Asenapine - CAS 85650-56-2
Catalog number: 85650-56-2
Category: Inhibitor
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5-HT Receptor
Asenapine is a high-affinity antagonist of serotonin, norepinephrine, dopamine and histamine receptors, used for the treatment of schizophrenia and acute mania associated with bipolar disorder.
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1.Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds.
Richelson E;Souder T Life Sci. 2000 Nov 24;68(1):29-39.
Using radioligand binding assays and post-mortem normal human brain tissue, we obtained equilibrium dissociation constants (K(d)s) for nine new antipsychotic drugs (iloperidone, melperone, olanzapine, ORG 5222, quetiapine, risperidone, sertindole, ziprasidone, and zotepine), one metabolite of a new drug (9-OH-risperidone), and three older antipsychotics (clozapine, haloperidol, and pimozide) at nine different receptors (alpha1-adrenergic, alpha2-adrenergic, dopamine D2, histamine H1, muscarinic, and serotonin 5-HT1A, 5-HT1D, 5-HT2A, and 5-HT2C receptors). Iloperidone was the most potent drug at the two adrenergic receptors. ORG 5222 was the most potent drug at dopamine D2 and 5-HT2c receptors, while ziprasidone was the most potent compound at three serotonergic receptors (5-HT1A, 5-HT1D, and 5-HT2A). At the remaining two receptors, olanzapine was the most potent drug at the histamine H1 receptor (Kd=0.087 nM); clozapine at the muscarinic receptor (Kd=9 nM). Certain therapeutic and adverse effects, as well as certain drug interactions can be predicted from a drug's potency for blocking a specific receptor. These data can provide guidelines for the clinician in the choice of antipsychotic drug.
2.Neurochemical studies with the potential antipsychotic compound trans-5-Chloro-2-methyl-2,3,3a,12b-tetrahydro-1H- dibenz[2,3:6,7]oxepino[4,5-c]pyrrolidine maleate.
De Boer T;Tonnaer JA;De Vos CJ;Van Delft AM Arzneimittelforschung. 1990 May;40(5):550-4.
trans-5-Chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenz [2,3:6,7]oxepino[4,5-c]pyrrolidine maleate (Org 5222) has dopamine D2 antagonistic and negligible anticholinergic properties of the classical neuroleptic haloperidol. In addition it combines the strong antiserotonergic and antihistaminergic properties of chlorpromazine and clozapine with the potent dopamine D-1 antagonistic properties of Sch 23390 (R-(+)-delta-chloro-2,3,4,5-tetrahydro-3-methyl-5- phenyl-1H-3-benazepin-7-ol(Z)-2-buteneoate). This in conjunction to its behavioural properties, warrants clinical testing in psychotic patients.
3.The effects of antipsychotics with 5-HT(2C) receptor affinity in behavioral assays selective for 5-HT(2C) receptor antagonist properties of compounds.
Prinssen EP;Koek W;Kleven MS Eur J Pharmacol. 2000 Jan 24;388(1):57-67.
Many antipsychotics have marked antagonist effects at 5-hydroxytryptamine (5-HT(2C)) receptors in vitro, which, however, have been difficult to show in behavioral assays. Here, we used two assays - hypolocomotion and hypophagia induced by the 5-HT(2C) receptor agonist 1-(3-chlorophenyl)piperazine (mCPP) - to try to characterize the 5-HT(2C) receptor antagonist properties of antipsychotics in vivo. Clozapine, olanzapine, pipamperone, and trans-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenz-[2,3:6, 7]oxepino[4,5-C] pyrrolidino maleate (ORG 5222), modestly, but significantly, attenuated mCPP (10 mg/kg)-induced hypolocomotion. In contrast, risperidone and loxapine were inactive. The putative antipsychotic ORG 5222 significantly attenuated mCPP (5 mg/kg)-induced hypophagia, whereas the other antipsychotics were inactive. Selective antagonists at dopamine D(2)-like receptors, alpha(1)-adrenoceptors, alpha(2)-adrenoceptors, or muscarinic receptors were not able to antagonize the effects of mCPP in either assay. The results suggest that mCPP-induced hypolocomotion can be used to characterize the 5-HT(2C) receptor antagonist properties of antipsychotics, whereas mCPP-induced hypophagia appeared to be sensitive only to compounds highly selective for 5-HT(2C) receptors.
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CAS 85650-56-2 Asenapine

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