Pharmacologic characterization of excitatory and inhibitory cholecystokinin receptors of the cat gallbladder and sphincter of Oddi.
Pharmacologic characterization of excitatory and inhibitory cholecystokinin receptors of the cat gallbladder and sphincter of Oddi.
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猫胆囊和 Oddi 括约肌的兴奋性和抑制性胆囊收缩素受体的药理学特征。
DOI：
10.1016/0016-5085(87)90030-8
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发表时间：
1987
期刊：
影响因子：
29.4
通讯作者：
P. Biancani
中科院分区：
文献类型：
--
作者：
J. Behar;P. Biancani
通过测试各种硫酸化和脱硫 CCK 级分以及使用特定的 CCK-胃泌素拮抗剂，研究了胆道缩胆囊素 (CCK) 受体的药理学特性和特异性。硫酸化 CCK-7 (5-80 pmol/kg) 引起胆囊收缩和 Oddi 括约肌松弛。河豚毒素去神经使胆囊反应降低了 50%，并使 Oddi 括约肌反应从松弛变为收缩。脱硫 CCK-7 (80-400 pmol/kg) 会导致胆囊收缩微弱，但不受河豚毒素的影响。胆囊对 CCK-3 (10-80 nmol/kg) 或 CCK-2 (10-160 nmol/kg) 剂量完全松弛 Oddi 括约肌没有反应。然而，这些剂量比硫酸化 CCK-7 的最大剂量高 5-2000 倍。用河豚毒素去神经后，即使剂量比硫酸化 CCK-7 最大剂量大五倍，脱硫 CCK-7 (10-400 pmol/kg) 也会诱导 Oddi 括约肌收缩较弱。去神经的 Oddi 括约肌对 CCK-3 (10-80 nmol/kg) 或 CCK-2 (10-160 nmol/kg) 没有反应。此外，连续输注丙谷胺（5-20 mg/kg·min）和推注二丁酰环鸟苷单磷酸（250-1000 μg/kg）可阻断硫酸化CCK-8对胆囊和Oddi括约肌的作用。然而，需要更高剂量的这些拮抗剂来阻断 CCK 对 Oddi 括约肌的作用，而不是对胆囊的作用。相反，高剂量的脱硫CCK-7（100 pmol/kg）或CCK-3（200 nmol/kg）并不能拮抗硫酸化CCK-8（10-80 pmol/kg）对胆囊的作用。这些发现表明存在三组特定的 CCK 受体，其分子构型要求由这些受体所在的细胞类型决定：节后胆碱能神经元、胆囊平滑肌细胞和 Oddi 括约肌，或节后非胆碱能、非肾上腺素能抑制神经元。
The pharmacologic properties and specificity of cholecystokinin (CCK) receptors of the biliary tract were investigated by testing various sulfated and desulfated CCK fractions and by using specific CCK-gastrin antagonists. Sulfated CCK-7 (5–80 pmol/kg) caused gallbladder contraction and sphincter of Oddi relaxation. Denervation with tetrodotoxin decreased the gallbladder response by 50% and changed the sphincter of Oddi response from relaxation to contraction. Desulfated CCK-7 (80–400 pmol/kg) caused a weak gallbladder contraction that was unaffected by tetrodotoxin. The gallbladder did not respond to CCK-3 (10–80 nmol/kg) or to CCK-2 (10–160 nmol/kg) in doses that completely relaxed the sphincter of Oddi. These doses, however, were 5–2000 times higher than the maximal dose of sulfated CCK-7. After denervation with tetrodotoxin, desulfated CCK-7 (10–400 pmol/kg) induced a weak sphincter of Oddi contraction even with doses five times greater than the maximal dose of sulfated CCK-7. The denervated sphincter of Oddi did not respond to CCK-3 (10–80 nmol/kg) or CCK-2 (10–160 nmol/kg). Furthermore, a continuous proglumide infusion (5–20 mg/kg · min) and bolus doses of dibutyryl cyclic guanosine monophosphate (250–1000 μg/kg) blocked the effect of sulfated CCK-8 on the gallbladder and sphincter of Oddi. Higher doses of these antagonists were needed, however, to block the CCK effect on the sphincter of Oddi than on the gallbladder. In contrast, high doses of desulfated CCK-7 (100 pmol/kg) or CCK-3 (200 nmol/kg) did not antagonize the effect of sulfated CCK-8 (10–80 pmol/kg) on the gallbladder. These findings suggest the existence of three sets of specific CCK receptors with molecular configuration requirements determined by the type of cell where these receptors are located: on the postganglionic cholinergic neurons, on the smooth muscle cells of the gallbladder, and sphincter of Oddi, or on the postganglionic noncholinergic, nonadrenergic inhibitory neurons.
二丁酰环鸟苷 3:5-单磷酸和胆囊收缩素之间的可溶性相互作用：抑制胆囊收缩素活性的可能机制。
影响因子：
29.4
作者：
Miller,LJ;Reilly,WM;Rosenzweig,SA;Jamieson,JD;Go,VL
通讯作者：
Go,VL