Huhtaniemi I T, Stewart J M, Channabasavaiah K, Fraser H M, Clayton R N
Mol Cell Endocrinol. 1984 Feb;34(2):137-43. doi: 10.1016/0303-7207(84)90065-0.
The effects of a GnRH antagonist analogue (N-acetyl-Ala1,D-p-Cl-Phe2,D-Trp3,6-GnRH, Ant.) and a GnRH antiserum (A/S) on the development of pituitary-testicular function were studied in immature (23/24-31/32-day-old) rats. In another experiment the Ant. treatment was combined with bromocriptine (BR)-induced hypoprolactinaemia. Ant. and A/S decreased serum and pituitary levels of LH and FSH, and BR those of Prl (P less than 0.01-0.05). Testicular testosterone (T) and progesterone (P) contents were significantly decreased only by Ant. (P less than 0.01). Ant. decreased the weights of the testes, ventral prostates and seminal vesicles, as well as testicular LH, FSH and Prl receptors (R) (P less than 0.01-0.05). BR decreased LH-R but had no effect on Prl-R. Both Ant. and A/S decreased available pituitary GnRH-R (P less than 0.01), but free testicular GnRH-R were reduced only by Ant. BR increased GnRH receptors in the pituitaries. It is concluded that Ant.-induced low gonadotropin levels in immature animals inhibit the developmental increase of testicular weight, gonadotropin and Prl-R, steroidogenesis and androgen action on accessory sex glands. Hypoprolactinaemia had an additive inhibitory effect to the antigonadal effects of Ant. The testis tissue of immature (23/24-day-old) animals already contains GnRH-R. In general, developing animals are clearly very sensitive to the antigonadal actions of Ant. and BR, whereas the effect of GnRH-A/S is less pronounced than in adults.
在未成熟(23/24至31/32日龄)大鼠中研究了促性腺激素释放激素(GnRH)拮抗剂类似物(N-乙酰基-Ala1,D-对氯苯丙氨酸2,D-色氨酸3,6-GnRH,Ant.)和GnRH抗血清(A/S)对垂体-睾丸功能发育的影响。在另一项实验中,将Ant.治疗与溴隐亭(BR)诱导的低催乳素血症相结合。Ant.和A/S降低了血清和垂体中促黄体生成素(LH)和促卵泡生成素(FSH)的水平,而BR降低了催乳素(Prl)的水平(P<0.01至0.05)。仅Ant.显著降低了睾丸睾酮(T)和孕酮(P)的含量(P<0.01)。Ant.降低了睾丸、腹侧前列腺和精囊的重量,以及睾丸LH、FSH和Prl受体(R)(P<0.01至0.05)。BR降低了LH-R,但对Prl-R没有影响。Ant.和A/S均降低了垂体中可用的GnRH-R(P<0.01),但仅Ant.降低了睾丸中游离的GnRH-R。BR增加了垂体中的GnRH受体。得出的结论是,Ant.诱导的未成熟动物低促性腺激素水平抑制了睾丸重量、促性腺激素和Prl-R的发育性增加、类固醇生成以及雄激素对附属性腺的作用。低催乳素血症对Ant.的抗性腺作用具有累加抑制作用。未成熟(23/24日龄)动物的睾丸组织中已经含有GnRH-R。一般来说,发育中的动物对Ant.和BR的抗性腺作用明显非常敏感,而GnRH-A/S的作用不如在成年动物中明显。