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Age-related change of the role of alpha1L-adrenoceptor in canine urethral smooth muscle.

机译:与年龄相关的α1L-肾上腺素受体在犬尿道平滑肌中的作用变化。

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摘要

To examine age-related alteration of the role of alpha1L-adrenoceptor in the urethra, young non-parous and aged parous female dogs were used. In a functional study, we evaluated phenylephrine-induced contraction and antagonistic effects of JTH-601, a newly synthesized alpha1-adrenoceptor antagonist, and prazosin; in a localization survey using autoradiographic technique, we investigated specific [3H]JTH-601 and [3H]tamsulosin binding. Concentration-response curves were obtained for phenylephrine (pD2 = 5.0-5.3). JTH-601 and prazosin antagonized this contraction with pA2 values of 8.2-8.3 and 8.0-8.1, respectively. Specific binding of both [3H]JTH-601 and [3H]tamsulosin were observed in the bladder neck and proximal section of urethra. There were no significant differences of the pD2, pA2, and radio ligand binding between young non-parous and aged parous dogs.
机译:为了检查与α1L-肾上腺素受体在尿道中的作用有关的年龄相关变化,使用了幼小的非雌性和老年性雌性狗。在一项功能研究中,我们评估了苯肾上腺素诱导的JTH-601(一种新合成的α1-肾上腺素受体拮抗剂)和哌唑嗪的收缩和拮抗作用。在使用放射自显影技术进行的定位调查中,我们研究了特定的[3H] JTH-601和[3H]坦索罗辛结合。获得了苯肾上腺素的浓度-响应曲线(pD2 = 5.0-5.3)。 JTH-601和prazosin分别以8.2-8.3和8.0-8.1的pA2拮抗这种收缩。在膀胱颈部和尿道近端观察到了[3H] JTH-601和[3H]坦洛新的特异性结合。在非幼犬和成年幼犬之间,pD2,pA2和放射性配体结合没有显着差异。

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