RWJ-51204

RWJ-51204
	File:RWJ-51204.svg
Systematic (IUPAC) name
	5-ethoxymethyl-7-fluoro-3-oxo-1,2,3,5-tetrahydrobenzo[4,5] imidazo[1,2a]pyridine-4-N-(2-fluorophenyl)carboxamide
Identifiers
CAS Number	205701-85-5
Chemical data
Formula	C21H19F2N3O3
Molar mass	399.390 g/mol[[Script error: No such module "String".]]

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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 GABA_A 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. Anxioselective compounds acting at the GABA(A) receptor benzodiazepine binding site. Current Drug Targets. CNS and Neurological Disorders. 2003 Aug;2(4):213-32.
↑ 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. 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. Journal of Pharmacology and Experimental Therapeutics. 2002 Nov;303(2):777-90.
↑ Reitz AB, Jordan AD, Sanfilippo PJ, and Vavouyios-Smith A (1998) U.S. Patent 5,817,668.
↑ Cohen JH, Maryanoff CA, Stefanik SM, Sorgi KL, Villani FJ. Process research for the synthesis of RWJ-51204, a novel anxiolytic agent. Organic Process Research & Development. 1999; 3(4):260-265.

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[1] Atack JR. Anxioselective compounds acting at the GABA(A) receptor benzodiazepine binding site. Current Drug Targets. CNS and Neurological Disorders. 2003 Aug;2(4):213-32.

[2] 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. 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. Journal of Pharmacology and Experimental Therapeutics. 2002 Nov;303(2):777-90.

[3] Reitz AB, Jordan AD, Sanfilippo PJ, and Vavouyios-Smith A (1998) U.S. Patent 5,817,668.

[4] Cohen JH, Maryanoff CA, Stefanik SM, Sorgi KL, Villani FJ. Process research for the synthesis of RWJ-51204, a novel anxiolytic agent. Organic Process Research & Development. 1999; 3(4):260-265.

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RWJ-51204

References

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