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Chemical compound
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
GABAA
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
^ Nakao T, Obata M, Kawakami M, Morita K, Tanaka H, Morimoto Y, et al. (October 1991).
"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.
doi :
10.1248/cpb.39.2556 .
PMID
1687209 .
^ Nakao T, Obata M, Yamaguchi Y, Marubayashi N, Ikeda K, Morimoto Y (January 1992).
"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.
doi :
10.1248/cpb.40.117 .
PMID
1349512 .
^ Yakushiji T, Shirasaki T, Munakata M, Hirata A, Akaike N (July 1993).
"Differential properties of type I and type II benzodiazepine receptors in mammalian CNS neurones" . British Journal of Pharmacology . 109 (3): 819–25.
doi :
10.1111/j.1476-5381.1993.tb13648.x .
PMC
2175650 .
PMID
8395299 .
^ Yasumatsu H, Morimoto Y, Yamamoto Y, Takehara S, Fukuda T, Nakao T, Setoguchi M (April 1994).
"The pharmacological properties of Y-23684, a benzodiazepine receptor partial agonist" . British Journal of Pharmacology . 111 (4): 1170–8.
doi :
10.1111/j.1476-5381.1994.tb14868.x .
PMC
1910153 .
PMID
7913372 .
^ Griebel G, Perrault G, Sanger DJ (April 1999). "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.
doi :
10.1016/s0091-3057(98)00209-3 .
PMID
10208374 .
S2CID
9894109 .
^ Griebel G, Perrault G, Tan S, Schoemaker H, Sanger DJ (September 1999). "Comparison of the pharmacological properties of classical and novel BZ-omega receptor ligands". Behavioural Pharmacology . 10 (5): 483–95.
doi :
10.1097/00008877-199909000-00007 .
PMID
10780255 .
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