Functional assessment of beta adrenoceptor subtypes in human colonic circular and longitudinal (taenia coli) smooth muscle.
Luciano Manara,T. Croci,Giulio Aureggi,Fabio Guagnini,J P Maffrand,G. Le Fur,Sylvain Mukenge,Gianfranco Ferla +7 more
TL;DR: β1, β2, and β3 adrenoceptors are functionally detectable in the human colon; agonist stimulation of any one type relaxed taenia but only isoprenaline was fully effective at the β3 subtype.
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Abstract: Background and aims—The subtype and species related heterogeneity of ‚ adrenoceptors prompted a functional reappraisal of these molecular targets of motility inhibition in the human colon. Methods—Relaxation of muscle strips was measured in vitro. Results—The following agonists had decreasing relaxing potency (eVective concentration range 10 ˛8 ‐10 ˛4 mol/l): (˛)isoprenaline (non-selective), terbutaline (‚2 selective), CGP 12177 (‚3 selective, also ‚1, ‚2 antagonist), and SR 58611A (‚3 selective). Isoprenaline and terbutaline were more potent on circular than taenia strips; CGP 12177 and SR 58611A weakly and partially relaxed taenia but had little eVect on circular strips. The potency of isoprenaline on circular strips was greatly reduced by the ‚1 selective antagonist CGP 20712 (10 ˛7 mol/l), and less so by ICI 118551 (10
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References
Some quantitative uses of drug antagonists
O. Arunlakshana,H. O. Schild +1 more
TL;DR: Various applications of pAx measurements are discussed based on the hypothesis that drugs and drug antagonists compete for receptors according to the mass law, and a new measure, pAh, is introduced to express the activity of unsurmountable antagonists.
3.9K
A study of the adrenotropic receptors
TL;DR: Experiments described in this paper indicate that although there are two kinds of adrenotropic receptors they cannot be classified simply as excitatory or inhibitory since each kind of receptor may have either action depending upon where it is found.
2.9K
Differentiation of receptor systems activated by sympathomimetic amines.
TL;DR: The classification of receptor systems which are activated by sympathomimetic amines has engaged the attention of many investigators as mentioned in this paper, who have suggested the convenient designations of alpha (α) and beta (β) to distinguish major differences in the responses elicited in various organ systems.
2.1K
Some quantitative uses of drug antagonists. 1958.
O Arunlakshana,H O Schild +1 more
TL;DR: Various applications of pAx measurements are discussed based on the hypothesis that drugs and drug antagonists compete for receptors according to the mass law, and a new measure, pAh, is introduced to express the activity of unsurmountable antagonists.
1.9K