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西格玛1受体亚型与大鼠的刻板行为无关。

Sigma1 receptor subtype does not interact with stereotyped behaviors in rats.

作者信息

Kobayashi T, Matsuno K, Mita S

机构信息

Central Research Laboratories, Santen Pharmaceutical Co., Ltd., Higashiyodogawa, Osaka, Japan.

出版信息

Pharmacol Biochem Behav. 1998 Dec;61(4):381-4. doi: 10.1016/s0091-3057(98)00105-1.

Abstract

In the present study, we clearly showed that the sigma1 receptor subtype did not interact with the induction of stereotyped behaviors in rats. Namely, (+)-N-allylnormetazocine [(+)-SKF-10,047] (5.0, 10.0, and 20.0 mg/kg, SC), a traditional sigma receptor ligand that has affinities for the sigma1 receptor subtype and the N-methyl-D-aspartate (NMDA)/phencyclidine (PCP) receptor channel complex, markedly produced PCP-like stereotyped behaviors, such as head weaving, turning, and backpedaling, in rats. On the contrary, 1-(3,4-dimethoxyphenyl)-4-(3-phenylpropyl)piperazine dihydrochloride (SA4503), a potent and selective sigma1 receptor agonist, did not produce these behaviors. Additionally, PCP-induced stereotyped behaviors were significantly augmented by (+)-SKF-10,047, but not by SA4503. We thus suggest that the induction of PCP-like stereotyped behaviors elicited by (+)-SKF-10,047 closely interacts with NMDA/PCP receptor channel complex but not with the sigma1 receptor subtype.

摘要

在本研究中,我们明确表明西格玛1受体亚型与大鼠刻板行为的诱导无关。也就是说,(+)-N-烯丙基去甲美沙酮[(+)-SKF-10,047](5.0、10.0和20.0 mg/kg,皮下注射),一种对西格玛1受体亚型以及N-甲基-D-天冬氨酸(NMDA)/苯环利定(PCP)受体通道复合物具有亲和力的传统西格玛受体配体,能在大鼠中显著产生类似PCP的刻板行为,如头部摆动、转身和倒退。相反,1-(3,4-二甲氧基苯基)-4-(3-苯基丙基)哌嗪二盐酸盐(SA4503),一种强效且选择性的西格玛1受体激动剂,并未产生这些行为。此外,PCP诱导的刻板行为被(+)-SKF-10,047显著增强,但未被SA4503增强。因此,我们认为(+)-SKF-10,047引发的类似PCP的刻板行为的诱导与NMDA/PCP受体通道复合物密切相关,而与西格玛1受体亚型无关。

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