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一种在体内同时评估组胺H1和H2受体活性的简单技术。

A simple technique to simultaneously assess activity at histamine H1- and H2-receptors in vivo.

作者信息

Owen D A, Pipkin M A

出版信息

J Pharmacol Methods. 1985 Jul;13(4):309-15. doi: 10.1016/0160-5402(85)90012-9.

DOI:10.1016/0160-5402(85)90012-9
PMID:4021497
Abstract

A technique is described that allows simultaneous and quantitative assay of the action of agonists and antagonists at histamine H1- and H2-receptors in anesthetized guinea pigs. The principle of the technique is based on H1-receptor bronchoconstriction and H2-receptor tachycardia. Studies have been made to assay antagonists at either receptor and provide simultaneous evidence of selectivity or to assay combined antagonists such as Smith Kline & French 93319. Studies with histamine receptor agonists provide evidence of the potency and selectivity of these compounds relative to histamine.

摘要

本文描述了一种技术,可同时定量测定麻醉豚鼠体内组胺H1和H2受体上激动剂和拮抗剂的作用。该技术原理基于H1受体介导的支气管收缩和H2受体介导的心动过速。已开展研究来测定任一受体上的拮抗剂,并同时提供其选择性证据,或测定联合拮抗剂,如史克必成93319。对组胺受体激动剂的研究提供了这些化合物相对于组胺的效价和选择性证据。

相似文献

1
A simple technique to simultaneously assess activity at histamine H1- and H2-receptors in vivo.一种在体内同时评估组胺H1和H2受体活性的简单技术。
J Pharmacol Methods. 1985 Jul;13(4):309-15. doi: 10.1016/0160-5402(85)90012-9.
2
Evidence for histamine H1 and H2 receptors in guinea-pig oxyntic cells.豚鼠壁细胞中组胺H1和H2受体的证据。
J Pharmacol Exp Ther. 1983 Oct;227(1):115-21.
3
The effects of cimetidine on histamine atrial chronotropic receptor activity.西咪替丁对组胺心房变时性受体活性的影响。
Agents Actions. 1982 Oct;12(4):425-30. doi: 10.1007/BF01965921.
4
The effect of histamine, H1 and H2 agonists, and H1 and H2 antagonists on postprandial pancreatic polypeptide release in dogs.组胺、H1和H2激动剂以及H1和H2拮抗剂对犬餐后胰多肽释放的影响。
Scand J Gastroenterol. 1983 Mar;18(2):165-8. doi: 10.3109/00365528309181578.
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Comparison of the effects of histamine H1- and H2-receptor agonists on large and small airways in normal and asthmatic subjects.组胺H1和H2受体激动剂对正常和哮喘受试者大、小气道影响的比较。
Br J Dis Chest. 1987 Apr;81(2):155-69. doi: 10.1016/0007-0971(87)90134-3.
6
The effects of stimulants and inhibitors of histamine receptors on acid secretion from guinea pig gastric fundus.组胺受体激动剂和抑制剂对豚鼠胃底泌酸的影响。
Eur J Pharmacol. 1978 Apr 1;48(3):249-54. doi: 10.1016/0014-2999(78)90083-3.
7
Occurrence of H1- and H2-histamine receptors in the guinea-pig gall bladder in situ.豚鼠原位胆囊中H1和H2组胺受体的存在情况。
Br J Pharmacol. 1978 Oct;64(2):219-22. doi: 10.1111/j.1476-5381.1978.tb17292.x.
8
Cyclic nucleotides and contraction/relaxation in airway muscle: H1 and H2 agonists and antagonists.环核苷酸与气道平滑肌的收缩/舒张:H1和H2激动剂及拮抗剂
J Pharmacol Exp Ther. 1980 Nov;215(2):434-42.
9
Pharmacological analysis of the tachycardia produced by histamine and specific H1-and H2-receptor agonists in anesthetized dogs.
Eur J Pharmacol. 1978 Oct 15;51(4):351-9. doi: 10.1016/0014-2999(78)90427-2.
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A question of the specificity of rabbit atrial chronotropic histamine receptors and agents which affect their activity.兔心房变时性组胺受体的特异性以及影响其活性的药物问题。
J Clin Pharmacol. 1980 Jan;20(1):10-9. doi: 10.1002/j.1552-4604.1980.tb01661.x.

引用本文的文献

1
Pharmacological studies with SK&F 93944 (temelastine), a novel histamine H1-receptor antagonist with negligible ability to penetrate the central nervous system.对SK&F 93944(替美斯汀)进行的药理学研究,SK&F 93944是一种新型组胺H1受体拮抗剂,穿透中枢神经系统的能力可忽略不计。
Br J Pharmacol. 1986 Mar;87(3):569-78. doi: 10.1111/j.1476-5381.1986.tb10199.x.