Receptor antagonism

Antihistamine. Compound that, by occupying the histamine receptors, antagonizes the effects of histamine. 

An example of the procedure is shown in Figure 6.22. Specifically, a series of Schild analyses were done for the reference antagonist scopolamine in the presence of different concentrations of the test antagonist atropine. The resultant plot according to Equation 6.38 yields an estimate of the KB for atropine as the intercept (Log (k— 1) = 0). If atropine had secondary effects on the system, this procedure will cancel them and allow measurement of the receptor antagonism. An example of this procedure is given in Section 12.2.5. 

Resultant analysis, this procedure, developed by James Black and colleagues (Br. J. Pharmacol. 84,561-571, 1985), allows measurement of the receptor affinity of a competitive antagonist, which has secondary properties that obscure the receptor antagonism see Chapter 6.6 for further discussion. 

Mode of action Enzyme inhibition Reuptake inhibition Receptor antagonism... 

Jooste E, Klafter F, Hirshman CA, Emala CW A 31 mechanism for rapacuronium-induced bronchos-pasm M2 muscarinic receptor antagonism Anesthesiology 2003 98 906. 

Parenty G, Appelbe S, Milligan G (2008) CXCR2 chemokine receptor antagonism enhances DOP opioid receptor function via allosteric regulation of the CXCR2-DOP receptor heterodimer. Biochem J 412 245-256... 

Cao, BJ and Rodgers, RJ (1997) Influence of 5-HTia receptor antagonism on plus-maze behaviour in mice. II WAY 100635, SDZ 216-525 and NAN-190. Pharmacol. Biochem. Behav. 58 593-603. 

Makriyannis and Liu claimed a series of pyrazole analogues in a patent application published in 2003 [272]. Of the 29 compounds specifically exemplified in the patent application, compound (389) was demonstrated to reduce lever presses when administered to rats that were trained to expect delivery of a food pellet as the outcome. It was proposed that the reduction in lever pressing was the result of decreased appetite brought about by CBi receptor antagonism. 

No Other work has appeared from the Merck group for a number of years and oxytocin receptor antagonism appears to be no longer an active research area for the company. 

Jacobson, A.E. and O Donohue, T.L. A specific acylating ligand for phencyclidine (PCP) receptors antagonizes PCP behavioral effects. ur J Pharmacol 111 405-406, 1985. 

Ogilvie P, Thelen S, Moepps B, et al. Unusual chemokine receptor antagonism involving a mitogen-activated protein kinase pathway. J Immunol 2004 172 6715-6722. 

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