Asenapine(Org 5222) inhibits adrenergic receptor (α1, α2A, α2B, α2C) with Ki of 0.25-1.2 nM and also inhibits 5-HT receptor (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) with Ki of 0.03-4.0 nM.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||10mM in DMSO|
Asenapine versus placebo for schizophrenia.
Hay A, et al. Cochrane Database Syst Rev. 2015 Nov 24;(11):CD011458. PMID: 26599405.
|Related 5-HT Receptor Products|
MIN-101 (Roluperidone) is a novel compound with affinities for 5-HT2A and sigma-2 receptors with Ki values of 7.53 nM and 8.19 nM, respectively.
GSK163090 is a potent, selective, and orally active 5-HT1A/B/D receptor antagonist.
Eptapirone (F11440) is a potent 5HT(1A) receptor agonist with marked anxiolytic and antidepressant potential.
TG6-10-1 is a potent and selective antagonist for the prostaglandin E2 receptor subtype EP2.
WAY-100135 dihydrochloride is a potent, selective 5-HT1A receptor antagonist (IC50 = 15 nM).
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