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Mechanism of activation of A2 adenosine receptors. II. A restricted collision-coupling model of receptor-effector interaction

W Gross and MJ Lohse

Pharmakologisches Institut, Universitat Heidelberg, FRG.

Existing models describing the kinetics of receptor-effector interaction were found to be insufficient to account for the experimental findings on adenylate cyclase activation by A2 adenosine receptors described in the preceding manuscript [Mol. Pharmacol. 39: 517-523 (1991)]. We have, therefore, chosen another approach and have developed discrete computer simulations of receptor-effector interactions taking place on a spherical membrane. These simulations were based on the following principles: (a) receptors activate effectors in a catalytic manner, and (b) diffusion of receptors and effectors is slow, so that receptors will only activate effectors that are in their vicinity at the time of agonist occupation. Using several experimentally determined parameters, these simulations could reproduce the experimental findings on adenylate cyclase activation by A2 adenosine receptors described in the preceding manuscript. In addition, by appropriate choice of the simulation parameters, they are shown to accommodate the behavior of several other models of receptor-effector interactions.

Volume 39, Issue 4, pp. 524-530, 04/01/1991
Copyright © 1991 by American Society for Pharmacology and Experimental Therapeutics




This article has been cited by other articles:


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C. Charalambous, I. Gsandtner, S. Keuerleber, L. Milan-Lobo, O. Kudlacek, M. Freissmuth, and J. Zezula
Restricted Collision Coupling of the A2A Receptor Revisited: EVIDENCE FOR PHYSICAL SEPARATION OF TWO SIGNALING CASCADES
J. Biol. Chem., April 4, 2008; 283(14): 9276 - 9288.
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Copyright © 1991 by the American Society for Pharmacology and Experimental Therapeutics