介导大鼠离体空肠对儿茶酚胺产生舒张反应的肾上腺素能受体。
Adrenoceptors mediating relaxation to catecholamines in rat isolated jejunum.
作者信息
MacDonald A, Forbes I J, Gallacher D, Heeps G, McLaughlin D P
机构信息
Department of Biological Sciences, Glasgow Caledonian University, Glasgow.
出版信息
Br J Pharmacol. 1994 Jun;112(2):576-8. doi: 10.1111/j.1476-5381.1994.tb13113.x.
Abstract
- The characteristics of adrenoceptors mediating relaxation to catecholamines in rat isolated jejunum were investigated. 2. Catecholamines and BRL 37344 produced relaxation of the KCl-contracted strips with an order of potency of isoprenaline (1.0) > BRL 37344 (0.63) > noradrenaline (0.1) > adrenaline (0.04). 3. In the presence of both prazosin (1 microM) and propranolol (1 microM) only small dextral shifts of the concentration-response curves to agonists were observed and an order of potency of BRL 37344 (2.5) > isoprenaline (1.0) > noradrenaline (0.2) > adrenaline (0.1) was obtained. 4. In the presence of prazosin (1 microM) and propranolol (1 microM), cyanopindolol (0.1-10 microM) produced a concentration-dependent rightward shift of the concentration-response curve to adrenaline with a Schild slope not significantly different from unity and a mean pA2 value of 7.01. 5. The resistance of relaxant responses to propranolol, the relatively high potency of BRL 37344 compared to catecholamines and the competitive antagonism of relaxant responses to adrenaline by cyanopindolol suggest that beta-adrenoceptors in rat small intestine are mainly atypical in nature.
摘要
- 研究了大鼠离体空肠中介导对儿茶酚胺舒张反应的肾上腺素能受体的特性。2. 儿茶酚胺和BRL 37344使氯化钾收缩的肠条舒张，其效力顺序为异丙肾上腺素（1.0）> BRL 37344（0.63）>去甲肾上腺素（0.1）>肾上腺素（0.04）。3. 在哌唑嗪（1微摩尔）和普萘洛尔（1微摩尔）同时存在的情况下，仅观察到激动剂浓度 - 反应曲线有小的右旋位移，且得到的效力顺序为BRL 37344（2.5）>异丙肾上腺素（1.0）>去甲肾上腺素（0.2）>肾上腺素（0.1）。4. 在哌唑嗪（1微摩尔）和普萘洛尔（1微摩尔）存在的情况下，氰吲哚洛尔（0.1 - 10微摩尔）使肾上腺素的浓度 - 反应曲线产生浓度依赖性右移，其希尔德斜率与1无显著差异，平均pA2值为7.01。5. 舒张反应对普萘洛尔的抗性、BRL 37344相对于儿茶酚胺的较高效力以及氰吲哚洛尔对肾上腺素舒张反应的竞争性拮抗表明，大鼠小肠中的β - 肾上腺素能受体在本质上主要是非典型的。
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本文引用的文献
1
Some quantitative uses of drug antagonists.药物拮抗剂的一些定量应用。
Br J Pharmacol Chemother. 1959 Mar;14(1):48-58. doi: 10.1111/j.1476-5381.1959.tb00928.x.
2
Changes in configuration of spontaneously discharged spike potentials from smooth muscle of the guinea-pig's taenia coli; the effect of electrotonic currents and of adrenaline, acetylcholine and histamine.豚鼠结肠带平滑肌自发放电锋电位的构型变化；电紧张电流以及肾上腺素、乙酰胆碱和组胺的作用。
J Physiol. 1957 Feb 15;135(2):412-25. doi: 10.1113/jphysiol.1957.sp005720.
3
Membrane potentials of smooth muscle fibres of the taenia coli of the guinea-pig.豚鼠结肠带平滑肌纤维的膜电位
J Physiol. 1954 Aug 27;125(2):302-15. doi: 10.1113/jphysiol.1954.sp005159.
4
Atypical beta-adrenoceptor on brown adipocytes as target for anti-obesity drugs.棕色脂肪细胞上的非典型β-肾上腺素能受体作为抗肥胖药物的靶点。
Nature. 1984;309(5964):163-5. doi: 10.1038/309163a0.
5
(+/-)[125Iodo] cyanopindolol, a new ligand for beta-adrenoceptors: identification and quantitation of subclasses of beta-adrenoceptors in guinea pig.（±）[125碘]氰基吲哚洛尔，一种新型β-肾上腺素能受体配体：豚鼠β-肾上腺素能受体亚型的鉴定与定量
Naunyn Schmiedebergs Arch Pharmacol. 1981;317(4):277-85. doi: 10.1007/BF00501307.
6
Effects of noradrenaline and isoprenaline on the electrical and mechanical activities of guinea pig depolarized taenia coli.去甲肾上腺素和异丙肾上腺素对豚鼠去极化结肠带的电活动和机械活动的影响
Jpn J Physiol. 1972 Jun;22(3):253-70. doi: 10.2170/jjphysiol.22.253.
7
Catecholamine action on smooth muscle.儿茶酚胺对平滑肌的作用。
Pharmacol Rev. 1987 Mar;39(1):49-96.
8
Agonist and antagonist characterization of a putative adrenoceptor with distinct pharmacological properties from the alpha- and beta-subtypes.一种推定的肾上腺素能受体的激动剂和拮抗剂特性，其具有与α和β亚型不同的药理学特性。
Br J Pharmacol. 1988 Nov;95(3):723-34. doi: 10.1111/j.1476-5381.1988.tb11698.x.
9
Is the adipocyte beta-adrenoceptor a prototype for the recently cloned atypical 'beta 3-adrenoceptor'?
Trends Pharmacol Sci. 1990 Jan;11(1):3-7. doi: 10.1016/0165-6147(90)90032-4.
10
Probing the molecular dimensions of general anaesthetic target sites in tadpoles (Xenopus laevis) and model systems using cycloalcohols.利用环醇探究蝌蚪（非洲爪蟾）和模型系统中全身麻醉靶点的分子尺寸。
Br J Pharmacol. 1991 Jan;102(1):167-73. doi: 10.1111/j.1476-5381.1991.tb12148.x.
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