HTS and Rational Drug Design to Generate a Class of 5‐HT2C‐Selective Ligands for Possible Use in Schizophrenia.

The expanded biology of serotonin

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Pharmacological studies of prepulse inhibition models of sensorimotor gating deficits in schizophrenia: a decade in review

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Eating disorder and epilepsy in mice lacking 5-HT2C serotonin receptors

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Hallucinogens

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Evidence for Possible Involvement of 5-HT _2B Receptors in the Cardiac Valvulopathy Associated With Fenfluramine and Other Serotonergic Medications

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Assessing the Validity of an Animal Model of Deficient Sensorimotor Gating in Schizophrenic Patients

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Drugs and Valvular Heart Disease

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N-Desalkylquetiapine, a Potent Norepinephrine Reuptake Inhibitor and Partial 5-HT1A Agonist, as a Putative Mediator of Quetiapine's Antidepressant Activity

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Molecular Biology of Serotonin Receptors - Structure and Function at the Molecular Level

Kroeze, W. K., Kristiansen, K., & Roth, B. (2002) · Current Topics in Medicinal Chemistry · doi:10.2174/1568026023393796 · Cited by 278 · see citing works

Animal behavior models of the mechanisms underlying antipsychotic atypicality

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Enhanced Locomotor, Reinforcing, and Neurochemical Effects of Cocaine in Serotonin 5-Hydroxytryptamine 2C Receptor Mutant Mice

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WAY-163909 [(7 bR,10 aR)-1,2,3,4,8,9,10,10 a-Octahydro-7 bH-cyclopenta-[b][1,4]diazepino[6,7,1hi]indole]: A Novel 5-Hydroxytryptamine 2C Receptor-Selective Agonist with Preclinical Antipsychotic-Like Activity

Marquis, K. L., Sabb, A. L., Logue, S. F., Brennan, J. A., Piesla, M. J., Comery, T. A., Grauer, S. M., Ashby, C. R., Nguyen, H. Q., Dawson, L. A., et al. (2006) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.106.106989 · Cited by 145 · see citing works

Compulsive behavior in the 5-HT2C receptor knockout mouse

Chou-Green, J. M., Holscher, T. D., Dallman, M. F., & Akana, S. F. (2003) · Physiology & Behavior · doi:10.1016/s0031-9384(03)00047-7 · Cited by 143 · see citing works

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 137 · see citing works

5-HT2C receptors mediate penile erections in rats: actions of novel and selective agonists and antagonists

Millan, M. J., Péglion, J.-L., Lavielle, G., & Monneyron, S. (1997) · European Journal of Pharmacology · doi:10.1016/s0014-2999(97)89962-1 · Cited by 124 · see citing works

SEROTONIN 5-HT2C RECEPTOR AGONISTS: POTENTIAL FOR THE TREATMENT OF OBESITY

Miller, K. J. (2005) · Molecular Interventions · doi:10.1124/mi.5.5.8 · Cited by 95 · see citing works

Pharmacological Profile of the 5‐HT2C Receptor Agonist WAY‐163909; Therapeutic Potential in Multiple Indications

Dunlop, J., Marquis, K. L., Lim, H., Leung, L., Kao, J., Cheesman, C., & Rosenzweig-Lipson, S. J. (2006) · CNS Drug Reviews · doi:10.1111/j.1527-3458.2006.00167.x · Cited by 80 · see citing works

5-Hydroxytryptamine 2C (5-HT2C) Receptor Agonists as Potential Antiobesity Agents

Nilsson, B. M. (2006) · Journal of Medicinal Chemistry · doi:10.1021/jm058240i · Cited by 75 · see citing works

Stimulation of serotonin2C receptors influences cocaine-seeking behavior in response to drug-associated stimuli in rats

Burbassi, S., & Cervo, L. (2007) · Psychopharmacology · doi:10.1007/s00213-007-0916-7 · Cited by 74 · see citing works

Self-Repairing DNA Based on a Reductive Electron Transfer through the Base Stack

Schwögler, A., Burgdorf, L. T., & Carell, T. (2000) · Angewandte Chemie International Edition · doi:10.1002/1521-3773(20001103)39:21 · Cited by 59 · see citing works

Selective 5-Hydroxytryptamine 2C Receptor Agonists Derived from the Lead Compound Tranylcypromine: Identification of Drugs with Antidepressant-Like Action

Cho, S. J., Jensen, N., Kurome, T., Kadari, S., Manzano, M. L., Malberg, J. E., Caldarone, B. J., Roth, B. L., & Kozikowski, A. P. (2009) · Journal of Medicinal Chemistry · doi:10.1021/jm801354e · Cited by 54 · see citing works

(1R, 3S)-(−)-Trans-PAT: A novel full-efficacy serotonin 5-HT2C receptor agonist with 5-HT2A and 5-HT2B receptor inverse agonist/antagonist activity

Booth, R. G., Fang, L., Huang, Y.-S., Wilczynski, A. M., & Sivendran, S. (2009) · European Journal of Pharmacology · doi:10.1016/j.ejphar.2009.04.035 · Cited by 39 · see citing works

Agonists of the serotonin 5-HT2C receptor: preclinical and clinical progression in multiple diseases.

Wacker, D. A., & Miller, K. J. (2008) · PubMed · Cited by 34 · see citing works

Tricyclic dihydroquinazolinones as novel 5-HT2C selective and orally efficacious anti-obesity agents

Ahmad, S., Ngu, K., Miller, K. J., Wu, G. Y., Hung, C.-P., Malmstrom, S. E., Zhang, G., O’Tanyi, E., Keim, W. J., Cullen, M. J., et al. (2009) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2009.12.014 · Cited by 20 · see citing works

Selbstreparierende DNA basierend auf einem reduktiven Elektronentransfer durch den Basenstapel

Schwögler, A., Burgdorf, L. T., & Carell, T. (2000) · Angewandte Chemie · doi:10.1002/1521-3757(20001103)112:21 · Cited by 15 · see citing works

Selective Agents for Serotonin2C (5-HT2C) Receptor

Lacivita, E., & Leopoldo, M. (2006) · Current Topics in Medicinal Chemistry · doi:10.2174/156802606778522168 · Cited by 15 · see citing works

Food and Drugs: Arena Pharmaceuticals Develops Next Generation Obesity Drug

Wolfson, W. (2008) · Chemistry & Biology · doi:10.1016/j.chembiol.2008.11.002 · Cited by 1 · see citing works

A Fluoride-Derived Electrophilic Late-Stage Fluorination Reagent for PET Imaging

Lee, E., Kamlet, A. S., Powers, D. C., Neumann, C. N., Boursalian, G. B., Furuya, T., Choi, D. S., Hooker, J. M., & Ritter, T. (2011) · Science · doi:10.1126/science.1212625 · Cited by 420 · see citing works

Schizophrenia, “Just the Facts” 5. Treatment and prevention Past, present, and future

Tandon, R., Nasrallah, H. A., & Keshavan, M. S. (2010) · Schizophrenia Research · doi:10.1016/j.schres.2010.05.025 · Cited by 385 · see citing works

Reward circuitry dysfunction in psychiatric and neurodevelopmental disorders and genetic syndromes: animal models and clinical findings

Dichter, G. S., Damiano, C. A., & Allen, J. A. (2012) · Journal of Neurodevelopmental Disorders · doi:10.1186/1866-1955-4-19 · Cited by 299 · see citing works

Serotonin receptors and heart valve disease—It was meant 2B

Hutcheson, J. D., Setola, V., Roth, B. L., & Merryman, W. D. (2011) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2011.03.008 · Cited by 256 · see citing works

Application of Palladium-Mediated 18F-Fluorination to PET Radiotracer Development: Overcoming Hurdles to Translation

Kamlet, A. S., Neumann, C. N., Lee, E., Carlin, S. M., Moseley, C. K., Stephenson, N. A., Hooker, J. M., & Ritter, T. (2013) · PLoS ONE · doi:10.1371/journal.pone.0059187 · Cited by 99 · see citing works

Serotonergic Mechanisms as Targets for Existing and Novel Antipsychotics

Meltzer, H. Y. (2012) · Handbook of experimental pharmacology · doi:10.1007/978-3-642-25761-2_4 · Cited by 96 · see citing works

“Selective” serotonin 5-HT2A receptor antagonists

Casey, A. B., Cui, M., Booth, R. G., & Canal, C. E. (2022) · Biochemical Pharmacology · doi:10.1016/j.bcp.2022.115028 · Cited by 94 · see citing works

Irving Page Lecture: 5-HT2A serotonin receptor biology: Interacting proteins, kinases and paradoxical regulation

Roth, B. L. (2011) · Neuropharmacology · doi:10.1016/j.neuropharm.2011.01.012 · Cited by 66 · see citing works

5-HT2C Agonists as Therapeutics for the Treatment of Schizophrenia

Rosenzweig-Lipson, S. J., Comery, T. A., Marquis, K. L., Groß, J., & Dunlop, J. (2012) · Handbook of experimental pharmacology · doi:10.1007/978-3-642-25758-2_6 · Cited by 42 · see citing works

In silico pharmacology for a multidisciplinary drug discovery process

Schiaffino‐Ortega, S., Lopez-Cara, L. C., & Salvador, M. K. (2012) · Drug metabolism and drug interactions · doi:10.1515/dmdi-2012-0021 · Cited by 42 · see citing works

Optimization of 2-Phenylcyclopropylmethylamines as Selective Serotonin 2C Receptor Agonists and Their Evaluation as Potential Antipsychotic Agents

Cheng, J., Giguère, P. M., Onajole, O. K., Lv, W., Gaisin, A. M., Gunosewoyo, H., Schmerberg, C. M., Pogorelov, V. M., Rodriguiz, R. M., Vistoli, G., et al. (2015) · Journal of Medicinal Chemistry · doi:10.1021/jm5019274 · Cited by 38 · see citing works

An Overview of Phenylcyclopropylamine Derivatives: Biochemical and Biological Significance and Recent Developments

Khan, M. N. A., Suzuki, T., & Miyata, N. (2012) · Medicinal Research Reviews · doi:10.1002/med.21269 · Cited by 33 · see citing works

Further Advances in Optimizing (2-Phenylcyclopropyl)methylamines as Novel Serotonin 2C Agonists: Effects on Hyperlocomotion, Prepulse Inhibition, and Cognition Models

Cheng, J., Giguère, P. M., Schmerberg, C. M., Pogorelov, V. M., Rodriguiz, R. M., Huang, X., Zhu, H., McCorvy, J. D., Wetsel, W. C., Roth, B. L., et al. (2015) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5b01153 · Cited by 28 · see citing works

Cataloging the interactome of small molecules and the human proteome

Gurwitz, D. (2010) · Drug Development Research · doi:10.1002/ddr.20396 · Cited by 26 · see citing works

We Need 2C but Not 2B: Developing Serotonin 2C (5‐HT2C) Receptor Agonists for the Treatment of CNS Disorders

Cheng, J., & Kozikowski, A. P. (2015) · ChemMedChem · doi:10.1002/cmdc.201500437 · Cited by 26 · see citing works

Rational Drug Design Leading to the Identification of a Potent 5-HT2C Agonist Lacking 5-HT2B Activity

Chen, G., Sung, J.-C., Huang, X.-P., Jensen, N. H., Svennebring, A., Sassano, M. F., Roth, B., & Kozikowski, A. (2011) · ACS Medicinal Chemistry Letters · doi:10.1021/ml200206z · Cited by 16 · see citing works

Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors

Fu, H., Rong, J., Chen, Z., Zhou, J., Collier, T. L., & Liang, S. H. (2022) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.2c00633 · Cited by 15 · see citing works

Synthesis and Biological Evaluation of Disubstituted Pyrimidines as Selective 5-HT2C Agonists

Kim, J., Kim, Y. J., Londhe, A. M., Pae, A. N., Choo, H., Kim, H. J., & Min, S. (2019) · Molecules · doi:10.3390/molecules24183234 · Cited by 8 · see citing works

2-Phenylcyclopropylmethylamine (PCPMA) as a privileged scaffold for central nervous system drug design

Li, H., & Cheng, J. (2024) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2024.129654 · Cited by 4 · see citing works

18F-FPP: A PET Ligand for the 5-HT2C Receptor?

Higgins, G. A. (2017) · ACS Chemical Neuroscience · doi:10.1021/acschemneuro.7b00133 · Cited by 4 · see citing works

Does green tea have an ameliorative effect against cabergoline-induced cardiotoxicity in adult male albino rats? A histological and biochemical study

Ibrahim, N., Zidan, R. A., & Karam, R. A. (2012) · The Egyptian Journal of Histology · doi:10.1097/01.ehx.0000410916.13936.83 · Cited by 3 · see citing works

Identification of Optically Active Pyrimidine Derivatives as Selective 5-HT2C Modulators

Kim, J., Jo, H., Lee, H., Choo, H., Kim, H. J., Pae, A. N., Cho, Y. W., & Min, S. (2017) · Molecules · doi:10.3390/molecules22091416 · Cited by 2 · see citing works

Discovery of New N-H Aporphine Derivatives As Brain-Penetrant Gq-Biased 5-HT2C Receptor Agonists and Dual 5-HT2C/5-HT2A Receptor Agonists.

Qin, W.-Z., Zhang, B., Wang, Q., Jiang, G., Cui, J., Chen, F., Wang, L., Chen, J.-J., Tian, S., Zhen, X.-C., et al. (2025) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5c02115 · Cited by 1 · see citing works

Cannabinoid Regulation of Serotonin 2A (5-HT 2A ) Receptor Signaling

Franklin, J. M. (2013)

Monoaminergic Approaches for Treatment of Schizophrenia

Rotella, D. P. (2012) · Royal Society of Chemistry eBooks · doi:10.1039/9781849734943-00035

TGF-beta1-induced calcification of valvular myofibroblasts: Mechanisms and therapeutic strategies

Hutcheson, J. D. (2012)

Authors Profile

Kozikowski, A. P. (2010) · ChemMedChem · doi:10.1002/cmdc.201000497

BindingDB Entry 50019614: 2-Phenylcyclopropylmethylamine (PCPMA) as a privileged scaffold for central nervous system drug design.

BindingDB (2024) · UC San Diego · doi:10.7270/q2gf0zx4

BindingDB Entry 50039696: Rational Drug Design Leading to the Identification of a Potent 5-HT(2C) Agonist Lacking 5-HT(2B) Activity.

BindingDB (2013) · UC San Diego · doi:10.7270/q2959jks

BindingDB Entry 50045700: Optimization of 2-phenylcyclopropylmethylamines as selective serotonin 2C receptor agonists and their evaluation as potential antipsychotic agents.

BindingDB (2016) · UC San Diego · doi:10.7270/q2bc4181

BindingDB Entry 50047108: Further Advances in Optimizing (2-Phenylcyclopropyl)methylamines as Novel Serotonin 2C Agonists: Effects on Hyperlocomotion, Prepulse Inhibition, and Cognition Models.

BindingDB (2017) · UC San Diego · doi:10.7270/q28c9z4p

BindingDB Entry 50015936: Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors.

BindingDB (2023) · UC San Diego · doi:10.7270/q26m3bs8

HTS and Rational Drug Design [RDD] to Generate a Class of 5-HT2C-Selective Ligands for Possible Use in Schizophrenia

Kozikowski, A. P., Cho, S. J., Allen, J. A., Jensen, N., Roth, B. L., & Svennebring, A. M. (2020) · Carolina Digital Repository (University of North Carolina at Chapel Hill) · doi:10.17615/aged-v972

Rational Drug Design Leading to the Identification of a Potent 5-HT 2C Agonist Lacking 5-HT 2B Activity

Sassano, M. F., Svennebring, A. M., Kozikowski, A. P., Jensen, N., Roth, B. L., Cho, S. J., Huang, X., & Chen, G. (2020) · Carolina Digital Repository (University of North Carolina at Chapel Hill) · doi:10.17615/5qmt-v586

We Need 2C but Not 2B: Developing Serotonin 2C (5‐HT2C) Receptor Agonists for the Treatment of CNS Disorders

Cheng, J., & Kozikowski, A. P. (2015) · ChemMedChem · doi:10.1002/cmdc.201500437 · Cited by 26 · see citing works

5-HT2C Agonists as Therapeutics for the Treatment of Schizophrenia

Rosenzweig-Lipson, S. J., Comery, T. A., Marquis, K. L., Groß, J., & Dunlop, J. (2012) · Handbook of experimental pharmacology · doi:10.1007/978-3-642-25758-2_6 · Cited by 42 · see citing works

Optimization of 2-Phenylcyclopropylmethylamines as Selective Serotonin 2C Receptor Agonists and Their Evaluation as Potential Antipsychotic Agents

Cheng, J., Giguère, P. M., Onajole, O. K., Lv, W., Gaisin, A. M., Gunosewoyo, H., Schmerberg, C. M., Pogorelov, V. M., Rodriguiz, R. M., Vistoli, G., et al. (2015) · Journal of Medicinal Chemistry · doi:10.1021/jm5019274 · Cited by 38 · see citing works