EFFECTS OF BENZOIC-ACID AND ITS ANALOGS ON INSULIN AND GLUCAGON-SECRETION IN SHEEP

EFFECTS OF BENZOIC-ACID AND ITS ANALOGS ON INSULIN AND GLUCAGON-SECRETION IN SHEEP
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DOI:
10.1016/0014-2999(95)00192-n
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发表时间:
1995-07-04
影响因子:
5
通讯作者:
YANAIHARA, N
YANAIHARA, N
中科院分区:
医学2区
文献类型:
--
作者:
MINEO, H;OHDATE, T;YANAIHARA, N

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在清醒绵羊上研究了苯甲酸及其类似物对胰岛素和胰高血糖素分泌的影响。静脉注射苯甲酸以剂量依赖性方式增加血浆胰岛素和胰高血糖素浓度,在39-1250 μ mol/kg之间,增加两种激素的艾德(50)s约为625 μ mol/kg。给予苯甲酸的各种衍生物(625 μ mol/kg),并检查结构-活性关系。一个单一的羧基是必不可少的刺激胰岛素和胰高血糖素分泌,因为这两种激素的反应被废除的化合物,其中羧基被取代的磺酸或磷酸基团,或其中另一个羧基元素被引入(邻苯二甲酸)。在苯环上引入其他元素(氨基、羟基和卤素)的大多数化合物都具有改变的刺激活性。因此,绵羊的胰腺内分泌系统可以详细识别苯甲酸及其衍生物的化学结构,并诱导胰岛素和胰高血糖素的分泌。
The effects of benzoic acid and its analogues on insulin and glucagon secretion were investigated in conscious sheep. Intravenous injections of benzoic acid increased plasma insulin and glucagon concentrations in a dose-dependent manner between 39-1250 mu mol/kg, with ED(50)s for increasing both hormones of about 625 mu mol/kg. Various derivatives of benzoic acid (625 mu mol/kg) were administered and structure-activity relationships were examined. A single carboxylic group was essential for stimulating insulin and glucagon secretion, since both hormone responses were abolished with compounds in which the carboxylic group was replaced by sulfonic or phosphoric groups, or in which another carboxylic element was introduced (phthalic acids). Most of the compounds which introduced other elements (amino and hydroxy groups, and halogens) onto the benzene ring had an altered stimulating activity. Thus the pancreatic endocrine system can recognize the chemical structure of benzoic acid and its derivatives in detail and induce insulin and glucagon secretion in sheep.