Abstract:
:If one drug, B, antagonizes another, A, by producing the opposite physiological effect, the antagonist concentration-effect curves should be affected by the recording system, which limits the range of agonist responses. With pieces of isolated guinea-pig ileum taken from adjacent parts of the same animal, one recorded isotonically, the other isometrically with the same load, the isotonic IC(50) values for (-)isoprenaline opposing carbachol or histamine were lower than the isometric values (P<0.01) but there was a significant correlation between them (P<0.01): the isotonic curves were steeper (P<0.01) and there were wider shifts in IC(50) before increasing the agonist reduced the maximum relaxation. In similar experiments with pieces of rat uterus in oestrus from the same animal, the concentration-effect curves for carbachol opposed by increasing concentrations of (-)isoprenaline or (-)adrenaline had slightly lower EC(50) values with isometric recording but there was a significant correlation (P<0.01) with isotonic values. The antagonist effect (ratio of the EC(50) relative to that for the control) was higher with isotonic recording (P<0.01 for (-)isoprenaline, P<0.025 for (-)adrenaline) and all (27) curves were steeper than the corresponding isometric curve (P<0.001). The influence of the method of recording on the results is expected from the narrower operational window and smaller upper limit to relaxation with isotonic recording. A way of obtaining measurements of IC(50) against a standard agonist effect is suggested in an Appendix.
journal_name
Br J Pharmacoljournal_title
British journal of pharmacologyauthors
Barlow RB,Bond SM,Grant C,McQueen DS,Yaqoob Zdoi
10.1038/sj.bjp.0704169subject
Has Abstractpub_date
2001-08-01 00:00:00pages
1087-95issue
7eissn
0007-1188issn
1476-5381journal_volume
133pub_type
杂志文章abstract::1. The purpose of this study was to compare the pharmacological properties (i.e. the AV nodal depressant, vasodilator, and inotropic effects) of two AV nodal blocking agents belonging to different drug classes; a novel A1 adenosine receptor (A1 receptor) agonist, N-(3(R)-tetrahydrofuranyl)-6-aminopurine riboside (CVT-...
journal_title:British journal of pharmacology
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doi:10.1038/sj.bjp.0702287
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journal_title:British journal of pharmacology
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更新日期:2001-09-01 00:00:00
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abstract::1. The 37 amino acid human calcitonin gene-related peptide (CGRP), was injected intra-arterially into the isolated, blood perfused spleen of the dog. 2. The only vascular response observed to CGRP, once threshold had been reached (10-20 fmol), was a dose-dependent splenic arterial vasodilatation. 3. The mean intra-art...
journal_title:British journal of pharmacology
pub_type: 杂志文章
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abstract::1. The aim of the present study was to test the effects of DAU 6215 (endo-N-(8-methyl-8-azabicyclo-[3.2.1]-octo-3-yl)-2,3-dihydro-2-ox o-1H- benzimidazole-1-carboxamide carboxamide hydrochloride), a newly synthesized, selective 5-hydroxytryptamine3 (5-HT3) antagonist, on the cell membrane properties and on characteriz...
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abstract:BACKGROUND AND PURPOSE:Quercetin is a natural polyphenolic flavonoid that displays anti-diabetic properties in vivo. Its mechanism of action on insulin-secreting beta cells is poorly documented. In this work, we have analysed the effects of quercetin both on insulin secretion and on the intracellular calcium concentrat...
journal_title:British journal of pharmacology
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更新日期:2013-07-01 00:00:00
abstract::1. Human mast cell tryptase appears to display considerable variation in activating proteinase-activated receptor 2 (PAR(2)). We found tryptase to be an inefficient activator of wild-type rat-PAR(2) (wt-rPAR(2)) and therefore decided to explore the factors that may influence tryptase activation of PAR(2). 2. Using a 2...
journal_title:British journal of pharmacology
pub_type: 杂志文章
doi:10.1038/sj.bjp.0704303
更新日期:2001-10-01 00:00:00
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journal_title:British journal of pharmacology
pub_type: 杂志文章
doi:10.1111/j.1476-5381.1978.tb17312.x
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journal_title:British journal of pharmacology
pub_type: 杂志文章
doi:10.1111/bph.14455
更新日期:2018-10-01 00:00:00
abstract::1. The subtype of alpha1-adrenoceptor mediating contractions to phenylephrine of the rat thoracic aorta, mesenteric artery and pulmonary artery were investigated by use of antagonists which show selectivity between the cloned alpha1-adrenoceptor subtypes in binding studies. 2. Cumulative concentration-contraction curv...
journal_title:British journal of pharmacology
pub_type: 杂志文章
doi:10.1038/sj.bjp.0701461
更新日期:1997-11-01 00:00:00