NATURE OF THE HEPATIC RECEPTORS INVOLVED IN VASOPRESSIN-INDUCED GLYCOGENOLYSIS
NATURE OF THE HEPATIC RECEPTORS INVOLVED IN VASOPRESSIN-INDUCED GLYCOGENOLYSIS
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DOI：
10.1016/0304-4165(79)90371-4
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发表时间：
1979-01-01
期刊：
影响因子：
--
通讯作者：
DEWULF, H
中科院分区：
文献类型：
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作者：
KEPPENS, S;DEWULF, H
精氨酸加压素的血管加压效力与14种结构类似物[（Arg 8）催产素;（Lys 8）加压素;（1，6-α-氨基）-精氨酸]之间存在密切相关性。脱氨基胱硫醚，Orn 8）加压素; 1-脱氨基-（Arg 8）催产素;（1，6-α- 1-脱氨基-（Thr 4）催产素;催产素;（D-Arg 8）加压素; 1-脱氨基-（D-Arg 8）加压素;（Val 4，D-Arg 8）加压素; 1-脱氨基-（Val 4，D-Arg 8）加压素; 1-脱氨基-（Thr 4，D-Arg 8）加压素; 1-L-2-羟基巯基丙酸，Arg 8-加压素]及其激活离体大鼠肝细胞中糖原磷酸化酶的能力;与类似物的已知抗利尿活性无关。表征5种类似物[（1-（β-D-1）]的已知抗加压剂能力的pA 2值巯基-β，.贝塔环戊亚甲基丙酸）Val 4，D-Arg 8）加压素;（1-脱氨基青霉胺，Thr 4）催产素; 1（脱氨基青霉胺，Val 4，D-Arg 8）加压素;（1-脱氨基青霉胺，2-（O-Me）Tyr，Arg 8）-加压素]对加压素的作用接近于它们抑制加压素诱导的肝糖原磷酸化酶活化所获得的那些。负责血管加压素糖原分解活性的肝受体显然与负责体内升压活性的肝受体具有相同的特征并与其相关。
There is a close correlation between the vasopressor potency of arginine vasopressin and 14 structural analogs [(Arg8)vasotocin; (Lys8) vasopressin; (1,6-.alpha.-deaminocystathionine, Orn8)vasopressin; 1-deamino-(Arg8)vasotocin; (1,6-.alpha.-deaminocystathionine, Arg8)vasopressin; 1-deamino-(Thr4)vasotocin; oxytocin; (D-Arg8)vasopressin; 1-deamino-(D-Arg8)vasopressin; (Val4,D-Arg8)vasopressin; 1-deamino-(Val4,D-Arg8)vasopressin; 1-deamino-(Thr4,D-Arg8)vasopressin; 1-L-2-hydroxymercaptopropanoic acid, Arg8-vasopressin] and their ability to activate glycogen phosphorylase in isolated rat hepatocytes; there is no relation with the known antidiuretic activity of the analogs. The pA2 values characterizing the known antivasopressor capacity of 5 analogs [(1-(.beta.-mercapto-.beta.,.beta.-cyclopentamethylenepropionic acid) Val4,D-Arg8)vasopressin; (1-deaminopenicillamine, Thr4)oxytocin; 1(deaminopenicillamine, Val4,D-Arg8)vasopressin; (1-deaminopenicillamine, 2-(O-Me)Tyr, Arg8)-vasopressin] against vasopressin were close to those obtained for their inhibition of the vasopressin-induced activation of hepatic glycogen phosphorylase. The hepatic receptors responsible for the glycogenolytic activity of vasopressin apparently share characteristics with and are related to those responsible for pressor activity in vivo.