RWJ-51204 is an anxiolytic drug used in scientific research. It has similar effects to benzodiazepine drugs, but is structurally distinct and so is classed as a nonbenzodiazepine anxiolytic.
RWJ-51204 is a nonselective partial agonist at GABAA receptors.[1] It produces primarily anxiolytic effects at low doses, with sedative, ataxia and muscle relaxant effects only appearing at some 20x the effective anxiolytic dose.[2] It was discovered by researchers at the pharmaceutical company Johnson & Johnson,[3][4] but its development has been discontinued.
References
- ^ Atack JR (August 2003). "Anxioselective compounds acting at the GABA(A) receptor benzodiazepine binding site". Current Drug Targets. CNS and Neurological Disorders. 2 (4): 213–32. doi:10.2174/1568007033482841. PMID 12871032.
- ^ Dubinsky B, Vaidya AH, Rosenthal DI, Hochman C, Crooke JJ, DeLuca S, DeVine A, Cheo-Isaacs CT, Carter AR, Jordan AD, Reitz AB, Shank RP (November 2002). "5-ethoxymethyl-7-fluoro-3-oxo-1,2,3,5-tetrahydrobenzo[4,5]imidazo[1,2a]pyridine-4-N-(2-fluorophenyl)carboxamide (RWJ-51204), a new nonbenzodiazepine anxiolytic". The Journal of Pharmacology and Experimental Therapeutics. 303 (2): 777–90. doi:10.1124/jpet.102.036954. PMID 12388665. S2CID 23880756.
- ^ US 5817668, Reitz AB, Jordan AD, Sanfilippo PJ, Vavouyios-Smith A, issued 6 October 1998, assigned to Ortho Pharma Corp
- ^ Cohen JH, Maryanoff CA, Stefanik SM, Sorgi KL, Villani FJ (1999). "Process research for the synthesis of RWJ-51204, a novel anxiolytic agent". Organic Process Research & Development. 3 (4): 260–265. doi:10.1021/op990182l.