两种新型多巴胺激动剂，它们在体内作用时间长，但在体外作用时间短。

Two new dopamine agonists that are long acting in vivo but short acting in vitro.

作者信息

Grossman A, Yeo T, Delitala G, Hathway N R, Besser G M

出版信息

Clin Endocrinol (Oxf). 1980 Dec;13(6):595-9. doi: 10.1111/j.1365-2265.1980.tb03428.x.

DOI:10.1111/j.1365-2265.1980.tb03428.x

Abstract

The effects of two new ergolines, pergolide and CH29-717, on prolactin secretion in vitro and in vivo were compared with those of bromocriptine. Both ergolines had in vitro potencies similar to that of bromocriptine, but had a shorter duration of action. However, in vivo both were longer acting than bromocriptine after a single dose of 100 micrograms, and effectively suppressed prolactin secretion for greater than 24 h. It would appear that the pharmacokinetics of these ergolines are different to those of bromocriptine, and this may have considerable therapeutic importance.

摘要

将两种新的麦角碱（培高利特和CH29 - 717）在体外和体内对催乳素分泌的影响与溴隐亭的影响进行了比较。两种麦角碱在体外的效力与溴隐亭相似，但作用持续时间较短。然而，在体内，单次给予100微克后，两者的作用时间均比溴隐亭长，并且能有效抑制催乳素分泌超过24小时。看来这些麦角碱的药代动力学与溴隐亭不同，这可能具有相当大的治疗意义。