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鸡直肠对雷马克神经或嘌呤受体刺激的收缩反应:苏拉明的作用

Contractile responses of chicken rectum to stimulation of Remak's nerve or purinoceptors: effect of suramin.

作者信息

Bartlet A L

机构信息

Department of Preclinical Veterinary Sciences, University of Edinburgh, UK.

出版信息

J Pharm Pharmacol. 1992 Dec;44(12):986-9. doi: 10.1111/j.2042-7158.1992.tb07079.x.

Abstract

Stimulation of Remak's nerve produced a rapid contraction of the rectal muscle which was resistant to blockade by hyoscine, followed by a slow contractile response which was cholinergic. With hyoscine (1 microM) in the Tyrode solution, the non-cholinergic contractile response to nerve stimulation was compared with the responses to adenosine triphosphate (ATP) and alpha,beta-methylene adenosine triphosphate (alpha,beta-Me ATP). In the presence of suramin (300 microM), the contractile response to ATP was increased by about 100%, whereas that to nerve stimulation was inhibited by approximately 17%. Suramin (60 microM) also discriminated between the contractile responses to ATP and nerve stimulation, only the former being potentiated by the drug. It seems probable that suramin potentiated the action of ATP in the rectum through inhibition of ectonucleotidase activity. If so, the potentiation should not extend to alpha,beta-Me ATP, as this analogue of ATP is resistant to inactivation by the enzyme. Suramin inhibited the contractile response to alpha,beta-Me ATP. Thus the neurotransmitter which mediated the hyoscine-resistant contractile response to stimulation of Remak's nerve was dissimilar to ATP, in that it was not potentiated by suramin and presumably was not inactivated by ectonucleotidase activity.

摘要

刺激雷马克神经可使直肠肌肉快速收缩,该收缩对东莨菪碱的阻断具有抗性,随后是缓慢的收缩反应,此反应是胆碱能的。在台氏液中加入东莨菪碱(1微摩尔)后,将对神经刺激的非胆碱能收缩反应与对三磷酸腺苷(ATP)和α,β-亚甲基三磷酸腺苷(α,β-Me ATP)的反应进行比较。在有苏拉明(300微摩尔)存在的情况下,对ATP的收缩反应增加了约100%,而对神经刺激的反应则被抑制了约17%。苏拉明(60微摩尔)也区分了对ATP和神经刺激的收缩反应,只有前者被该药物增强。苏拉明似乎可能通过抑制胞外核苷酸酶活性来增强ATP在直肠中的作用。如果是这样,这种增强作用不应扩展到α,β-Me ATP,因为这种ATP类似物对该酶的失活具有抗性。苏拉明抑制了对α,β-Me ATP的收缩反应。因此,介导对雷马克神经刺激产生的东莨菪碱抗性收缩反应的神经递质与ATP不同,因为它不会被苏拉明增强,并且大概不会被胞外核苷酸酶活性失活。

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