118
Views
3
CrossRef citations to date
0
Altmetric
Research Article

FUNCTIONAL METHODS FOR QUANTIFYING AGONISTS AND ANTAGONISTS

Pages 117-137 | Published online: 31 Aug 2001

REFERENCES

  • Leff P., Dougall I. G. Is pharmacological analysis of agonist action useful in medicinal chemistry?. Trends in Receptor Research, P. Angeli, U. Gulini, W. Quaglia. Elsevier Science Publishers BV, Amsterdam 1992; 43–60
  • Clark A. J. General pharmacology. Heffter's Handbuch Der Experimentallen Pharmakologie Erganzungswerk. Springer-Verlag, Berlin 1937; 4: 1–223
  • Arie¨ns E. J. Affinity and intrinsic activity in the theory of competitive inhibition. Arch. Int. Pharmacodyn. Ther. 1954; 99: 32–49
  • Stephenson R. P. A modification of receptor theory. Br. J. Pharmacol. 1956; 11: 379–393
  • Mackay D. A flux-carrier hypothesis of drug-action. Nature 1963; 197: 1171–1173
  • Furchgott R. F. The use of β-haloalkylamines in the differentiation of receptors and in the determination of dissociation constants of receptor-agonist complexes. Adv. Drug Res., N. J. Harper, A. B. Simmonds. Academic Press, New York 1966; 3: 21–55
  • Paton W. D.M. A theory of drug action based on the rate of drug-receptor combination. Proc. R. Soc. Lond. B 1961; 154: 21–69
  • Colquhoun D. The relationship between classical and cooperative models for drug action. Drug Receptors, H. P. Rang. University Park Press, Baltimore 1973; 149–182
  • Gosselin R. E. Drug-receptor inactivation: a new kinetic model. Kinetics of Drug Action, J. M. Van Rossum. Springer-Verlag, Berlin 1977; 323–356
  • Ruffolo R. R. Important concepts of receptor theory. J. Autonom Pharmacol. 1982; 2: 277–295
  • Mackay D. A critical survey of receptor theories of drug action. Kinetics of Drug Action, J. M. Van Rossum. Springer-Verlag, Berlin 1977; 255–322
  • Black J. W., Leff P. Operational models of pharmacological agonism. Proc. R. Soc. Lond. B 1983; 220: 141–162
  • Leff P. The two-state model of receptor activation. Trends Pharmacol. Sci. 1995; 16: 89–97
  • Leff P., Prentice D. J., Giles H., Martin G. R., Wood J. Estimation of agonist affinity and efficacy by direct operational model fitting. J. Pharmacol. Methods 1990; 23: 225–237
  • Nickerson M. Receptor occupancy and tissue response. Nature 1956; 178: 697–698
  • Waud D. R. On the measurement of the affinity of partial agonists for receptors. J. Pharmacol. Exp. Ther. 1969; 170: 117–122
  • Leff P. Can operational models of agonism provide a framework for classifying hormone receptors?. Perspectives on Receptor Classification, J. W. Black, D. H. Jenkinson, V. P. Gerskowitch. Alan R Liss, New York 1987; 157–167
  • Black J. W., Left P., Shankley N. P., Wood J. An operational model of pharmacological agonism: the effect of E/[A] curve shape on agonist dissociation constant estimation. Br. J. Pharmacol. 1985; 84: 561–571
  • Barlow R. B., Scott N. C., Stephenson R. P. The affinity and efficacy of onium salts on frog rectus abdominis. Br. J. Pharmacol. 1967; 31: 188–196
  • Leff P., Dougall I. G., Harper D. Estimation of partial agonist affinity by interaction with a full agonist: a direct operational model-fitting approach. Br. J. Pharmacol. 1993; 110: 239–244
  • MacKay D. Concentration-response curves and receptor classification: null method or operational model?. Trends Pharmacol. Sci. 1988; 9: 202–205
  • Leff P. Analysis of agonist action using the operational model. Trends Pharmacol. Sci. 1988; 9: 395–398
  • Thron C. D. Graphical and weighted regression analyses for the determination of agonist dissociation constants. J. Pharmacol. Exp. Ther. 1970; 175: 541–553
  • Parker R. B., Waud D. R. Pharmacological estimation of drug-receptor dissociation constants. Statistical evaluation. I. Agonists. J. Pharmacol. Exp. Ther. 1971; 177: 1–12
  • James M. K., Morgan P. H., Leighton H. F. A new method for estimation of agonist dissociation constants (KA); directly fitting the postinactivation concentration-response curve to a nested hyperbolic equation. J. Pharmacol. Exp. Ther. 1989; 249: 61–69
  • Kramer T. H., Davis P., Hruby V. J., Burks T. F., Porreca F. In vitro potency, affinity and agonist efficacy of highly selective delta opioid receptor ligands. J. Pharmacol. Exp. Ther. 1993; 266: 577–584
  • Wiener L. H., Thalody G. P. Differential attenuation of the responses to adenosine and methoxamine in isolated rabbit aorta. J. Pharmacol. Exp. Ther. 1993; 267: 828–837
  • Sallés J., Giraldo J., Badia A. Analysis of agonism at functional prejunctional α2-adrenoceptors of rat vas deferens using operational and null approaches. Eur. J. Pharmacol. 1994; 258: 229–238
  • Palea S., Corsi M., Rimland J. M., Trist D. G. Discrimination by benextramine between the NPY-Y1receptor subtypes present in rabbit isolated vas deferens and saphenous vein. Br. J. Pharmacol. 1995; 115: 3–10
  • Zernig G., Issaevitch T., Woods J. H. Calculation of agonist efficacy, apparent affinity and receptor population changes after administration of insurmountable antagonists: comparison of different analytical approaches. J. Pharmacol. Toxicol. Methods 1996; 35: 223–237
  • Zaborowsky B. R., McMahan W. C., Griffin W. A., Norris F. H., Ruffolo R. R. Computerized graphic methods for determining dissociation constants of agonists, partial agonists and competitive antagonists in isolated smooth muscle preparations. J. Pharmacol. Methods 1980; 4: 165–178
  • McPherson G. A., Molenaar P., Raper C., Malta E. Analysis of dose-response curves and calculation of agonist dissociation constants using a weighted non-linear curve fitting program. J. Pharmacol. Methods 1983; 10: 231–241
  • Schild H. O. pAx and competitive drug antagonism. Br. J. Pharmacol. 1949; 4: 277–280
  • Arunlakshana O., Schild H. O. Some quantitative uses of drug antagonists. Br. J. Pharmacol. 1959; 14: 48–58
  • Kenakin T. P. Pharmacological Analysis of Drug-Receptor Interaction. 2nd Ed., Raven Press, New York 1993
  • Lemoine H., Kaumann A. J. A model for the interaction of competitive antagonists with two receptor subtypes characterized by a Schild plot with apparent slope unity. Naunyn Schmiedeberg's Arch. Pharmacol. 1983; 322: 111–120
  • Stone M., Angus J. A. Developments of computer-based estimation of pA2 values and associated analysis. J. Pharmacol. Exp. Ther. 1978; 207: 705–718
  • Trist D. G., Leff P. Quantification of H2-agonism by clonidine and dimaprit in an adenylate cyclase assay. Agents Actions 1985; 16: 222–226
  • Lew M. J., Angus J. A. Analysis of competitive agonist-antagonist interactions by nonlinear regression. Trends Pharmacol. Sci. 1995; 16: 328–337
  • Dougall I. G., Harper D., Lydford S. J., Leff P., Unpublished
  • BMDP Statistical Software, W. J. Dixon. University of California Press, Berkeley 1981
  • Lydford S. J., McKechnie K. C.W., Leff P. Interaction of BW A868C, a prostanoid DP-receptor antagonist, with two receptor subtypes in the rabbit isolated saphenous vein. Prostaglandins 1996; 52: 125–139
  • DeMarinis R. M., Hieble J. P. Dopamine receptor agonists: chemical and biological studies of the aminoethylindolones. Drugs Fut. 1989; 14: 780–797

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.