Substance P receptors in human pituitary: a potential inhibitor of luteinizing hormone secretion.
Substance P receptors in human pituitary: a potential inhibitor of luteinizing hormone secretion.
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人垂体中的 P 物质受体：黄体生成素分泌的潜在抑制剂。
DOI：
10.1210/jcem-69-3-612
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发表时间：
1989
期刊：
影响因子：
--
通讯作者：
B. Kerdelhué
中科院分区：
文献类型：
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作者：
P. Wormald;R. Millar;B. Kerdelhué
P 物质 (SP) 的特异性可饱和高亲和力受体存在于死后获得的人类垂体中。人垂体 SP 受体与 SP 及其两个类似物 [D-Tyr0]SP 和 [D-Tyr0,Nor,Leu11]SP 结合，具有相似的亲和力（Kd 分别为 1.76 X 10(-8)、3.53 X 10(-8) 和 1.93 X 10(-8) mol/L）。片段SP-(3-11)和SP-(7-10)对受体的亲和力比SP低(Kd分别为9.24×10(-8)和2.86×10(-7)mol/L)。 SP-(5-8)和SP-(1-4)与受体的结合较差(Kd大于10(-6)mol/L)。随着从分子的N-或C-末端去除氨基酸残基，结合逐渐减少，这与在大鼠中观察到的相似。 GnRH 和 TRH 不竞争 SP 结合位点。 SP能够以剂量依赖性方式抑制培养的人垂体细胞中GnRH刺激的LH分泌，同时对GnRH刺激的FSH分泌没有影响。 TSH、PRL、GH 和 ACTH 的基础释放不受 SP 的影响。这些发现表明 SP 可能在调节人类 LH 分泌中具有生理作用。
Specific saturable high affinity receptors for substance-P (SP) are present in human pituitaries obtained post-mortem. The human pituitary SP receptor bound SP and two of its analogs, [D-Tyr0]SP and [D-Tyr0,Nor,Leu11]SP, with similar affinities (Kd, 1.76 X 10(-8), 3.53 X 10(-8), and 1.93 X 10(-8) mol/L, respectively). The fragments SP-(3-11) and SP-(7-10) had lower affinities for the receptor than SP (Kd, 9.24 X 10(-8) and 2.86 X 10(-7) mol/L, respectively). SP-(5-8) and SP-(1-4) were poorly bound by the receptor (Kd, greater than 10(-6) mol/L). The progressive decrease in binding with the removal of amino acid residues from the N- or C-termini of the molecule is similar to that observed in the rat. GnRH and TRH did not compete for the SP-binding sites. SP was able to inhibit GnRH-stimulated LH secretion from cultured human pituitary cells in a dose-dependent manner, while having no effect on GnRH-stimulated FSH secretion. Basal release of TSH, PRL, GH, and ACTH was unaffected by SP. These findings suggest that SP may have a physiological role in the regulation of LH secretion in man.