Bissette G, Nemeroff C B, Loosen P T, Prange A J, Lipton M A
Pharmacol Biochem Behav. 1976;5(Suppl 1):135-8. doi: 10.1016/0091-3057(76)90342-7.
Various peptide hormones appear to exert behavioral and pharmacologic effects apart from their classical endocrine actions. Thytrotopin-releasing hormone (TRH), for example, antagonizes the sedation and hypothermia produced by barbiturate and other depressant drugs and de Wied has shown that ACTH 4-10, TRH, LHRH and certain related substances show some activity in inhibition of extinction of a pole-jumping avoidance response in the rat. These data provided the impetus for screening ACTH 4-10, LHRH, and related peptides for analeptic activity. ACTH 4-10 and ACTH 4-7 were inactive in antagonizing pentobarbital whether administered peripherally or centrally. ACTH 4-7 amide and 4-Met(O2), 8-D-Lys,9-Phe-ACTH 4-9 were active regardless of route of administration LHRH and two tripeptide fragments (pGlu-His-Trp-NH, and pGlu-His-Phe-NH2) showed analeptic activity only after intracisternal administration. Thus, some peptide fragments related to ACTH 4-10 and LHRH were shown to share to some degree the analeptic properties previously demonstrated for TRH.
各种肽类激素除了具有经典的内分泌作用外，似乎还发挥行为和药理作用。例如，促甲状腺激素释放激素（TRH）可拮抗巴比妥类药物和其他抑制性药物引起的镇静和体温过低，德维德发现促肾上腺皮质激素4-10（ACTH 4-10）、TRH、促黄体生成素释放激素（LHRH）及某些相关物质在抑制大鼠跳杆回避反应消退方面具有一定活性。这些数据为筛选ACTH 4-10、LHRH及相关肽类的兴奋活性提供了动力。ACTH 4-10和ACTH 4-7无论经外周还是中枢给药，在拮抗戊巴比妥方面均无活性。ACTH 4-7酰胺和4-甲硫氨酸（亚砜），8-D-赖氨酸，9-苯丙氨酸-ACTH 4-9无论给药途径如何均有活性。LHRH和两个三肽片段（焦谷氨酸-组氨酸-色氨酸-酰胺和焦谷氨酸-组氨酸-苯丙氨酸-酰胺）仅在脑池内给药后显示兴奋活性。因此，一些与ACTH 4-10和LHRH相关的肽片段在一定程度上具有先前已证明的TRH的兴奋特性。
