促甲状腺激素释放激素硫代类似物及其非对映异构体的生物活性。
Biological activity of TRH thionalogue and its diastereoisomers.
作者信息
Alexandrová M, Strbák V, Herman Z S, Stachura Z, Kruszyński M
出版信息
Endocrinol Exp. 1987 Mar;21(1):43-9.
Binding affinity and TSH-releasing activity of [Prot3] TRH analogue (L-pyroglutamyl-L-histidyl-L-proline thioamide), TRH and their LDL and LLD diastereoisomers were compared in rats. Binding affinity and dose-related increase of TSH secretion were similar for both [Prot3] TRH and TRH. Moreover, similar effect of both peptides on sleeping time and motoric activity of rat was found. Substitution of L- for D-amino acids of TRH and [Prot3] TRH decreased the binding affinity and TSH-releasing activity as well. It was concluded that [Prot3] TRH analogue is as active as native TRH.
在大鼠中比较了[Prot3]TRH类似物（L-焦谷氨酰-L-组氨酰-L-脯氨酸硫代酰胺）、TRH及其LDL和LLD非对映异构体的结合亲和力和促甲状腺激素释放活性。[Prot3]TRH和TRH的结合亲和力以及促甲状腺激素分泌的剂量相关增加相似。此外，还发现两种肽对大鼠睡眠时间和运动活性的影响相似。将TRH和[Prot3]TRH中的L-氨基酸替换为D-氨基酸也会降低结合亲和力和促甲状腺激素释放活性。得出的结论是，[Prot3]TRH类似物与天然TRH具有相同的活性。
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