HYPERGLYCEMIA OF DIABETIC RATS DECREASED BY A GLUCAGON RECEPTOR ANTAGONIST

HYPERGLYCEMIA OF DIABETIC RATS DECREASED BY A GLUCAGON RECEPTOR ANTAGONIST
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DOI:
10.1126/science.6278587
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发表时间:
1982-01-01
期刊:
影响因子:
56.9
通讯作者:
TRIVEDI, D
TRIVEDI, D
中科院分区:
综合性期刊1区
文献类型:
--
作者:
JOHNSON, DG;GOEBEL, CU;TRIVEDI, D

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检查胰高血糖素类似物[1-N.α-三硝基苯基组氨酸,12-高精氨酸]-胰高血糖素(THG)降低链脲佐菌素糖尿病大鼠血糖浓度的能力。在体外,THG 是肝腺苷酸环化酶检测系统胰高血糖素激活的有效拮抗剂。静脉注射推注 THG 导致血糖短期快速下降 (20-35%)。连续输注低浓度抑制剂导致血糖持续大幅下降(30-65%)。胰高血糖素受体拮抗剂可以在不添加外源胰岛素的情况下显着降低糖尿病动物的血糖水平。
The glucagon analog [l-N.alpha.-trinitrophenylhistidine, 12-homoarginine]-glucagon (THG) was examined for its ability to lower blood glucose concentrations in rats made diabetic with streptozotocin. In vitro, THG is a potent antagonist of glucagon activation of the hepatic adenylate cyclase assay system. I.v. bolus injections of THG caused rapid decreases (20-35%) of short duration in blood glucose. Continuous infusion of low concentrations of the inhibitor led to larger sustained decreases in blood glucose (30-65%). A glucagon receptor antagonist can substantially reduce blood glucose levels in diabetic animals without addition of exogenous insulin.