Application

SB-277011-A hydrochloride hydrate may be used in D3 dopamine receptor-mediated cell signaling studies.

SB-277011-A hydrochloride hydrate has been used:as a dopamine D3 receptor-selective antagonist in rats to test its effect on 4-propyl-9-hydroxynaphthoxazine ([3H]-(+)-PHNO) radiotracer in cerebellum L9/10 and striatumas an acetylcholine inhibitor to test its negative allosteric modulation on Ascarissuumnicotinicacetylcholinereceptor (Asu-ACR-16) expressed inXenopusoocytes and its inhibitory effect on locomotion in Caenorhabditis elegansto test its effect on alcohol consumption in mice

Biochem/physiol Actions

SB-277011-A is a potent, selective brain-penetrant D3 dopamine receptor antagonist; 80-100x selective for D3 over D2; pKi = 7.95 for hD3 receptor.

The D₃ dopamine receptor antagonist, SB-277011-A inhibits the cocaine-seeking behavior and cocaine-enhances brain stimulation reward in in rats. It decreases drug-seeking behavior and may be useful in treatment of cocaine and methamphetamine addiction.

Features and Benefits

This compound is featured on the Dopamine Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

This compound was developed by GlaxoSmithKline. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Packaging

5, 25 mg in glass bottle