Laburthe M, Amiranoff B, Boige N, Rouyer-Fessard C, Tatemoto K, Moroder L
FEBS Lett. 1983 Aug 8;159(1-2):89-92. doi: 10.1016/0014-5793(83)80422-0.
GRF (10(-8) - 10(-5) M) is shown to inhibit competitively the binding of [125I]VIP to human and rat intestinal epithelial membranes. The affinity of GRF for VIP receptor is 700-800-times lower than that of VIP in both species. The order of affinity of different peptides is VIP greater than PHI greater than secretin greater than GRF in rat, and VIP greater than GRF greater than PHI greater than secretin in man. The important species specificity of VIP receptors in recognizing PHI and secretin does not occur in the case of GRF. GRF stimulates adenylate cyclase through its interaction with VIP receptors in rat and human membranes. However, while GRF behaves as a VIP agonist in human tissue, it is a partial agonist/antagonist of VIP in the rat.
已表明生长激素释放因子(GRF,10⁻⁸ - 10⁻⁵M)可竞争性抑制[¹²⁵I]血管活性肠肽(VIP)与人及大鼠肠上皮细胞膜的结合。在这两个物种中,GRF对VIP受体的亲和力比VIP低700 - 800倍。不同肽类的亲和力顺序在大鼠中为VIP>肽组氨酸异亮氨酸肽(PHI)>促胰液素>GRF,在人类中为VIP>GRF>PHI>促胰液素。VIP受体识别PHI和促胰液素时重要的物种特异性在GRF的情况下并不出现。GRF通过与大鼠和人类膜中的VIP受体相互作用来刺激腺苷酸环化酶。然而,虽然GRF在人体组织中表现为VIP激动剂,但在大鼠中它是VIP的部分激动剂/拮抗剂。