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麦角新碱、洛林和多巴胺拮抗剂对大鼠垂体细胞催乳素体外释放的影响。

Effect of ergovaline, loline, and dopamine antagonists on rat pituitary cell prolactin release in vitro.

作者信息

Strickland J R, Cross D L, Birrenkott G P, Grimes L W

机构信息

Animal Science Department, College of Veterinary Medicine, University of Tennessee, Knoxville 37901-1071.

出版信息

Am J Vet Res. 1994 May;55(5):716-21.

PMID:8067623
Abstract

Cultured rat pituitary cells were studied to: determine the effects of ergovaline and loline on in vitro prolactin release; delineate the agonistic activity of these alkaloids at the D2 dopamine receptor, using 2 selective D2 dopamine receptor antagonists; and compare the efficacy of 2 dopamine receptor antagonists in reversing effects of the treatments on in vitro prolactin secretion. Ergovaline reduced in vitro prolactin release by at least 40% (P < 0.05) at concentrations of 10(-4), 10(-6), and 10(-8) M. However, loline reduced (P < 0.05) prolactin release only at the highest concentration, 10(-4) M. Two standard dopamine agonists, dopamine and alpha-ergocryptine, were used to verify that the inhibitory control mechanisms of in vitro prolactin release were intact. Both compounds reduced prolactin release by at least 40% for concentrations of 10(-4), 10(-6), or 10(-8) M. Selective D2 dopamine receptor antagonists (10(-6) M), domperidone and sulpiride, reversed (P < 0.05) the effect of loline on in vitro prolactin release. However, only domperidone (10(-6) M) was able to reverse (P < 0.05) the effect of ergovaline and only at the lowest ergovaline concentration (10(-8) M). Domperidone was more effective (P < 0.05) in reversing the prolactin-suppressing effect of alpha-ergocryptine than was sulpiride. The dose-response curve for domperidone (cubic fit, P < 0.0001) indicated a threshold concentration (10(-7) M) for reversal of alpha-ergocryptine's (10(-8) M) effect on prolactin release. However, at similar concentration of sulpiride (quadratic fit, P < 0.007), a threshold level was not obtained.(ABSTRACT TRUNCATED AT 250 WORDS)

摘要

对培养的大鼠垂体细胞进行研究,目的是:确定麦角新碱和洛林对体外催乳素释放的影响;使用两种选择性D2多巴胺受体拮抗剂,描述这些生物碱在D2多巴胺受体上的激动活性;比较两种多巴胺受体拮抗剂逆转这些处理对体外催乳素分泌影响的效果。麦角新碱在浓度为10^(-4)、10^(-6)和10^(-8) M时,可使体外催乳素释放减少至少40%(P < 0.05)。然而,洛林仅在最高浓度10^(-4) M时才使催乳素释放减少(P < 0.05)。使用两种标准多巴胺激动剂多巴胺和α-麦角隐亭来验证体外催乳素释放的抑制控制机制是否完整。两种化合物在浓度为10^(-4)、10^(-6)或10^(-8) M时,均可使催乳素释放减少至少40%。选择性D2多巴胺受体拮抗剂(10^(-6) M)多潘立酮和舒必利可逆转(P < 0.05)洛林对体外催乳素释放的影响。然而,只有多潘立酮(10^(-6) M)能够逆转(P < 0.05)麦角新碱的作用,且仅在最低麦角新碱浓度(10^(-8) M)时有效。在逆转α-麦角隐亭对催乳素的抑制作用方面,多潘立酮比舒必利更有效(P < 0.05)。多潘立酮的剂量反应曲线(三次拟合,P < 0.0001)表明,存在一个逆转α-麦角隐亭(10^(-8) M)对催乳素释放影响的阈值浓度(10^(-7) M)。然而,在舒必利的类似浓度下(二次拟合,P < 0.007),未获得阈值水平。(摘要截短为250字)

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