β-肾上腺素能受体拮抗剂对雌激素主导的兔子宫中异丙肾上腺素反应的作用。

Action of beta-adrenoceptor antagonists on the response to isoprenaline in the oestrogen dominated rabbit uterus.

作者信息

Nesheim B I

出版信息

Br J Pharmacol. 1975 Mar;53(3):393-401. doi: 10.1111/j.1476-5381.1975.tb07375.x.

DOI:10.1111/j.1476-5381.1975.tb07375.x

PMID:236797

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1666435/

Abstract

Log dose-response curves to isoprenaline from spontaneously contracting muscle strips from rabbit uterus have been obtained. The effects of the alpha-adrenoceptor antagonists phentolamine and phenoxybenzamine, the beta- adrenoceptor antagonists propranolol and practolol, and (+)-propranolol on the log dose-response curves were studied. 2. Phentolamine 5.3 times 10- minus 7 M had a stimulating effect on the muscle strips, moving the log dose-response curve of isoprenaline to the right. Phenoxybenzamine 2.9 times 10- minus 5 M had no effect on the curves. 3. Propranolol 3.4 times 10- minus 6 M had no effect on the curves from circular muscle strips, with either phentolamine 5.4 times 10- minus 7 M or with phenoxybenzamine 2.9 times 10- minus 5 M as alpha-blocker. The curves from the longitudinal muscle strips were shifted somewhat to the right, the same shift, however, being obtained with (+)-propranolol 3.4 times 10- minus 6 M. 4. Practolol 3.8 times 10- minus 6, 3.8 times 10- minus 5 and 3.8 times 10- minus 4 M was without effect on the curves, either in the circular or in the longitudinal strips. 5. It is concluded that neither propranolol at 3.4 times 10- minus 6 M nor practolol act as beta-adrenoceptor antagonists in oestrogen dominated rabbit uterus. In all other tissues investigated, propranolol or practolol block the effect of isoprenaline. Whether the effect of isoprenaline in this tissue may be termed a beta-effect, is then a question of definition. In addition there is no evidence for any extraneuronal uptake mechanisms for isoprenaline. 6. Variations in sensitivity to beta-stimulation with the time of the year were observed, the sensitivity being greatest in the winter and lowest in the summer.

摘要

已获得兔子宫自发收缩肌条对异丙肾上腺素的对数剂量-反应曲线。研究了α-肾上腺素能拮抗剂酚妥拉明和酚苄明、β-肾上腺素能拮抗剂普萘洛尔和醋丁洛尔以及（+）-普萘洛尔对对数剂量-反应曲线的影响。2. 5.3×10⁻⁷ M的酚妥拉明对肌条有刺激作用，使异丙肾上腺素的对数剂量-反应曲线右移。2.9×10⁻⁵ M的酚苄明对曲线无影响。3. 3.4×10⁻⁶ M的普萘洛尔，无论是与5.4×10⁻⁷ M的酚妥拉明还是与2.9×10⁻⁵ M的酚苄明作为α-阻滞剂联合使用时，对环形肌条的曲线均无影响。纵行肌条的曲线略有右移，然而，3.4×10⁻⁶ M的（+）-普萘洛尔也能产生相同程度的右移。4. 3.8×10⁻⁶ M、3.8×10⁻⁵ M和3.8×10⁻⁴ M的醋丁洛尔，无论是对环形肌条还是纵行肌条的曲线均无影响。5. 得出的结论是，在雌激素占主导的兔子宫中，3.4×10⁻⁶ M的普萘洛尔和醋丁洛尔均不表现为β-肾上腺素能拮抗剂的作用。在所有其他研究的组织中，普萘洛尔或醋丁洛尔可阻断异丙肾上腺素的作用。异丙肾上腺素在该组织中的作用是否可称为β-效应，这是一个定义问题。此外，没有证据表明存在异丙肾上腺素的任何非神经摄取机制。6. 观察到对β-刺激的敏感性随一年中的时间而变化，冬季敏感性最高，夏季最低。