H1-Histamine Receptor Affinity Predicts Short-Term Weight Gain for Typical and Atypical Antipsychotic Drugs

Allison DB, Mentore JL, Heo M, Chandler LP, Cappelleri JC, Infante MC et al (1999). Antipsychotic-induced weight gain: a comprehensive research synthesis. Am J Psychiatry 156: 1686–1696.

Altamura AC, Percudani M, Guercetti G, Invernizzi G (1989). Efficacy and tolerability of fluoxetine in the elderly: a double-blind study versus amitryptiline. Int Clin Psychopharmacol 4 (Suppl 1): 103–106.

Bolden C, Cusack B, Richelson E (1992). Antagonism by antimuscarinic and neuroleptic compounds at the five cloned human muscarinic cholinergic receptors expressed in Chinese hamster ovary cells. J Pharmacol Exper Therap 260: 576–580.

Burns CM, Chu H, Rueter SM, Hutchinson LK, Canton H, Sanders-Bush E et al (1997). Regulation of serotonin-2C receptor G-protein coupling by RNA editing. Nature 387: 303–308.

Canton H, Verriele L, Colpaert FC (1990). Binding of typical and atypical antipsychotics to 5-HT1C and 5-HT2 sites: clozapine potently interacts with 5-HT1C sites. Eur J Pharmacol 191: 93–96.

Fontaine KR, Heo M, Harrigan EP, Shear CL, Lakshminarayanan M, Casey DE et al (2001). Estimating the consequences of anti-psychotic induced weight gain on health and mortality rate. Psychiatry Res 101: 277–288.

Fukagawa K, Sakata T, Shiraishi T, Yoshimatsu H, Fujimoto K, Ookuma K et al (1989). Neuronal histamine modulates feeding behavior through H1-receptor in rat hypothalamus. Am J Physiol 256: R605–R611.

Glennon RA, Lee M, Rangisetty JB, Dukat M, Roth BL, Savage JE et al (2000). 2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors. J Med Chem 43: 1011–1018.

Herrick-Davis K, Grinde E, Teitler M (2000). Inverse agonist activity of atypical antipsychotic drugs at human 5-hydroxytryptamine2C receptors. J Pharmacol Exp Ther 295: 226–232.

Kane J, Honigfield G, Singer J, Meltzer HY, Group at CCS (1988). Clozapine for the treatment-resistant schizophrenic. Arch Gen Psychiatry 45: 789–796.

Lappalainen J, Zhang L, Dean M, Oz M, Ozaki N, Yu DH et al (1995). Identification, expression, and pharmacology of a Cys23-Ser23 substitution in the human 5-HT2c receptor gene (HTR2C). Genomics 27: 274–279.

Masaki T, Yoshimatsu H, Chiba S, Watanabe T, Sakata T (2001a). Central infusion of histamine reduces fat accumulation and upregulates UCP family in leptin-resistant obese mice. Diabetes 50: 376–384.

Masaki T, Yoshimatsu H, Chiba S, Watanabe T, Sakata T (2001b). Targeted disruption of histamine H1-receptor attenuates regulatory effects of leptin on feeding, adiposity, and UCP family in mice. Diabetes 50: 385–391.

McIntyre RS, McCann SM, Kennedy SH (2001). Antipsychotic metabolic effects: weight gain, diabetes mellitus, and lipid abnormalities. Can J Psychiatry 46: 273–281.

Meltzer HY (1999a). The role of serotonin in antipsychotic drug action. Neuropsychopharmacology 21: 106S–115S.

Meltzer HY (1999b). Suicide and schizophrenia: clozapine and the InterSePT study. International Clozaril/Leponex Suicide Prevention Trial. J Clin Psychiatry 60: 47–50.

Meltzer HY, Matsubara S, Lee J-C (1989). Classification of typical and atypical antipsychotic drugs on the basis of dopamine D-1, D-2 and serotonin2 pKi values. J Pharmacol Exper Therap 251: 238–246.

Meltzer HY, McGurk SR (1999). The effects of clozapine, risperidone, and olanzapine on cognitive function in schizophrenia. Schizophr Bull 25: 233–255.

Meltzer HY, Okayli G (1995). Reduction of suicidality during clozapine treatment of neuroleptic-resistant schizophrenia: impact on risk-benefit assessment. Am J Psychiatry 152: 183–190.

Meltzer HY, Park S, Kessler R (1999). Cognition, schizophrenia, and the atypical antipsychotic drugs. Proc Natl Acad Sci USA 96: 13591–13593.

Menon MK, Clark WG, Aures D (1971). Effect of thiazol-4-ylmethoxyamine, a new inhibition of histamine biosynthesis on brain histamine, monoamine levels and behavior. Life Sci I 10: 1097–1109.

Nguyen T, Shapiro DA, George SR, Setola V, Lee DK, Cheng R et al (2001). Discovery of a novel member of the histamine receptor family. Mol Pharmacol 59: 427–433.

Peroutka SJ, Synder SH, Snyder SH (1980). Relationship of neuroleptic drug effects at brain dopamine, serotonin, alpha-adrenergic, and histamine receptors to clinical potency. Long-term antidepressant treatment decreases spiroperidol-labeled serotonin receptor binding. Am J Psychiatry 137: 1518–1522.

Rauser L, Savage JE, Meltzer HY, Roth BL (2001). Inverse agonist actions of typical and atypical antipsychotic drugs at the human 5-hydroxytryptamine(2C) receptor. J Pharmacol Exp Ther 299: 83–89.

Reynolds GP, Zhang ZJ, Zhang XB (2002). Association of antipsychotic drug-induced weight gain with a 5-HT2C receptor gene polymorphism. Lancet 359: 2086–2087.

Roth BL, Ciaranello RD, Meltzer HY (1992). Binding of typical and atypical antipsychotic agents to transiently expressed 5-HT1C receptors. J Pharmacol Exp Ther 260: 1361–1365.

Roth BL, Craigo SC, Choudhary MS, Uluer A, Monsma Jr FJ, Shen Y et al (1994). Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors. J Pharmacol Exp Ther 268: 1403–1410.

Roth BL, Meltzer H, Khan N (1998). Binding of typical and atypical antipsychotic drugs to multiple neurotransmitter receptors. In: Goldstein DS, Eisen Hoffer G, Mc Carty R (eds). Advances in Pharmacology. Academic Press: San Diego, pp 482–485.

Rothman RB, Baumann MH, Savage JE, Rauser L, McBride A, Hufeisen SJ et al (2000). Evidence for possible involvement of 5-HT(2B) receptors in the cardiac valvulopathy associated with fenfluramine and other serotonergic medications. Circulation 102: 2836–2841.

Sakai N, Sakurai E, Onodera K, Asada H, Miura Y, Watanabe T (1995). Long-term depletion of brain histamine induced by alpha-fluoromethylhistidine increases feeding-associated locomotor activity in mice with a modulation of brain amino acid levels. Behav Brain Res 72: 83–88.

Sakata T, Ookuma K, Fukagawa K, Fujimoto K, Yoshimatsu H, Shiraishi T et al (1988). Blockade of the histamine H1-receptor in the rat ventromedial hypothalamus and feeding elicitation. Brain Res 441: 403–407.

Seeman P, Corbett R, van Tol HHM (1997). Atypical neuroleptics have low affinity for dopamine D2 receptors or are selective for D4 receptors. Neuropsychopharmacology 16: 93–135.

Seeman P, Lee T (1975). Antipsychotic drugs: direct correlation between clinical potency and presynaptic action on dopamine neurons. Science 188: 1217–1219.

Taylor DM, McAskill R (2000). Atypical antipsychotics and weight gain—a systematic review. Acta Psychiatr Scand 101: 416–432.

Tecott LH, Sun LM, Akana SF, Strack AM, Lowenstein DH, Dallman MF et al (1995). Eating disorder and epilepsy in mice lacking 5-HT2c serotonin receptors [see comments]. Nature 374: 542–546.

Van Tol HHM, Bunzow JR, Guan HC, Sunahara H-C, Seeman P, Niznik HB et al (1991). Cloning of the gene for a human dopamine D4 receptor with high affinity for the antipsychotic clozapine. Nature 350: 610–614.

Vickers SP, Clifton PG, Dourish CT, Tecott LH (1999). Reduced satiating effect of d-fenfluramine in serotonin 5-HT(2C) receptor mutant mice. Psychopharmacology (Berl) 143: 309–314.

Wetterling T (2001). Bodyweight gain with atypical antipsychotics. A comparative review. Drug Safety 24: 59–73.

Wood MD, Reavill C, Trail B, Wilson A, Stean T, Kennett GA et al (2001). SB-243213; a selective 5-HT2C receptor inverse agonist with improved anxiolytic profile: lack of tolerance and withdrawal anxiety. Neuropharmacology 41: 186–199.

Yamada M, Miyakawa T, Duttaroy A, Yamanaka A, Moriguchi T, Makita R et al (2001). Mice lacking the M3 muscarinic acetylcholine receptor are hypophagic and lean. Nature 410: 207–212.

Zeng XP, Le F, Richelson E (1997). Muscarinic m4 receptor activation by some atypical antipsychotic drugs. Eur J Pharmacol 321: 349–354.