SCH 23390 hydrochloride is a potent dopamine receptor antagonist (Ki values are 0.2 nM and 0.3 nM at D1 and D5 receptor sub-types, respectively). SCH 23390 hydrochloride is also an agonist at 5-HT1C and 5-HT2C receptors in vitro (Ki values are 6.3 nM and 9.3 nM respectively). SCH 23390 hydrochloride blocks quinpirole-induced Kir3 (GIRK) currents (EC50 = 268 nM) independently of receptors.
The repeated administration of SCH 23390 (0.05 mg/kg s.c., thrice daily for 21 days) enhances the steady-state density of dopamine D1 receptors in the striatum (+30%) and substantia nigra (+24%). This treatment also increases the production rates of dopamine D1 receptors in the striatum (+44%) and substantia nigra (+54%).
|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||Water 30 mg/mL (with gentle warming)|
AF-DX 384 binding in rabbit cingulate cortex: two site kinetics and section autoradiography.
Dopke, et al. J Pharmacol Exp Ther. 1995;274: 562. PMID: 7616446.
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