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已知,长期用 GnRH 高活性类似物或拈抗性类似物治疗,能抑制雄大鼠生殖激素的功能和精子生成。这两种 GnRH 类似物的作用机制不同。高活性类似物(GnRH A)对生殖功能的影响至少有三种方式:(1)最初刺激、继而抑制促性腺激素(GTH)分泌;(2)最初 LH 分泌的过度刺激导致大鼠睾丸 LH/hCG 受体的减少;(3)GnRH A对性腺水平有直接作用。而拮抗性类似物(GnRHANT)对垂体水平只有抑制作用,可能由于抑制内源GnRH所致。Rivier 等报告,大鼠用 GnRHANT 长期治疗(每天1 mg),可失去交配行为,
It is known that long-term treatment with GnRH highly active analogs or transcripts can inhibit reproductive hormone function and sperm production in male rats. The mechanism of action of these two GnRH analogues is different. The effect of GnRH A on reproductive function is at least in three ways: (1) initial stimulation followed by inhibition of GTH secretion; (2) overstimulation of initial LH secretion leads to a decrease in LH / hCG Receptor reduction; (3) GnRH A has a direct effect on gonadal levels. The antagonistic analog (GnRHANT) only pituitary inhibitory effect may be due to inhibition of endogenous GnRH caused. Rivier et al reported that rats with long-term treatment with GnRHANT (1 mg daily), can lose the mating behavior,