The classical competitive antagonism of phentolamine on smooth muscle preparations, investigated by two procedures

Autonomic and Autacoid Pharmacology

Volumn 27, Issue 1, 2007, Pages 71-77

  Patil, P N ^a  

^a OHIO STATE UNIVERSITY   (United States)

Author keywords

adrenoceptor; Drug antagonism phentolamine; Drug receptor interactions; IC50 K ratios; Tyramine; Various agonists; Vascular muscles

Indexed keywords

ALPHA ADRENERGIC RECEPTOR BLOCKING AGENT; ALPHA ADRENERGIC RECEPTOR STIMULATING AGENT; OXYMETAZOLINE; PHENTOLAMINE; PHENYLEPHRINE; SPASMOGEN;

ANIMAL EXPERIMENT; ANIMAL TISSUE; AORTA; ARTICLE; COMPETITIVE INHIBITION; CONCENTRATION (PARAMETERS); CONTROLLED STUDY; DISSOCIATION CONSTANT; DRUG ANTAGONISM; EQUILIBRIUM CONSTANT; GUINEA PIG; IC 50; MASS ACTION; NONHUMAN; RABBIT; RAT; SMOOTH MUSCLE; SMOOTH MUSCLE CONTRACTION; STATISTICAL SIGNIFICANCE; VALIDITY;

ADRENERGIC ALPHA-ANTAGONISTS; ANIMALS; AORTA; BINDING, COMPETITIVE; GUINEA PIGS; INHIBITORY CONCENTRATION 50; KINETICS; MALE; MUSCLE, SMOOTH; PHENTOLAMINE; RABBITS; RATS; RECEPTORS, ADRENERGIC, ALPHA; VAS DEFERENS;

EID: 33845607676     PISSN: 14748665     EISSN: None     Source Type: Journal    
DOI: 10.1111/j.1474-8673.2006.00386.x     Document Type: Article

References (33)

1. ARIËNS, E.J. (1954). Affinity and intrinsic activity in the theory of competitive inhibition. Part I. Problems and theory. Arch. Int. Pharmacodyn. Ther., 99, 32-49.
2. ARUNLAKSHANA, O. & SCHILD, H.O. (1959). Some quantitative uses of drug antagonists. Br. J. Pharmacol., 14, 48-58.
3. BEVAN, J.A., SU, C. & LJUNG, B. (1973). On the blockade of neuronal and exogenous noradrenaline. J. Pharm. Pharmacol., 25, 78-79.
4. BROADLEY, K.J. & WILLIAMS, R.G. (1983). Temperature-induced changes in dissociation constants (KA) of agonists at cardiac β-adrenoceptors determined by use of the irreversible antagonist Ro 03-7894. Br. J. Pharmacol., 79, 517-524.
5. BUCKNER, C.K. & PATIL, P.N. (1971). The rate of onset of beta-adrenergic blockade by the optical isomers of alprenolol. Eur. J. Pharmacol., 14, 308-311.
6. i) and the concentration of inhibitor, which causes 50 percent inhibition (IC50) of an enzymatic reaction. Biochem. Pharmacol., 22, 3099-3108.
7. 2C-adrenergic receptors enable cold-induced vasoconstriction in cutaneous arteries. Am. J. Physiol. Heart Circ. Physiol., 278, H1075-H1083.
8. EGLEN, R.M. & WHITING, R.L. (1989). Problems associated with the application of the Cheng-Prusoff relationship to estimate atropine affinity constant using functional tissue responses. Life Sci., 44, 81-94.
9. EL TAYAR, N., TESTA, B., VAN DE WATERBEEMD, H., CARRUPT, P.A. & KAUMANN, A.J. (1988). Influence of liposolubility and chirality on the selectivity of ligands for β1- and β2-adrenoceptors. J. Pharm. Pharmacol., 40, 609-612.
10. FOSTER, R.W. (1967). The potentiation of the responses to noradrenaline and isoprenaline on the guinea-pig isolated tracheal chain preparation by desipramine, cocaine, phentolamine, phenoxybenzamine, guanethidine, metanephrine and cooling. Br. J. Pharmacol. Chemother., 31, 466-482.
11. FURCHGOTT, R.F. (1964). Receptor mechanisms. Annu. Rev. Pharmacol., 4, 21-50.
12. FURCHGOTT, R.F. (1967). The pharmacological differentiation of adrenergic receptors. Ann. N. Y. Acad. Sci., 139, 553-570.
13. FURCHGOTT, R.F. (1972). The classification of adrenoceptors (adrenergic receptors). An evaluation from the standpoint of receptor theory. In: Catecholamines (Eds H. BLASCHKO & E. MUSCHOLL), pp. 283-335. Springer-Verlag, New York.
14. GADDUM, J.H. (1937). The quantitative effects of antagonistic drugs. J. Physiol., 87, 7P-9P.
15. GADDUM, J.H. (1957). Drug antagonism. Pharmacol. Rev., 9, 211-217.
16. GILLESPIE, J.S. (1972). The rat anococcygeus muscle and its response to nerve stimulation and to some drugs. Br. J. Pharmacol., 45, 404-416.
17. HARKER, C.T. & VAN HOUTTE, P.M. (1989). Cooling and alpha adrenergic responses in saphenous vein of the rabbit. J. Pharmacol. Exp. Ther., 249, 56-60.
18. KARASAWA, T., FUNAKOSHI, H., FURUKAWA, K. & YOSHIDA, K. (1973). EDTA prevents the photocatalyzed destruction of the products of catecholamine oxidation. Anal. Biochem., 53, 278-281.
19. LAZARENO, S. & BIRDSALL, N.J.M. (1993). Estimation of competitive antagonist affinity from inhibition curves using the Gaddum, Schild and Cheng-Prusoff equation. Br. J. Pharmacol., 109, 1110-1119.
20. PATIL, P.N. (1992). Reactivity of human iris sphincter to muscarinic drugs. NS Arch. Pharmacol., 346, 614-619.
21. PATIL, P.N. (1996). Pharmacologic quantitation. Indian J. Exp. Biol., 34, 615-633.
22. PATIL, P.N. (1999). Enhanced sensitivity of the iris sphincter to the muscarinic agonist carbachol at lower temperature. J. Ocul. Pharmacol. Ther., 15, 65-72.
23. PATIL, P.N. (2001). Reversal of cholinergic response of intraocular muscles by atropine: Drug antagonism re-examined. In: Pharmacology and Therapeutics in the New Millennium (Ed. S.K. GUPTA), pp. 579-586. Narosa Publishing House, New Delhi.
24. PATIL, P.N. (2004). Parameters of drug antagonism: re-examination of two modes of functional competitive drug antagonism on intraocular muscles. J. Pharm. Pharmacol., 56, 1045-1053.
25. PATIL, P.N., FUDGE, K. & JACOBOWITZ, D. (1972). Steric aspects of adrenergic drugs. XVIII α-adrenergic receptors of mammalian aorta. Eur. J. Pharmacol., 19, 79-87.
26. PATIL, P.N., FUDER, H. & VENKATARAMAN, B. (1994). Responses of iris and other tissues at lower temperatures. Can. J. Physiol., Abstract no. 15.1.1, XII International Congress of Pharmacology (July 24-29, 1994), pp. 481.
27. RAFFA, R.B., ACETO, J.F. & TALLARIDA, R.J. (1985). Measurements of thermodynamic parameters for norepinephrine contraction of isolated rabbit thoracic aorta. J. Pharm. Exp. Ther., 235, 596-600.
28. SALAZAR, M., SHIMADA, K. & PATIL, P.N. (1976). Iris pigmentation and atropine mydriasis. J. Pharm. Exp. Ther., 97, 79-88.
29. SCHILD, H.O. (1947). pA, a new scale for the measurement of drug antagonism. Br. J. Pharmacol., 2, 189-206.
30. TRENDELENBURG, U. (1972). Classification of sympathomimetic amines. In: Catecholamines (Eds H. BLASCHKO & E. MUSCHOLL), pp. 336-362. Springer-Verlag, New York.
31. TRENDELENBURG, U., MAXWELL, R.A. & PLUCHINO, S. (1970). Methoxamine as a tool to assess the importance of intraneuronal uptake of l-norepinephrine in cat's nictitating membrane. J. Pharmacol. Exp. Ther., 172, 91-99.
32. URQUILLA, P.R., STITZEL, R.E. & FLEMING, W.W. (1970). The antagonism of phentolamine against exogenously administered and endogenously released norepinephrine in rabbit aortic strips. J. Pharmacol. Exp. Ther., 172, 310-319.
33. VAN ROSSUM, J.M. & VAN DEN-BRINK, F.G. (1963). Cumulative dose-response curves I. Introduction to the technique. Arch. Int. Pharmacodyn. Ther., 143, 240-246.