Labrie F, Savary M, Coy D H, Coy E J, Schally A V
Endocrinology. 1976 Feb;98(2):289-94. doi: 10.1210/endo-98-2-289.
Sixteen synthetic analogs of LH-releasing hormone (LHRH) were tested for their ability to inhibit the stimulation of LH release induced by 3 X 10(-9)M LHRH in anterior pituitary cells in monolayer culture. Half-maximal inhibition of LHRH-induced LH release was obtained with 7 analogs at concentrations which ranged from 3 X 10(-6)M to 3 X 10(-5)M. None of these seven analogs had significant LH-releasing activity at concentrations up to 10-5M. Nine analogs had no detectable antagonistic activity when tested in up to a 3000-fold molar ratio of analog to LHRH.
对16种促黄体生成激素释放激素(LHRH)的合成类似物进行了测试,以考察它们抑制单层培养的垂体前叶细胞中由3×10⁻⁹M LHRH诱导的促黄体生成激素(LH)释放刺激的能力。7种类似物在浓度范围为3×10⁻⁶M至3×10⁻⁵M时,对LHRH诱导的LH释放产生了半数最大抑制。这7种类似物在浓度高达10⁻⁵M时均无显著的LH释放活性。当以高达类似物与LHRH 3000倍的摩尔比进行测试时,9种类似物未检测到拮抗活性。