Yeo T, Grossman A, Belchetz P, Besser G M
J Endocrinol. 1981 Oct;91(1):33-41. doi: 10.1677/joe.0.0910033.
The response of LH from a perfused column of dispersed rat anterior pituitary cells to LH releasing hormone (LH-RH) and the analogue, D-Ser(But)6-desGly10-Proethylamide9-LH-RH (Hoe 766), was investigated. Dose-response curves showed non-parallelism between LH-RH and the analogue. but it was evident that the analogue was considerably more potent. After a single pulse of LH-RH, LH output returned to basal values in 8 min; this was prolonged to 20 min in the case of the analogue. During this 20 min the cells were refractory to pulses of LH-RH but pulses of the analogue maintained output of LH. During constant-dose perfusion with either synthetic LH-RH or the analogue, output of LH rapidly reached a peak and then gradually fell over several hours to approach baseline values. However, a pulse of 50 mmol potassium chloride/l was still able to release LH at this time. The data are consistent with the view that this analogue of LH-RH is highly potent and is strongly bound by the LH-RH receptor. Furthermore, since it desensitizes the LH-RH receptor, it appears that continued turnover of either LH-RH or the analogue at the receptor is necessary for output of LH to be maintained.
研究了从分散的大鼠垂体前叶细胞灌注柱中释放的促黄体生成素（LH）对促黄体生成素释放激素（LH-RH）及其类似物D-丝氨酸（叔丁基）6-去甘氨酸10-脯氨酰胺9-LH-RH（Hoe 766）的反应。剂量反应曲线显示LH-RH与类似物之间不平行，但很明显该类似物的效力要强得多。给予单次LH-RH脉冲后，LH输出在8分钟内恢复到基础值；而类似物的情况下，这一过程延长至20分钟。在这20分钟内，细胞对LH-RH脉冲无反应，但类似物脉冲能维持LH的输出。在用合成LH-RH或类似物进行恒量灌注期间，LH输出迅速达到峰值，然后在数小时内逐渐下降至接近基线值。然而，此时50 mmol/L氯化钾脉冲仍能释放LH。这些数据与以下观点一致，即这种LH-RH类似物效力很高，且与LH-RH受体紧密结合。此外，由于它使LH-RH受体脱敏，似乎LH-RH或类似物在受体处持续更新对于维持LH输出是必要的。
