Methiothepin attenuates gastric secretion and motility effects of vagal stimulants at the dorsal vagal complex.
Methiothepin attenuates gastric secretion and motility effects of vagal stimulants at the dorsal vagal complex.
复制标题
甲硫替平减弱迷走神经刺激物对背侧迷走神经复合体的胃分泌和运动作用。
DOI：
10.1016/s0014-2999(01)01579-5
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发表时间：
2002
影响因子：
5
通讯作者：
StephensJr,RobertL
中科院分区：
文献类型：
--
作者：
Varanasi,Sridhar;Chi,Jinhan;StephensJr,RobertL
采用非选择性5-羟色胺受体拮抗剂甲氧thepin研究5-羟色胺对背迷走神经复合体-促甲状腺激素类似物刺激胃功能参数的调节作用。内源性甲氧thepin预处理（200,0.1 nmol）对TRH类似物p-Glu-His-（3,3′-二甲基）- pro NH2的抑制作用显著（分别为70%和44%）；RX 77368 (12 pmol)]诱导的胃酸输出量。脑内预处理甲基塞吉特（非特异性5-HT受体拮抗剂）或联合cyanopindolol （5-HT1A和1b受体拮抗剂）+利坦色林（5- ht2家族受体拮抗剂）不改变背迷走神经复合物- rx 77368的反应。单侧迷走背复合物经甲氧thepin （50 nmol/50 nl）预处理后，同侧迷走背复合物- trh类似物（12 pmol）的胃分泌反应降低57%。经胃内胆背髓甲素（0.1 nmol/10 μl）预处理后，胃促分泌反应（由TRH释放到迷走背复核介导）被抑制50%。内源性甲氧thepin （200 nmol/20 μl）对(a)背迷走神经复合物-谷氨酸（60 nmol/30 nl）刺激的胃酸分泌和(b)背迷走神经复合物- rx 77368 （12 pmol/30 nl）刺激的胃动力也有减弱作用。这些数据表明，除其5-HT受体拮抗剂作用外，甲氧thepin的其他特性介导了其对迷走背复合体的抑制作用。
Methiothepin, a nonselective 5-HT receptor antagonist was utilized to explore the 5-HT modulation of dorsal vagal complex–TRH (thyrotropin releasing hormone) analogue stimulated gastric functional parameters. Intracisternal methiothepin pretreatment (200, 0.1 nmol) produced significant inhibition (70%, 44%, respectively) of the TRH analogue [p-Glu-His-(3,3′-dimethyl)-Pro NH2; RX 77368 (12 pmol)]-induced gastric acid output compared to vehicle pretreatment. Intracisternal pretreatment with methysergide (nonspecific 5-HT receptor antagonist) or combined cyanopindolol (5-HT1A and 1Breceptor antagonist)+ritanserin (receptor antagonist of the 5-HT2family) did not alter the dorsal vagal complex–RX 77368 response. Unilateral dorsal vagal complex pretreatment with methiothepin (50 nmol/50 nl) attenuated ipsilateral dorsal vagal complex–TRH analog (12 pmol) induced gastric secretory response by 57%. The gastric secretagogue response to stimulation of the raphe obscurus (mediated by TRH release into the dorsal vagal complex) was inhibited 50% by pretreatment with intracisternal dorsal medullary methiothepin (0.1 nmol/10 μl). Intracisternal methiothepin (200 nmol/20 μl) also attenuated (a) dorsal vagal complex–glutamate (60 nmol/30 nl) stimulated gastric acid secretion and (b) gastric motility stimulated by dorsal vagal complex–RX 77368 (12 pmol/30 nl). The data suggest that other properties of methiothepin, alone or in addition to its 5-HT receptor antagonist effect, mediate its inhibitory actions at the dorsal vagal complex.