmacology and Experimental Therapeutics · doi:10.1016/s0022-3565(25)23167-6 · Cited by 176

Serotonin, But Not N -Methyltryptamines, Activates the Serotonin 2A Receptor Via a β-Arrestin2/Src/Akt Signaling Complex In Vivo

Schmid, C. L., & Bohn, L. M. (2010) · The Journal of Neuroscience · doi:10.1523/jneurosci.1665-10.2010 · Cited by 175

Synaptic multiprotein complexes associated with 5-HT2C receptors: a proteomic approach

Becamel, C. (2002) · The EMBO Journal · doi:10.1093/emboj/21.10.2332 · Cited by 173

Interaction of Serotonin 5-Hydroxytryptamine Type 2C Receptors with PDZ10 of the Multi-PDZ Domain Protein MUPP1

Bécamel, C., Figge, A., Poliak, S., Dumuis, A., Peles, E., Bockaert, J., Lübbert, H., & Ullmer, C. (2001) · Journal of Biological Chemistry · doi:10.1074/jbc.m008089200 · Cited by 172

The Serotonin 5-HT2A and 5-HT2C Receptors Interact with Specific Sets of PDZ Proteins

Bécamel, C., Gavarini, S., Chanrion, B., Alonso, G., Galéotti, N., Dumuis, A., Bockaert, J., & Marin, P. (2004) · Journal of Biological Chemistry · doi:10.1074/jbc.m312106200 · Cited by 170

Effects of serotonin 2A/1A receptor stimulation on social exclusion processing

Preller, K. H., Pokorny, T., Hock, A., Kraehenmann, R., Stämpfli, P., Seifritz, E., Scheidegger, M., & Vollenweider, F. X. (2016) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1524187113 · Cited by 169

Serotonin 5-Hydroxytryptamine2A Receptor-Coupled Phospholipase C and Phospholipase A2 Signaling Pathways Have Different Receptor Reserves

Kurrasch-Orbaugh, D. M., Watts, V. J., Barker, E. L., & Nichols, D. E. (2003) · The Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.102.042184 · Cited by 166

Behavioral Evidence for Interactions between a Hallucinogenic Drug and Group II Metabotropic Glutamate Receptors

Gewirtz, J. (2000) · Neuropsychopharmacology · doi:10.1016/s0893-133x(00)00136-6 · Cited by 164

A major role for thalamocortical afferents in serotonergic hallucinogen receptor function in the rat neocortex

Marek, G. J., Wright, R. A., Gewirtz, J. C., & Schoepp, D. D. (2001) · Neuroscience · doi:10.1016/s0306-4522(01)00199-3 · Cited by 158

DOI-Induced Activation of the Cortex: Dependence on 5-HT 2A Heteroceptors on Thalamocortical Glutamatergic Neurons

Scruggs, J. L., Patel, S., Bubser, M., & Deutch, A. Y. (2000) · Journal of Neuroscience · doi:10.1523/jneurosci.20-23-08846.2000 · Cited by 157

Animal Models of Serotonergic Psychedelics

Hanks, J. B., & González-Maeso, J. (2013) · ACS Chemical Neuroscience · doi:10.1021/cn300138m · Cited by 156

Reviews in Molecular Biology and Biotechnology: Transmembrane Signaling by G Protein-Coupled Receptors

Luttrell, L. M. (2008) · Molecular Biotechnology · doi:10.1007/s12033-008-9031-1 · Cited by 148

Identification of Three Residues Essential for 5-Hydroxytryptamine 2A-Metabotropic Glutamate 2 (5-HT2A·mGlu2) Receptor Heteromerization and Its Psychoactive Behavioral Function

Moreno, J. L., Muguruza, C., Umali, A., Mortillo, S., Holloway, T. D., Pilar-Cuéllar, F., Mocci, G., Seto, J., Callado, L. F., Neve, R. L., et al. (2012) · Journal of Biological Chemistry · doi:10.1074/jbc.m112.413161 · Cited by 142

PSD-95 Is Essential for Hallucinogen and Atypical Antipsychotic Drug Actions at Serotonin Receptors

Abbas, A. I., Yadav, P. N., Yao, W.-D., Arbuckle, M. I., Grant, S. G. N., Caron, M. G., & Roth, B. L. (2009) · Journal of Neuroscience · doi:10.1523/jneurosci.1090-09.2009 · Cited by 141

A complex signaling cascade links the serotonin2A receptor to phospholipase A2 activation: the involvement of MAP kinases

Kurrasch‐Orbaugh, D. M., Parrish, J. C., Watts, V. J., & Nichols, D. E. (2003) · Journal of Neurochemistry · doi:10.1046/j.1471-4159.2003.01921.x · Cited by 138 · cited 5×

Crosstalk between GABAB and mGlu1a receptors reveals new insight into GPCR signal integration

Rives, M., Vol, C., Fukazawa, Y., Tinel, N., Trinquet, E., Ayoub, M. A., Shigemoto, R., Pin, J., & Prézeau, L. (2009) · The EMBO Journal · doi:10.1038/emboj.2009.177 · Cited by 133

The Hallucinogen DOI Reduces Low-Frequency Oscillations in Rat Prefrontal Cortex: Reversal by Antipsychotic Drugs

Celada, P., Puig, M. V., Díaz-Mataix, L., & Artigas, F. (2008) · Biological Psychiatry · doi:10.1016/j.biopsych.2008.03.013 · Cited by 132

Effects of age on nerve fibers in the rhesus monkey optic nerve

Sandell, J. H., & Peters, A. (2000) · The Journal of Comparative Neurology · doi:10.1002/1096-9861(20010122)429:4<571::aid-cne5>3.0.co;2-x · Cited by 128

Evidence against dopamine D1/D2 receptor heteromers

Frederick, A. L., Yano, H., Trifilieff, P., Vishwasrao, H. D., Biezonski, D. K., Mészáros, J., Urizar, E. T., Sibley, D. R., Kellendonk, C., Sonntag, K., et al. (2015) · Molecular Psychiatry · doi:10.1038/mp.2014.166 · Cited by 128

Agonist activity of LSD and lisuride at cloned 5HT 2A and 5HT 2C receptors

Egan, C. T., Herrick‐Davis, K., Miller, K. J., Glennon, R. A., & Teitler, M. (1998) · Psychopharmacology · doi:10.1007/s002130050585 · Cited by 125

Reporter-gene systems for the study of G-protein-coupled receptors

Hill, S. J. (2001) · Current Opinion in Pharmacology · doi:10.1016/s1471-4892(01)00091-1 · Cited by 125

Activation of 5-HT2A/C Receptors Counteracts 5-HT1A Regulation of N-Methyl-D-aspartate Receptor Channels in Pyramidal Neurons of Prefrontal Cortex

Yuen, E. Y., Jiang, Q., Chen, P., Feng, J., & Yan, Z. (2008) · Journal of Biological Chemistry · doi:10.1074/jbc.m801713200 · Cited by 125

Allosteric signaling through an mGlu2 and 5-HT2Aheteromeric receptor complex and its potential contribution to schizophrenia

Moreno, J. L., Miranda-Azpiazu, P., García‐Bea, A., Younkin, J., Cui, M., Kozlenkov, A., Ben-Ezra, A., Voloudakis, G., Fakira, A. K., Baki, L., et al. (2016) · Science Signaling · doi:10.1126/scisignal.aab0467 · Cited by 119

The serotonin 2C receptor potently modulates the head-twitch response in mice induced by a phenethylamine hallucinogen

Canal, C. E., da Silva, U., Gresch, P. J., Watt, E. E., Sanders‐Bush, E., & Airey, D. C. (2010) · Psychopharmacology · doi:10.1007/s00213-010-1784-0 · Cited by 116

How LSD Originated

Hofmann, A. (1979) · Journal of Psychedelic Drugs · doi:10.1080/02791072.1979.10472092 · Cited by 110

Internalization and recycling of 5-HT 2A receptors activated by serotonin and protein kinase C-mediated mechanisms

Bhattacharyya, S., Puri, S., Miledi, R., & Panicker, M. M. (2002) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.212517999 · Cited by 103

The Prevalence, Maintenance, and Relevance of G Protein–Coupled Receptor Oligomerization

Milligan, G. (2013) · Molecular Pharmacology · doi:10.1124/mol.113.084780 · Cited by 103

Heterocomplex formation of 5-HT2A-mGlu2 and its relevance for cellular signaling cascades

Delille, H. K., Becker, J. M., Burkhardt, S., Bleher, B., Terstappen, G. C., Schmidt, M. U., Meyer, A. H., Unger, L., Marek, G. J., & Mezler, M. (2012) · Neuropharmacology · doi:10.1016/j.neuropharm.2012.01.010 · Cited by 98

The PDZ-binding domain is essential for the dendritic targeting of 5-HT2A serotonin receptors in cortical pyramidal neurons in vitro

Xia, Z., Hufeisen, S. J., Gray, J. A., & Roth, B. L. (2003) · Neuroscience · doi:10.1016/s0306-4522(03)00589-x · Cited by 89

GPCR oligomers in pharmacology and signaling

González‐Maeso, J. (2011) · Molecular Brain · doi:10.1186/1756-6606-4-20 · Cited by 88

Agonist-specific receptor conformations

Kenakin, T. P. (1997) · Trends in Pharmacological Sciences · doi:10.1016/s0165-6147(97)01127-9 · Cited by 88

Dysregulated 5-HT2A receptor binding in postmortem frontal cortex of schizophrenic subjects

Muguruza, C., Moreno, J. L., Umali, A., Callado, L. F., Meana, J. J., & González‐Maeso, J. (2012) · European Neuropsychopharmacology · doi:10.1016/j.euroneuro.2012.10.006 · Cited by 87

Integration of Mitogen-Activated Protein Kinase Kinase Activation in Vascular 5-Hydroxytryptamine2A Receptor Signal Transduction

Florian, J. A., & Watts, S. W. (1998) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1016/s0022-3565(24)37202-7 · Cited by 82

[3H]MDL 100,907: a novel selective 5-HT2A receptor ligand

Johnson, M., Siegel, B., & Carr, A. (1996) · Naunyn-Schmiedeberg s Archives of Pharmacology · doi:10.1007/bf00178722 · Cited by 80

[3H]MDL100,907 labels 5-HT2A serotonin receptors selectively in primate brain

López‐Giménez, J. F., Vilaró, M. T., Palacios, J. M., & Mengod, G. (1998) · Neuropharmacology · doi:10.1016/s0028-3908(98)00102-6 · Cited by 80

Quantitative Phosphoproteomics Unravels Biased Phosphorylation of Serotonin 2A Receptor at Ser280 by Hallucinogenic versus Nonhallucinogenic Agonists

Karaki, S., Bécamel, C., Murat, S., la Cour, C. M., Millan, M. J., Prézeau, L., Bockaert, J., Marin, P., & Vandermoere, F. (2014) · Molecular & Cellular Proteomics · doi:10.1074/mcp.m113.036558 · Cited by 80

CrossTalk opposing view: Weighing the evidence for class A GPCR dimers, the jury is still out

Lambert, N. A., & Javitch, J. A. (2014) · The Journal of Physiology · doi:10.1113/jphysiol.2014.272997 · Cited by 78

Role of Gq protein in behavioral effects of the hallucinogenic drug 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane

Garcia, E. E., Smith, R. L., & Sanders‐Bush, E. (2007) · Neuropharmacology · doi:10.1016/j.neuropharm.2007.03.013 · Cited by 78

Modulation of DOI-induced increases in cortical BDNF expression by group II mGlu receptors

Gewirtz, J. C., Chen, A. C. H., Terwilliger, R. Z., Duman, R. C., & Marek, G. J. (2002) · Pharmacology Biochemistry and Behavior · doi:10.1016/s0091-3057(02)00844-4 · Cited by 75

Clozapine Acts as an Agonist at Serotonin 2A Receptors to Counter MK-801-Induced Behaviors through a βArrestin2-Independent Activation of Akt

Schmid, C. L., Streicher, J. M., Meltzer, H. Y., & Bohn, L. (2014) · Neuropsychopharmacology · doi:10.1038/npp.2014.38 · Cited by 70

The 5-HT2A serotonin receptor enhances cell viability, affects cell cycle progression and activates MEK–ERK1/2 and JAK2–STAT3 signalling pathways in human choriocarcinoma cell lines

Oufkir, T., Arseneault, M., Sanderson, J. T., & Vaillancourt, C. (2010) · Placenta · doi:10.1016/j.placenta.2010.02.019 · Cited by 68

On the contraction of muscle, chiefly in relation to the presence of ‘receptive’ substances: Part IV. The effect of curari and of some other substances on the nicotine response of the sartorius and gastrocnemius muscles of the frog

Langley, J. N. (1909) · The Journal of Physiology · doi:10.1113/jphysiol.1909.sp001336 · Cited by 68

CrossTalk proposal: Weighing the evidence for Class A GPCR dimers, the evidence favours dimers

Bouvier, M., & Hébert, T. E. (2014) · The Journal of Physiology · doi:10.1113/jphysiol.2014.272252 · Cited by 65

Selective Interaction of ARF1 with the Carboxy-Terminal Tail Domain of the 5-HT2A Receptor

Robertson, D. N., Johnson, M. S., Moggach, L. O., Holland, P. J., Lutz, E. M., & Mitchell, R. (2003) · Molecular Pharmacology · doi:10.1124/mol.64.5.1239 · Cited by 65

Re-evaluation of lisuride pharmacology: 5-hydroxytryptamine 1A receptor-mediated behavioral effects overlap its other properties in rats

Marona‐Lewicka, D., Kurrasch‐Orbaugh, D. M., Selken, J., Cumbay, M. G., Lisnicchia, J., & Nichols, D. E. (2002) · Psychopharmacology · doi:10.1007/s00213-002-1141-z · Cited by 60

Structure-activity relationships and mechanism of action of hallucinogenic agents based on drug discrimination and radioligand binding studies.

Glennon, R. A., Titeler, M., & Young, R. (1986) · PubMed · Cited by 57

p90 ribosomal S6 kinase 2 exerts a tonic brake on G protein-coupled receptor signaling

Sheffler, D. J., Kroeze, W. K., Garcia, B. G., Deutch, A. Y., Hufeisen, S. J., Leahy, P. S., Brüning, J. C., & Roth, B. L. (2006) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0600585103 · Cited by 56

Manganese-enhanced magnetic resonance imaging reveals increased DOI-induced brain activity in a mouse model of schizophrenia

Malkova, N. V., Gallagher, J. J., Yu, C. Z., Jacobs, R. E., & Patterson, P. H. (2014) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1323287111 · Cited by 56

Lisuride and LSD: Dopaminergic and serotonergic interactions in the ?serotonin syndrome?

Silbergeld, E. K., & Hruska, R. E. (1979) · Psychopharmacology · doi:10.1007/bf00492209 · Cited by 50

Monitoring G-Protein-Coupled Receptor Signaling with DNA Microarrays and Real-Time Polymerase Chain Reaction

Yuen, T., Zhang, W., Ebersole, B. J., & Sealfon, S. C. (2002) · Methods in enzymology on CD-ROM/Methods in enzymology · doi:10.1016/s0076-6879(02)45047-1 · Cited by 48

Modeling “psychosis” in vitro by inducing disordered neuronal network activity in cortical brain slices

Aghajanian, G. K. (2009) · Psychopharmacology · doi:10.1007/s00213-009-1484-9 · Cited by 44

Binding sites for 5-hydroxytryptamine-2 receptor agonists are predominantly located in striosomes in the human basal ganglia

Waeber, C., & Palacios, J. M. (1994) · Molecular Brain Research · doi:10.1016/0169-328x(94)90133-3 · Cited by 41

A proteomic approach based on peptide affinity chromatography, 2-dimensional electrophoresis and mass spectrometry to identify multiprotein complexes interacting with membrane-bound receptors

Bécamel, C., Galéotti, N., Poncet, J., Jouin, P., Dumuis, A., Bockaert, J., & Marin, P. (2002) · Biological Procedures Online · doi:10.1251/bpo39 · Cited by 41

Enhanced prefrontal serotonin 2A receptor signaling in the subchronic phencyclidine mouse model of schizophrenia

Santini, M. A., Ratner, C., Aznar, S., Klein, A. B., Knudsen, G. M., & Mikkelsen, J. D. (2013) · Journal of Neuroscience Research · doi:10.1002/jnr.23198 · Cited by 38

Cross-signaling in metabotropic glutamate 2 and serotonin 2A receptor heteromers in mammalian cells

Baki, L., Fribourg, M., Younkin, J., Eltit, J. M., Moreno, J. L., Park, G., Vysotskaya, Z. V., Narahari, A. K., Sealfon, S. C., González‐Maeso, J., et al. (2016) · Pflügers Archiv - European Journal of Physiology · doi:10.1007/s00424-015-1780-7 · Cited by 38

Blockade of the behavioral effects of lysergic acid diethylamide, 2,5-dimethoxy-4-methylamphetamine, quipazine and lisuride by 5-hydroxytryptamine antagonists.

Mokler, D. J., Commissaris, R. L., Warner, M. R., & Rech, R. H. (1983) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1016/s0022-3565(25)22012-2 · Cited by 35

Human striosomes are enriched in 5‐HT 2A receptors: autoradiographical visualization with [ 3 H]MDL100,907, [ 125 I](±)DOI and [ 3 H]ketanserin

López‐Giménez, J. F., Mengod, G., Palacios, J. M., & Vilaró, M. T. (1999) · European Journal of Neuroscience · doi:10.1046/j.1460-9568.1999.00827.x · Cited by 35

Chemical Neuroanatomy of 5-HT Receptor Subtypes in the Mammalian Brain

Mengod, G., Vilaró, M. T., Cortés, R., López-Giménez, J. F., Raurich, A., & Palacios, J. M. (2006) · The Receptors · doi:10.1007/978-1-59745-080-5_10 · Cited by 33

The mGlu2/3 receptor agonist LY354740 suppresses immobilization stress-induced increase in rat prefrontal cortical BDNF mRNA expression

Lee, Y., Duman, R. S., & Marek, G. J. (2006) · Neuroscience Letters · doi:10.1016/j.neulet.2006.01.021 · Cited by 32

Gaddum and LSD: the birth and growth of experimental and clinical neuropharmacology research on 5‐HT in the UK

Green, A. R. (2008) · British Journal of Pharmacology · doi:10.1038/bjp.2008.207 · Cited by 31

Long-lasting alterations in 5-HT2A receptor after a binge regimen of methamphetamine in mice

Chiu, H., Chan, M., Lee, M.-Y., Chen, S., Zhan, Z.-Y., & Chen, H. (2014) · The International Journal of Neuropsychopharmacology · doi:10.1017/s1461145714000455 · Cited by 31

Differences in the C‐terminus contribute to variations in trafficking between rat and human 5‐HT2Areceptor isoforms: identification of a primate‐specific tripeptide ASK motif that confers GRK‐2 and β arrestin‐2 interactions

Bhattacharya, A., Sankar, S., & Panicker, M. M. (2009) · Journal of Neurochemistry · doi:10.1111/j.1471-4159.2009.06493.x · Cited by 26

Patterns of exploration in rats distinguish lisuride from lysergic acid diethylamide

Adams, L. M., & Geyer, M. A. (1985) · Pharmacology Biochemistry and Behavior · doi:10.1016/0091-3057(85)90022-x · Cited by 26

5-HT2A receptor signalling through phospholipase D1 associated with its C-terminal tail

Barclay, Z., Dickson, L., Robertson, D. N., Johnson, M. S., Holland, P. J., Rosie, R., Sun, L., Fleetwood‐Walker, S., Lutz, E. M., & Mitchell, R. (2011) · Biochemical Journal · doi:10.1042/bj20101844 · Cited by 20

N-acetylcysteine modulates hallucinogenic 5-HT2A receptor agonist-mediated responses: Behavioral, molecular, and electrophysiological studies

Lee, M.-Y., Chiang, C., Chiu, H., Chan, M., & Chen, H. (2014) · Neuropharmacology · doi:10.1016/j.neuropharm.2014.02.006 · Cited by 17

Activation of the JAK-STAT pathway is necessary for desensitization of 5-HT2A receptor-stimulated phospholipase C signalling by olanzapine, clozapine and MDL 100907

Singh, R. K., Dai, Y., Staudinger, J. L., & Muma, N. A. (2008) · The International Journal of Neuropsychopharmacology · doi:10.1017/s1461145708009590 · Cited by 14

Towards an understanding of psychedelic-induced neuroplasticity

Calder, A. E., & Hasler, G. (2023) · Neuropsychopharmacology · doi:10.1038/s41386-022-01389-z · Cited by 313

Transcriptional regulation in the rat prefrontal cortex and hippocampus after a single administration of psilocybin

Jefsen, O. H., Elfving, B., Wegener, G., & Müller, H. K. (2021) · Journal of Psychopharmacology · doi:10.1177/0269881120959614 · Cited by 127

Molecular Mechanisms of Psilocybin and Implications for the Treatment of Depression

Ling, S., Ceban, F., Lui, L. M. W., Lee, Y., Teopiz, K. M., Rodrigues, N. B., Lipsitz, O., Gill, H., Subramaniapillai, M., Mansur, R. B., et al. (2022) · CNS Drugs · doi:10.1007/s40263-021-00877-y · Cited by 127

Psilocybin targets a common molecular mechanism for cognitive impairment and increased craving in alcoholism

Meinhardt, M. W., Pfarr, S., Fouquet, G., Rohleder, C., Meinhardt, M. L., Barroso-Flores, J., Hoffmann, R., Jeanblanc, J., Paul, E., Wagner, K., et al. (2021) · Science Advances · doi:10.1126/sciadv.abh2399 · Cited by 89

Dark Classics in Chemical Neuroscience: Mescaline

Cassels, B. K., & Sáez-Briones, P. (2018) · ACS Chemical Neuroscience · doi:10.1021/acschemneuro.8b00215 · Cited by 85