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[毒蕈碱受体亚型在猫气管黏膜下腺分泌中的作用]

[The role of muscarinic receptor subtypes in feline tracheal submucosal gland secretion].

作者信息

Ishihara H, Shimura S

机构信息

First Department of Internal Medicine, Tohoku University School of Medicine.

出版信息

Nihon Kyobu Shikkan Gakkai Zasshi. 1992 Dec;30 Suppl:65-9.

PMID:1306240
Abstract

To determine what muscarinic receptor subtype regulates the rise of intracellular calcium concentration ([Ca2+]i) and resultant airway submucosal gland secretion on muscarinic receptor stimulation, we examined the effects of atropine (ART), pirenzepine (PZ), 11([2-(diethylamino) methyl-1-piperidinyl] acetyl)-5,11-dihydro-6H-pirido (2,3-b)(1,4)-benzodiazepine-6-one (AF-DX116) and 4-diphenylacetoxy-N-methylpiperidine methiodode (4-DAMP) on methacholine (MCh)-evoked [Ca2+]i rise in acinar cells, mucus glycoprotein (MGP) secretion and electrolyte secretion from submucosal glands isolated from feline tracheae. [Ca2+]i was measured with the Ca(2+)-sensitive fluorescent dye, fura2. We determined MGP secretion by measuring trichloroacetic acid (TCA)-precipitable 3H-labeled glycoconjugates and electrolyte secretion by the change in the rate constant of 22Na-efflux from isolated glands. Half maximal inhibitory concentrations (IC50) of PZ, AF-DX116, 4-DAMP and ATR against MCh (10(-5) M)-evoked [Ca2+]i rise were 10(-7) M, 6 x 10(-6) M, 8 x 10(-9) M and 6 x 10(-9) M, respectively. IC50 values of these antagonists against MCh (10(-5) M)-evoked MGP secretion were 10(-6) M, 2 x 10(-5) M, 8 x 10(-9) M and 6 x 10(-9) M, respectively. MCh (10(-5) M)-evoked 22Na-efflux was significantly inhibited by 10(-7) M 4-DAMP and 10(-7) M ATR (p < 0.01, respectively), but the inhibitory effect of PZ (10(-7) M) was not statistically significant.(ABSTRACT TRUNCATED AT 250 WORDS)

摘要

为了确定哪种毒蕈碱受体亚型在毒蕈碱受体受刺激时调节细胞内钙浓度([Ca2+]i)的升高及随后的气道黏膜下腺分泌,我们研究了阿托品(ART)、哌仑西平(PZ)、11([2-(二乙氨基)甲基-1-哌啶基]乙酰基)-5,11-二氢-6H-吡啶并(2,3-b)(1,4)-苯并二氮杂卓-6-酮(AF-DX116)和4-二苯乙酰氧基-N-甲基哌啶甲碘化物(4-DAMP)对乙酰甲胆碱(MCh)诱发的猫气管分离腺泡细胞[Ca2+]i升高、黏液糖蛋白(MGP)分泌及黏膜下腺电解质分泌的影响。用Ca(2+)敏感荧光染料fura2测量[Ca2+]i。我们通过测量三氯乙酸(TCA)沉淀的3H标记糖缀合物来测定MGP分泌,并通过分离腺泡中22Na外流速率常数的变化来测定电解质分泌。PZ、AF-DX116、4-DAMP和ATR对MCh(10(-5) M)诱发的[Ca2+]i升高的半数最大抑制浓度(IC50)分别为10(-7) M、6×10(-6) M、8×10(-9) M和6×10(-9) M。这些拮抗剂对MCh(10(-5) M)诱发的MGP分泌的IC50值分别为10(-6) M、2×10(-5) M、8×10(-9) M和6×10(-9) M。MCh(10(-5) M)诱发的22Na外流受到10(-7) M 4-DAMP和10(-7) M ATR的显著抑制(p分别<0.01),但PZ(10(-7) M)的抑制作用无统计学意义。(摘要截断于250字)

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