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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 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.
|Related Dopamine Receptor Products|
ML417 is a highly selective and brain penetrant D3 dopamine receptor (D3R) agonist, with EC50 of 38 nM.
Cariprazine is a D2 and D3 receptor partial agonist, with high selectivity towards the D3 receptor.
PD-168077 maleate is a potent D4 dopamine receptor agonist (Ki = 8.7 nM), with > 400-fold and > 300-fold selectivity over D2 / D3 subtypes, respectively.
SCH23390 is a potent dopamine receptor antagonist (Ki values are 0.2 nM and 0.3 nM at D1 and D5 receptor sub-types, respectively).
MPTP hcl is a compound to the neurotoxin MPP+ which causes permanent symptoms of Parkinson's disease.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.