Nakazawa M, Kobayashi T, Matsuno K, Mita S
Central Research Laboratories, Santen Pharmaceutical Co., Ltd., Higashiyodogawa, Osaka, Japan.
Pharmacol Biochem Behav. 1999 Jan;62(1):123-6. doi: 10.1016/s0091-3057(98)00146-4.
To clarify which subtype of sigma receptors is involved in the sigma receptor-mediated neck dystonia in rats, we examined whether 1-(3,4-dimethoxyphenethyl)-4-(3-phenylpropyl)piperazine dihydrochloride (SA4503), a selective sigma1 receptor agonist, and 1,3-di-(2-tolyl)guanidine (DTG), a sigma1 and sigma2 receptor agonist, induce neck dystonia in rats. Microinjection of SA4503 into the red nucleus of rat brain scarcely produced neck dystonia at the concentration of 10 nmol/0.5 microl. On the contrary, DTG produced significant dystonia at a concentrations of more than 5 nmol/0.5 microl. These results indicate that the sigma2 receptor subtype, but not sigma1 receptor subtype, may play an important role in the sigma receptor-mediated neck dystonia in rats.
为了阐明哪种亚型的σ受体参与了大鼠中σ受体介导的颈部肌张力障碍，我们研究了选择性σ1受体激动剂1-(3,4-二甲氧基苯乙基)-4-(3-苯丙基)哌嗪二盐酸盐(SA4503)和σ1及σ2受体激动剂1,3-二-(2-甲苯基)胍(DTG)是否会在大鼠中诱发颈部肌张力障碍。以10 nmol/0.5微升的浓度将SA4503微量注射到大鼠脑红核中几乎不会产生颈部肌张力障碍。相反，DTG在浓度高于5 nmol/0.5微升时会产生明显的肌张力障碍。这些结果表明，σ2受体亚型而非σ1受体亚型可能在大鼠中σ受体介导的颈部肌张力障碍中起重要作用。
