RWJ-51204

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RWJ-51204
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
ATC code  ?
PubChem  ?
Chemical data
Formula C21H19F2N3O3 
Mol. mass 399.390 g/mol
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.

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Legal status
Routes  ?

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

  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.
v • d • e
Psycholeptics: anxiolytics (tranquilisers) (N05B)
GABAA receptor
Adipiplon • Alpidem • CGS-9896 • CGS-20625 • DOV-51892 • ELB-139 • Etifoxine • L-838,417 • MK-0343 • NS-2664 • NS-2710 • Ocinaplon • Pagoclone • Panadiplon • Pipequaline • RWJ-51204 • SB-205,384 • TP-003 • TP-13 • TPA-023 • Tracazolate • Y-23684
Serotonin agonist
Histamine antagonist
Other/ungrouped
Dibenzobicyclooctadiene
Other


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