(+)-SK&F 10047 hydrochloride
(Synonyms:(+)-N-烯丙基去甲蛋氨酰氮杂环辛四烯盐酸盐;(+)-N-烯丙基去甲美他佐辛盐酸盐;1-甲基-5-硝基-2-羟甲基咪唑)
目录号 : KG11331
CAS No. : 133005-41-1
纯度 : 98%
IC50: N/A
SKF 10047 hydrochloride is a prototypical σ1 receptor agonist. Behaviorally active in animal models of memory and stress. It has been fully demonstrated that σ binding sites are distinct from phencyclidine binding sites on the NMDA receptor-ion channel complex, which has investigated extensively the functional role of σ receptors in the central nervous system .
In vitro: The effects of the stereoisomers of N-allylnormetazocine (SKF-10,047) were compared in rats on the hippocampal cholinergic functions. A putative σ1 receptor agonist, (+)-SKF-10,047, increased hippocampal extracellular acetylcholine level as well as anti-amnesic effect against scopolamine-induced memory dysfunctions in rats. Haloperidol, a putative σ1 receptor antagonist reversed these phenomena which were not produced by (-)-SKF-10,047. Such stereoselectivity and antagonism imply σ1 receptors involved in these (+)-SKF-10,047-stimulated hippocampal cholinergic functions .
In vivo: (+)-SKF-10,047 and dextromethorphan, being co-administered with phenytoin (10 mg/kg, an anticonvulsant drug), decreased conditioned fear stress with low doses (4 and 20 mg/kg, respectively). The effects were antagonized by the σ receptor antagonists, NE-100 and BMY-14802. Furthermore, the effects of (+)-SKF-10,047 or dextromethorphan plus phenytoin were inhibited by the dopamine D1 receptor antagonist (SCH 23390) and the dopamine D2 receptor antagonist ((-)-sulpiride), and they were also decreased by 6-hydroxydopamine-induced lesions of dopaminergic neurons. The ameliorating effects of (+)-SKF-10,047 and dextromethorphan on condition of fear stress using high doses (5 and 30 mg/kg, respectively) were also inhibited by both the dopamine receptor antagonists .
Clinical trial: So far, no clinical study has been conducted.
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分子式 |
C17H23NO.HCl
|
分子量 |
293.84
|
CAS号 |
133005-41-1
|
中文名称 |
1-甲基-5-硝基-2-羟甲基咪唑
|
储存方式 |
Store at -20°C
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