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豚鼠小肠纵行肌条对(3H)-丙基苯甲酰胆碱氮芥的结合

The binding of (3H)-propylbenzilycholine mustard by longitudinal muscle strips from guinea-pig small intestine.

作者信息

Burgen A S, Hiley C R, Young J M

出版信息

Br J Pharmacol. 1974 Jan;50(1):145-51. doi: 10.1111/j.1476-5381.1974.tb09602.x.

DOI:10.1111/j.1476-5381.1974.tb09602.x
PMID:4150888
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1776569/
Abstract

1 The synthesis of tritium labelled propylbenzilylcholine mustard ([(3)H]-PrBCM; N-2'-chloroethyl-N-[2'', 3''-(3)H(2)] propyl-2-aminoethyl benzilate) is described.2 The uptake by muscle strips was measured and shown to be considerably increased by previous immersion of the muscle in distilled water.3 A considerable part of the uptake is inhibited selectively by atropine, but not by nicotinic antagonists. A number of muscarinic agonists also inhibit uptake and their apparent affinity constants have been determined.4 The uptake by atropine-sensitive sites is temperature-insensitive, whereas the other sites are temperature-sensitive. Recovery is highly temperature-sensitive and there is good agreement between recovery of sensitivity to agonists and loss of radioactivity from the muscle.

摘要
  1. 描述了氚标记的丙基苯甲酰胆碱氮芥([(3)H]-PrBCM;N-2'-氯乙基-N-[2'', 3''-(3)H(2)]丙基-2-氨基乙基苯甲酸酯)的合成。

  2. 测量了肌肉条带的摄取情况,结果表明,之前将肌肉浸入蒸馏水中会使其摄取量显著增加。

  3. 摄取的很大一部分被阿托品选择性抑制,但不受烟碱拮抗剂抑制。一些毒蕈碱激动剂也抑制摄取,并已测定了它们的表观亲和常数。

  4. 对阿托品敏感位点的摄取对温度不敏感,而其他位点对温度敏感。恢复对温度高度敏感,并且对激动剂的敏感性恢复与肌肉中放射性的丧失之间有很好的一致性。

相似文献

1
The binding of (3H)-propylbenzilycholine mustard by longitudinal muscle strips from guinea-pig small intestine.豚鼠小肠纵行肌条对(3H)-丙基苯甲酰胆碱氮芥的结合
Br J Pharmacol. 1974 Jan;50(1):145-51. doi: 10.1111/j.1476-5381.1974.tb09602.x.
2
Muscarinic receptors in rat intestinal muscle: comparison with the guinea pig.大鼠肠肌中的毒蕈碱受体:与豚鼠的比较。
Eur J Pharmacol. 1975 Apr;31(2):319-26. doi: 10.1016/0014-2999(75)90055-2.
3
Ligand binding to muscarinic receptors in intact longitudinal muscle strips from guinea-pig intestine.豚鼠肠道完整纵肌条中配体与毒蕈碱受体的结合
Br J Pharmacol. 1977 Oct;61(2):189-97. doi: 10.1111/j.1476-5381.1977.tb08404.x.
4
The properties of muscarinic receptors in mammalian cerebral cortex.哺乳动物大脑皮层中毒蕈碱受体的特性。
Br J Pharmacol. 1974 Jun;51(2):279-85. doi: 10.1111/j.1476-5381.1974.tb09658.x.
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The number of muscarinic receptors in chick amnion muscle.鸡羊膜肌中毒蕈碱受体的数量。
Br J Pharmacol. 1973 Nov;49(3):498-505. doi: 10.1111/j.1476-5381.1973.tb17260.x.
6
Persistent effects of high concentrations of chlorpromazine on 3H-propylbenzilylcholine mustard binding to muscarinic receptors in guinea-pig intestinal muscle strips.高浓度氯丙嗪对豚鼠肠肌条中3H-丙基苄基胆碱氮芥与毒蕈碱受体结合的持续影响。
Arch Int Pharmacodyn Ther. 1980 Sep;247(1):21-30.
7
The irreversible binding of acetylcholine mustard to muscarinic receptors in intestinal smooth muscle of the guinea-pig.乙酰胆碱芥子气与豚鼠肠道平滑肌中毒蕈碱受体的不可逆结合。
Br J Pharmacol. 1975 Mar;53(3):363-70. doi: 10.1111/j.1476-5381.1975.tb07372.x.
8
The effect of propylbenzilylcholine mustard on contraction and radioligand binding parameters of muscarinic receptors in guinea pig ileum.丙基苄基胆碱氮芥对豚鼠回肠毒蕈碱受体收缩及放射性配体结合参数的影响。
Life Sci. 1987 Oct 26;41(17):2023-32. doi: 10.1016/0024-3205(87)90476-0.
9
Changes in muscarinic ligand binding to intestinal muscle strips produced by pre-exposure to hypotonic conditions.预先暴露于低渗条件下对毒蕈碱配体与肠肌条结合产生的影响。
J Pharm Pharmacol. 1978 Jan;30(1):27-35. doi: 10.1111/j.2042-7158.1978.tb13148.x.
10
Homologues of benzilylcholine mustard.苯甲酰胆碱氮芥的同源物。
J Pharm Pharmacol. 1972 Dec;24(12):950-4. doi: 10.1111/j.2042-7158.1972.tb08925.x.

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G-protein-coupled receptors: past, present and future.G蛋白偶联受体:过去、现在与未来。
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Mediation by the same muscarinic receptor subtype of phasic and tonic contractile activities in the rat isolated portal vein.大鼠离体门静脉中相同毒蕈碱受体亚型对相性和紧张性收缩活动的介导作用。
Br J Pharmacol. 1993 Jan;108(1):132-8. doi: 10.1111/j.1476-5381.1993.tb13452.x.
3
Binding of [3H]-pilocarpine to membranes from rat cerebral cortex.[3H]-毛果芸香碱与大鼠大脑皮质膜的结合
Naunyn Schmiedebergs Arch Pharmacol. 1981 Sep;317(2):126-30. doi: 10.1007/BF00500067.
4
Actions of various muscarinic agonists on membrane potential, potassium efflux, and contraction of longitudinal muscle of guinea-pig intestine.各种毒蕈碱激动剂对豚鼠肠纵肌膜电位、钾外流和收缩的作用。
Br J Pharmacol. 1981 Feb;72(2):319-34. doi: 10.1111/j.1476-5381.1981.tb09131.x.
5
Two ligands may bind simultaneously to the muscarine receptor.两种配体可能同时与毒蕈碱受体结合。
Naunyn Schmiedebergs Arch Pharmacol. 1982 Jul;320(1):3-13. doi: 10.1007/BF00499064.
6
Muscarinic receptor occupation and receptor activation in the guinea-pig ileum by some acetamides related to oxotremorine.与氧化震颤素相关的一些乙酰胺类化合物对豚鼠回肠中毒蕈碱受体的占据及受体激活作用。
Br J Pharmacol. 1984 May;82(1):269-74. doi: 10.1111/j.1476-5381.1984.tb16467.x.
7
Purification of muscarinic acetylcholine receptors by affinity chromatography.通过亲和色谱法纯化毒蕈碱型乙酰胆碱受体。
EMBO J. 1983;2(4):499-504. doi: 10.1002/j.1460-2075.1983.tb01453.x.
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Hydrodynamic properties of muscarinic acetylcholine receptors solubilized from rat forebrain.从大鼠前脑溶解出来的毒蕈碱型乙酰胆碱受体的流体动力学特性。
Br J Pharmacol. 1984 Aug;82(4):839-51. doi: 10.1111/j.1476-5381.1984.tb16481.x.
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Evidence that histamine and carbachol may open the same ion channels in longitudinal smooth muscle of guinea-pig ileum.组胺和卡巴胆碱可能在豚鼠回肠纵行平滑肌中打开相同离子通道的证据。
J Physiol. 1981 Nov;320:363-79. doi: 10.1113/jphysiol.1981.sp013955.
10
The properties of muscarinic receptors in mammalian cerebral cortex.哺乳动物大脑皮层中毒蕈碱受体的特性。
Br J Pharmacol. 1974 Jun;51(2):279-85. doi: 10.1111/j.1476-5381.1974.tb09658.x.

本文引用的文献

1
THE UPTAKE OF ATROPINE AND RELATED DRUGS BY INTESTINAL SMOOTH MUSCLE OF THE GUINEA-PIG IN RELATION TO ACETYLCHOLINE RECEPTORS.豚鼠肠道平滑肌对阿托品及相关药物的摄取与乙酰胆碱受体的关系
Proc R Soc Lond B Biol Sci. 1965 Aug 24;163:1-44. doi: 10.1098/rspb.1965.0058.
2
STIMULANT ACTIONS OF VOLATILE ANAESTHETICS ON SMOOTH MUSCLE.挥发性麻醉药对平滑肌的兴奋作用
Br J Pharmacol Chemother. 1964 Apr;22(2):356-65. doi: 10.1111/j.1476-5381.1964.tb02040.x.
3
An alkylating derivative of benzilylcholine with specific and long-lasting parasympatholytic activity.一种具有特异性和长效副交感神经阻滞活性的苄基胆碱烷基化衍生物。
Mol Pharmacol. 1966 Jul;2(4):284-97.
4
Distribution of bound 3 H-benzilylcholine mustard in subcellular fractions of smooth muscle from guinea-pig ileum.豚鼠回肠平滑肌亚细胞组分中结合的3H-苄基胆碱氮芥的分布
Br J Pharmacol. 1971 Oct;43(2):417P-418P.
5
Unmasking of insulin receptors in fat cells and fat cell membranes. Perturbation of membrane lipids.脂肪细胞和脂肪细胞膜中胰岛素受体的暴露。膜脂质的扰动。
J Biol Chem. 1971 Nov;246(21):6532-42.
6
Measurement of drug-receptor dissociation constants of muscarinic agonists on intestinal smooth muscle.毒蕈碱激动剂在肠道平滑肌上的药物-受体解离常数的测定。
J Pharmacol Exp Ther. 1972 Jan;180(1):62-70.
7
Determination of the number of muscarinic receptors in chick amnion muscle.鸡羊膜肌中毒蕈碱受体数量的测定。
Br J Pharmacol. 1973 Mar;47(3):631P-632P.
8
The dispositions of proteins in the plasma membranes of animal cells: analytical approaches using controlled peptidolysis and protein labels.动物细胞质膜中蛋白质的分布:利用可控肽解和蛋白质标记的分析方法
Biochim Biophys Acta. 1972 Feb 14;265(1):61-83. doi: 10.1016/0304-4157(72)90019-6.
9
Dissociation constants of D- and L-lactoylcholines and related compounds at cholinergic receptors.D-和L-乳酰胆碱及相关化合物在胆碱能受体处的解离常数。
J Pharmacol Exp Ther. 1972 Feb;180(2):326-39.
10
Homologues of benzilylcholine mustard.苯甲酰胆碱氮芥的同源物。
J Pharm Pharmacol. 1972 Dec;24(12):950-4. doi: 10.1111/j.2042-7158.1972.tb08925.x.