Interaction of antipsychotic drugs with neurotransmitter receptor sites in vitro and in vivo in relation to pharmacological and clinical effects: role of 5HT2 receptors

Arzneimittelforschung: Erstanwendung am Menschen in der Phase I

Miletzki, B., & Gleiter, C. H. (2005) · Bundesgesundheitsblatt Gesundheitsforsch.Gesundheitsschutz · doi:10.1007/s00103-005-1024-7 · Cited by 9,355

Clozapine for the Treatment-Resistant Schizophrenic: A Double-blind Comparison With Chlorpromazine

Kane, J. (1988) · Archives of General Psychiatry · doi:10.1001/archpsyc.1988.01800330013001 · Cited by 4,156

Molecular cloning and characterization of a novel dopamine receptor (D3) as a target for neuroleptics

Sokoloff, P., Giros, B., Martres, M.-P., Bouthenet, M.-L., & Schwartz, J.-C. (1990) · Nature · doi:10.1038/347146a0 · Cited by 2,609

Cloning of the gene for a human dopamine D4 receptor with high affinity for the antipsychotic clozapine

Van Tol, H. H. M., Bunzow, J. R., Guan, H.-C., Sunahara, R. K., Seeman, P., Niznik, H. B., & Civelli, O. (1991) · Nature · doi:10.1038/350610a0 · Cited by 2,014

Brain dopamine receptors.

Seeman, P. (1980) · Pharmacological Reviews · doi:10.1016/s0031-6997(25)06839-5 · Cited by 1,892

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

Neuropsychopharmacology: 1 and 2 Proceedings of the XVIth C.I.N.P. Congress, Munich, August, 15–19, 1988

(1990) · Springer eBooks · doi:10.1007/978-3-642-74034-3 · Cited by 1,523

Classification of typical and atypical antipsychotic drugs on the basis of dopamine D-1, D-2 and serotonin2 pKi values.

Meltzer, H. Y., Matsubara, S., & Lee, J. C. (1989) · The Journal of Pharmacology and Experimental Therapeutics · doi:10.1016/s0022-3565(25)20710-8 · Cited by 1,349

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

A proposal for the classification of sigma binding sites

Quirion, R., Bowen, W. D., Itzhak, Y., Junien, J. L., Musacchio, J., Rothman, R. B., Tsung-Ping, S., Tam, S. W., & Taylor, D. P. (1992) · Trends in Pharmacological Sciences · doi:10.1016/0165-6147(92)90030-a · Cited by 755

An Anatomy of Schizophrenia?

Stevens, J. R. (1973) · Archives of General Psychiatry · doi:10.1001/archpsyc.1973.04200020023003 · Cited by 722

Serotonergic component of neuroleptic receptors

LEYSEN, J. E., NIEMEGEERS, C. J. E., TOLLENAERE, J. P., & LADURON, P. M. (1978) · Nature · doi:10.1038/272168a0 · Cited by 623

Pharmacology of risperidone (R 64 766), a new antipsychotic with serotonin-S2 and dopamine-D2 antagonistic properties.

Janssen, P. A., Niemegeers, C. J., Awouters, F., Schellekens, K. H., Megens, A. A., & Meert, T. F. (1988) · The Journal of Pharmacology and Experimental Therapeutics · doi:10.1016/s0022-3565(25)24408-1 · Cited by 468

Biochemical profile of risperidone, a new antipsychotic.

Leysen, J. E., Gommeren, W., Eens, A., de Chaffoy de Courcelles, D., Stoof, J. C., & Janssen, P. A. (1988) · The Journal of Pharmacology and Experimental Therapeutics · doi:10.1016/s0022-3565(25)13416-2 · Cited by 411

Cloning, molecular characterization, and chromosomal assignment of a gene encoding a second D1 dopamine receptor subtype: differential expression pattern in rat brain compared with the D1A receptor.

Tiberi, M., Jarvie, K. R., Silvia, C., Falardeau, P., Gingrich, J. A., Godinot, N., Bertrand, L., Yang-Feng, T. L., Fremeau, R. T., & Caron, M. G. (1991) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.88.17.7491 · Cited by 359

A detailed mapping of dopamine D-2 receptors in rat central nervous system by autoradiography with [125I]iodosulpride

Bouthenet, M.-L., Martres, M.-P., Sales, N., & Schwartz, J.-C. (1987) · Neuroscience · doi:10.1016/0306-4522(87)90008-x · Cited by 356

The ratios of serotonin2 and dopamine2 affinities differentiate atypical and typical antipsychotic drugs.

Meltzer, H. Y., Matsubara, S., & Lee, J. C. (1989) · PubMed · Cited by 322

Risperidone versus haloperidol in the treatment of chronic schizophrenic inpatients: a multicentre double‐blind comparative study

Claus, A., Bollen, J., Cuyper, H. D., Eneman, M., Malfroid, M., Peuskens, J., & Heylen, S. (1992) · Acta Psychiatrica Scandinavica · doi:10.1111/j.1600-0447.1992.tb01473.x · Cited by 295

Effector Coupling Mechanisms of the Cloned 5-HT1A Receptor

Fargin, A., Raymond, J. R., Regan, J. W., Cotecchia, S., Lefkowitz, R. J., & Caron, M. G. (1989) · Journal of Biological Chemistry · doi:10.1016/s0021-9258(18)63778-0 · Cited by 274

Effects of antipsychotic drugs on serotonin receptors.

Meltzer, H. Y., & Nash, J. F. (1991) · Pharmacological Reviews · doi:10.1016/s0031-6997(25)06671-2 · Cited by 258

Clozapine: neuroleptic-induced EPS and tardive dyskinesia

Casey, D. E. (1989) · Psychopharmacology · doi:10.1007/bf00442559 · Cited by 251

Do functional relationships exist between 5-HT1A and 5-HT2 receptors?

Darmani, N. A., Martin, B. R., Pandey, U., & Glennon, R. A. (1990) · Pharmacology Biochemistry and Behavior · doi:10.1016/0091-3057(90)90098-3 · Cited by 244

Molecular biology of the dopamine receptors

Civelli, O., Bunzow, J. R., Grandy, D. K., Zhou, Q.-Y., & Van Tol, H. H. M. (1991) · European Journal of Pharmacology: Molecular Pharmacology · doi:10.1016/0922-4106(91)90001-x · Cited by 239

Inhibition of serotonergic dorsal raphe neurons by systemic and iontophoretic administration of buspirone, a non-benzodiazepine anxiolytic drug

VanderMaelen, C. P., Matheson, G. K., Wilderman, R. C., & Patterson, L. A. (1986) · European Journal of Pharmacology · doi:10.1016/0014-2999(86)90343-2 · Cited by 233

Multiple human D5 dopamine receptor genes: a functional receptor and two pseudogenes.

Grandy, D. K., Zhang, Y. A., Bouvier, C., Zhou, Q. Y., Johnson, R. A., Allen, L., Buck, K., Bunzow, J. R., Salon, J., & Civelli, O. (1991) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.88.20.9175 · Cited by 209

Novel antipsychotic drugs share high affinity for σ receptors

Largent, B. L., Wikström, H., Snowman, A. M., & Snyder, S. H. (1988) · European Journal of Pharmacology · doi:10.1016/0014-2999(88)90527-4 · Cited by 204

Thymosthenic effects of ritanserin (R 55667), a centrally acting serotonin‐S2 receptor blocker

Reyntjens, A., Gelders, Y. G., Hoppenbrouwers, M. J. A., & Vanden Bussche, G. (1986) · Drug Development Research · doi:10.1002/ddr.430080124 · Cited by 192

The third dopamine receptor (D3) as a novel target for antipsychotics

Sokoloff, P., Martres, M.-P., Giros, B., Bouthenet, M.-L., & Schwartz, J.-C. (1992) · Biochemical Pharmacology · doi:10.1016/0006-2952(92)90227-a · Cited by 191

Neuroleptic responsivity of negative and positive symptoms in schizophrenia

(1987) · American Journal of Psychiatry · doi:10.1176/ajp.144.12.1549 · Cited by 190

New Antipsychotics: Classification, Efficacy, and Adverse Effects

Gerlach, J. (1991) · Schizophrenia Bulletin · doi:10.1093/schbul/17.2.289 · Cited by 181

In vitro and in vivo receptor binding and effects on monoamine turnover in rat brain regions of the novel antipsychotics risperidone and ocaperidone.

Leysen, J. E., Janssen, P. F. M., Gommeren, W., Wynants, J., Pauwels, P. J., & Janssen, P. A. J. (1992) · Molecular Pharmacology · doi:10.1016/s0026-895x(25)08945-x · Cited by 150

Neurotensin-dopamine interactions in the CNS

Nemeroff, C. B., & Cain, S. T. (1985) · Trends in Pharmacological Sciences · doi:10.1016/0165-6147(85)90095-1 · Cited by 129

α1-adrenoceptors in the mammalian brain: similar pharmacology but different distribution in rodents and primates

Palacios, J. M., Hoyer, D., & Cortés, R. (1987) · Brain Research · doi:10.1016/0006-8993(87)90569-5 · Cited by 128

Structural determinants of sigma receptor affinity.

Largent, B. L., Wikström, H., Gundlach, A. L., & Snyder, S. H. (1987) · Molecular Pharmacology · doi:10.1016/s0026-895x(25)13068-x · Cited by 127

Neuroleptic affinities for human brain receptors and their use in predicting adverse effects.

Richelson, E. (1984) · PubMed · Cited by 127

Effect of drugs influencing central serotonergic mechanisms on haloperidol-induced catalepsy

Balsara, J. J., Jadhav, J. H., & Chandorkar, A. G. (1979) · Psychopharmacology · doi:10.1007/bf00426037 · Cited by 126

5-HT1A receptor responsivity in anxiety disorders and depression

Lesch, K. (1991) · Progress in Neuro-Psychopharmacology and Biological Psychiatry · doi:10.1016/0278-5846(91)90001-h · Cited by 126

Therapeutic effect and safety of increasing doses of risperidone (R 64766) in psychotic patients

Mesotten, F., Suy, E., Pietquin, M., et al. (1989) · Psychopharmacology · doi:10.1007/bf00589890 · Cited by 121

An open label trial of raclopride in acute schizophrenia. Confirmation of D2-dopamine receptor occupancy by PET

Farde, L., Wiesel, F. ‐., Jansson, P., Uppfeldt, G., Wahlén, A., & Sedvall, G. (1988) · Psychopharmacology · doi:10.1007/bf00735871 · Cited by 114

5-HT2 Antagonist Ritanserin in Neuroleptic-Induced Parkinsonism: A Double-Blind Comparison with Orphenadrine and Placebo

Bersani, G., Grispini, A., Marini, S., Pasini, A., Valducci, M., & Ciani, N. (1990) · Clinical Neuropharmacology · doi:10.1097/00002826-199012000-00003 · Cited by 105

5-HT2 receptor blockade by ICI 169,369 and other 5-HT2 antagonists modulates the effects of D-2 dopamine receptor blockade.

Saller, C. F., Czupryna, M. J., & Salama, A. I. (1990) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1016/s0022-3565(25)13217-5 · Cited by 88

The nucleus accumbens–possible site of antipsychotic action of neuroleptic drugs?

Crow, T. J., Deakin, J. F. W., & Longden, A. (1977) · Psychological Medicine · doi:10.1017/s0033291700029287 · Cited by 80

Potential neuroleptic agents. 4. Chemistry, behavioral pharmacology, and inhibition of [3H]spiperone binding of 3,5-disubstituted N-[(1-ethyl-2-pyrrolidinyl)methyl]-6-methoxysalicylamides

de Paulis, T., Kumar, Y., Johansson, L., Raemsby, S., Hall, H., Sällemark, M., Aengeby-Moeller, K., & Oegren, S. O. (1986) · Journal of Medicinal Chemistry · doi:10.1021/jm00151a010 · Cited by 71

Pilot Clinical Investigation of Risperidone in the Treatment of Psychotic Patients

Gelders, Y. G., Heylen, S., Bussche, G., et al. (1990) · Pharmacopsychiatry · doi:10.1055/s-2007-1014509 · Cited by 70

Ritanserin, a new therapeutic approach for drug abuse. Part 1: Effects on alcohol

Meert, T. F., & Janssen, P. A. J. (1991) · Drug Development Research · doi:10.1002/ddr.430240305 · Cited by 66

Gaps and peculiarities in 5-HT2 receptor studies.

(1990) · PubMed · Cited by 62

Effects of amperozide in schizophrenia

Axelsson, R., Nilsson, A., Christensson, E., & Björk, A. (1991) · Psychopharmacology · doi:10.1007/bf02246025 · Cited by 59

Use of 5HT Receptor Agonists and Antagonists for the Characterization of Their Respective Receptor Sites

Leysen, J. E. (2003) · Humana Press eBooks · doi:10.1385/0-89603-122-5:299 · Cited by 56

Sleep disorders in patients with severe mental depression: Double‐blind placebo‐controlled evaluation of the value of pipamperone (Dipiperon®)

Ansoms, C., Backer‐Dierick, G. D., & Vereecken, J. L. T. M. (1977) · Acta Psychiatrica Scandinavica · doi:10.1111/j.1600-0447.1977.tb00147.x · Cited by 39

Remoxipride, a new selective D2 antagonist, and haloperidol in cebus monkeys

Gerlach, J., & Casey, D. E. (1990) · Progress in Neuro-Psychopharmacology and Biological Psychiatry · doi:10.1016/0278-5846(90)90068-r · Cited by 32

Ritanserin, a new therapeutic approach for drug abuse. Part 2: Effects on cocaine

Meert, T. F., & Janssen, P. A. J. (1992) · Drug Development Research · doi:10.1002/ddr.430250105 · Cited by 32

Behavioral disinhibition and depression in amphetaminized rats: a comparison of risperidone, ocaperidone and haloperidol.

Megens, A. A. H. P., Niemegeers, C. J. E., & Awouters, F. H. L. (1992) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1016/s0022-3565(25)11209-3 · Cited by 28

PIPAMPERONE (DIPIPERON®, R 3345) IN TROUBLESOME MENTAL RETARDATES: A DOUBLE‐BLIND PLACEBO CONTROLLED CROSS‐OVER STUDY WITH LONG‐TERM FOLLOW‐UP

van Hemert, J. C. J. (1975) · Acta Psychiatrica Scandinavica · doi:10.1111/j.1600-0447.1975.tb00039.x · Cited by 24

Comparison of the effects of haloperidol, remoxipride and raclopride on ?pre?- and postsynaptic dopamine receptors in the rat brain

Magnusson, O., Fowler, C. J., Mohringe, B., Wijkstr�m, A., & Ögren, S. O. (1988) · Naunyn-Schmiedeberg s Archives of Pharmacology · doi:10.1007/bf00169527 · Cited by 23

Double blind comparative study of remoxipride and haloperidol in acute schizophrenic patients

den Boer, J. A., Ravelli, D. P., Huisman, J., Öhrvik, J., Verhoeven, W. M. A., & Westenberg, H. G. M. (1990) · Psychopharmacology · doi:10.1007/bf02245748 · Cited by 23

Interaction of haloperidol and risperidone (R 64 766) with amphetamine‐induced motility changes in rats

Megens, A. A. H. P., Awouters, F. H. L., & Niemegeers, C. J. E. (1989) · Drug Development Research · doi:10.1002/ddr.430170104 · Cited by 21

Efficacy and safety of tiospirone vs. haloperidol and thioridazine in a double-blind, placebo-controlled trial.

Borison, R. L., Sinha, D., Haverstock, S. L., Mc, M., & Diamond, B. I. (1989) · PubMed · Cited by 17

A retrospective evaluation of pipamperone (Dipiperon) in the treatment of behavioural deviations in severely mentally handicapped.

Haegeman, J., & Duyck, F. (1978) · PubMed · Cited by 13

Pipamperone (Dipiperon) in the treatment of behaviour disorders. A large-scale multicentre evaluation.

Deberdt, R. (1976) · PubMed · Cited by 12

Ritanserin, a new therapeutic approach for drug abuse. Part 3: Effects on fentanyl and sucrose

Meert, T. F., & Janssen, P. A. J. (1992) · Drug Development Research · doi:10.1002/ddr.430250106 · Cited by 12

5‐HT2A and D2 receptor blockade increases cortical DA release via 5‐HT1A receptor activation: a possible mechanism of atypical antipsychotic‐induced cortical dopamine release

Ichikawa, J., Ishii, H., Bonaccorso, S., Fowler, W. L., O'Laughlin, I. A., & Meltzer, H. Y. (2001) · Journal of Neurochemistry · doi:10.1046/j.1471-4159.2001.00154.x · Cited by 494

Pharmacology and behavioral pharmacology of the mesocortical dopamine system

Tzschentke, T. M. (2001) · Progress in Neurobiology · doi:10.1016/s0301-0082(00)00033-2 · Cited by 481

The "two-headed" latent inhibition model of schizophrenia: modeling positive and negative symptoms and their treatment

Weiner, I. (2003) · Psychopharmacology · doi:10.1007/s00213-002-1313-x · Cited by 391

Intra-prefrontal 8-OH-DPAT and M100907 improve visuospatial attention and decrease impulsivity on the five-choice serial reaction time task in rats

Winstanley, C. A., Chudasama, Y., Dalley, J. W., Theobald, D. E. H., Glennon, J. C., & Robbins, T. W. (2003) · Psychopharmacology · doi:10.1007/s00213-003-1398-x · Cited by 234

Neuropharmacology of second-generation antipsychotic drugs: a validity of the serotonin-dopamine hypothesis

KUROKI, T., NAGAO, N., & NAKAHARA, T. (2008) · Progress in brain research · doi:10.1016/s0079-6123(08)00910-2 · Cited by 146