Y-23684 Explained

Y-23684 is an anxiolytic drug with a novel chemical structure, which is used in scientific research.^{[1] [2]} It has similar effects to benzodiazepine drugs, but is structurally distinct and so is classed as a nonbenzodiazepine anxiolytic.

Y-23684 is a nonselective partial agonist at GABA_A receptors. It has primarily anxiolytic and anticonvulsant effects, with sedative and muscle relaxant effects only appearing at higher doses. It produces little ataxia or potentiation of other sedatives such as ethanol or barbiturates when compared to the benzodiazepines diazepam and clobazam in animal tests.^{[3] [4] [5]}

Y-23684 has a favourable pharmacological profile, producing strong anxiolytic and moderate anticonvulsant effects at low doses that cause little or no sedative side effects. It has been proposed for development for human medical use, but has not yet gone beyond animal tests.^[6]

References

1. Nakao T, Obata M, Kawakami M, Morita K, Tanaka H, Morimoto Y, Takehara S, Yakushiji T, Tahara T . 6 . Studies on the synthesis of condensed pyridazine derivatives. IV. Synthesis and anxiolytic activity of 2-aryl-5,6-dihydro-(1)benzothiepino[5,4- c]pyridazin-3(2H)-ones and related compound . Chemical & Pharmaceutical Bulletin . 39 . 10 . 2556–63 . October 1991 . 1687209. 10.1248/cpb.39.2556 . free .
2. Nakao T, Obata M, Yamaguchi Y, Marubayashi N, Ikeda K, Morimoto Y . Synthesis and biological activities of optical isomers of 2-(4-chlorophenyl)-5,6-dihydro-(1)benzothiepino[5,4-c]pyridazin-3(2H)-o ne 7-oxide . Chemical & Pharmaceutical Bulletin . 40 . 1 . 117–21 . January 1992 . 1349512 . 10.1248/cpb.40.117 . free .
3. Yakushiji T, Shirasaki T, Munakata M, Hirata A, Akaike N . Differential properties of type I and type II benzodiazepine receptors in mammalian CNS neurones . British Journal of Pharmacology . 109 . 3 . 819–25 . July 1993 . 8395299 . 2175650 . 10.1111/j.1476-5381.1993.tb13648.x .
4. Yasumatsu H, Morimoto Y, Yamamoto Y, Takehara S, Fukuda T, Nakao T, Setoguchi M . The pharmacological properties of Y-23684, a benzodiazepine receptor partial agonist . British Journal of Pharmacology . 111 . 4 . 1170–8 . April 1994 . 7913372 . 1910153 . 10.1111/j.1476-5381.1994.tb14868.x .
5. Griebel G, Perrault G, Sanger DJ . Differences in anxiolytic-like profile of two novel nonbenzodiazepine BZ (omega) receptor agonists on defensive behaviors of mice . Pharmacology, Biochemistry, and Behavior . 62 . 4 . 689–94 . April 1999 . 10208374 . 10.1016/s0091-3057(98)00209-3 . 9894109 .
6. Griebel G, Perrault G, Tan S, Schoemaker H, Sanger DJ . Comparison of the pharmacological properties of classical and novel BZ-omega receptor ligands . Behavioural Pharmacology . 10 . 5 . 483–95 . September 1999 . 10780255 . 10.1097/00008877-199909000-00007 .