Effect of substance P/bombesin antagonists on the release of growth hormone by GHRP and GHRH.
Effect of substance P/bombesin antagonists on the release of growth hormone by GHRP and GHRH.
复制标题
P 物质/铃蟾肽拮抗剂对 GHRP 和 GHRH 释放生长激素的影响。
DOI：
10.1016/s0006-291x(05)81269-0
复制
发表时间：
1991
影响因子：
3.1
通讯作者：
Coy,DH
中科院分区：
文献类型：
--
作者：
Bitar,KG;Bowers,CY;Coy,DH
P(SP)/铃蟾肽 (Bn) 拮抗剂 [DArg1DTrp7,9Leu11]SP(P-7482)、[DArg1-DPro2DTrp7,9Leu11]SP (P-7483)、[DArg1DPhe5DTrp7,9Leu11]SP(P-7492) 和生长激素释放激素 (GHRH) 拮抗剂在 GHRH 和生长激素释放肽 HisDTrpAlaTrpDPheLysNH2 (GHRP) 存在的情况下，测试了 [DArg2Ala8,9,15]GHRH(1–29)(DC21-366) 对生长激素 (GH) 释放的体外影响。 P-7492、P-7483 和 P-7482 剂量依赖性地减少 GHRP 释放的 GH（IC50 分别为 0.2μM、0.85μM 和 6 μM）。即使在高剂量下，这些拮抗剂对 GHRH 刺激的 GH 释放也只有 10-15% 的抑制作用。 DC21-366 减少 GHRH 刺激的 GH 释放 (IC50=0.16 μM)，但不减少 GHRP 刺激的 GH 释放。 SP 和 Bn 在此系统中均没有 GH 释放或抑制作用。
The substance P(SP)/bombesin (Bn) antagonists [DArg1DTrp7,9Leu11]SP(P-7482), [DArg1-DPro2DTrp7,9Leu11]SP (P-7483), [DArg1DPhe5DTrp7,9Leu11]SP(P-7492), and the growth hormone releasing hormone (GHRH) antagonist [DArg2Ala8,9,15]GHRH(1–29)(DC21-366) were tested for theirin vitroeffects on the release of growth hormone (GH) in the presence of GHRH and growth hormone releasing peptide, HisDTrpAlaTrpDPheLysNH2(GHRP). P-7492, P-7483, and P-7482 decreased, dose-dependently, the release of GH by GHRP (IC50=0.2μM, 0.85μM, and 6 μM, respectively). These antagonists had only a 10–15% inhibitory effect on the stimulated GH release of GHRH even at high dosage. DC21-366 decreased the stimulated release of GH by GHRH (IC50=0.16 μM) but not by GHRP. Neither SP nor Bn had GH releasing or inhibitory effects in this system.