SB242084 has anxiolytic effects, and enhances dopamine signalling in the limbic system, as well as having complex effects on the dopamine release produced by cocaine, increasing it in some brain regions but reducing it in others. It has been shown to increase the effectiveness of the selective serotonin reuptake inhibitor (SSRI) class of antidepressants, and may also reduce their side effects. In animal studies, SB-242,084 produced stimulant-type activity and reinforcing effects, somewhat similar to but much weaker than cocaine or amphetamines. SB 242084 is the first reported selective potent and brain penetrant 5-HT2C receptor antagonist and has anxiolytic-like activity, but does not possess either proconvulsant or hyperphagic properties which are characteristic of mutant mice lacking the 5-HT2C receptor.
|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.
SB 242084, a selective and brain penetrant 5-HT2C receptor antagonist.
Kennett GA, et al. Neuropharmacology. 1997 Apr-May;36(4-5):609-20. PMID: 9225286.
|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).
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.