Constitutive activity of receptors

Competitive antagonists affinity of, 261-264 description of, 75 IC50 correction factors for, 223 Schild analysis, 261-264 Concentration-dependent antagonism, 99 Concentration-response curve, 13 Confidence intervals, 228-229 Conformations, 13-14 Constitutive activity of receptors description of, 49—51 receptor density and, 56 Schild analysis, 108-111 Context-dependent biological effect, 188 Correction factors, 211-213, 223 Correlational research, 231 CP320626, 128... 

Lefkowitz, RJ, Cotecchia, S, Samama, P and Costa, T (1993) Constitutive activity of receptors coupled to guanine nucleotide regulatory proteins. TIPS 14 303-307. 

Schwartz, 1. C., Morisset, S., Rouleau, A., et al. (2003) Therapeutic impUcations of constitutive activity of receptors the example of the histamine H receptor. J. Neural. Transm. Suppl. 1-16. 

Therapeutic implications of constitutive activity of receptors the example of the histamine H3 receptor. J Neural Transm Suppl 1-16... 

A schematic representation of receptor systems in terms of the cubic ternary complex model is shown in Figure 3.13. The amount of signaling species (as a fraction of total receptor) as defined by the cubic ternary complex model (see Section 3.13.8) is expressed as predicts that the constitutive activity of receptor systems can reach a maximal asymptote that is below the system maximum (partial constitutive activity). This is because the cubic ternary complex model predicts the maximal constitutive activity, as given by Equation 3.24 ... 

Rational design, 148-149, 152 Real-time assays, 83, 88 Receptor(s). See also Drug receptors affinity for, 6, 63 allosteric model of, 143 Clark s work, 3 classical model of, 44-45 concept of, 2-4 conformations, 13-14, 13 Of conservation equation for, 76 constitutive activity of, 49-51 coupling of, 27 definition of, 2 desensitization of, 34 efficacy for, 6... 

This predicts the constitutive activity of the G-protein-coupled receptor. Note the dependence on the effective concentration of the G-protein. 

Morisset, S., Rouleau, A., Iigneau, X. el al. (2000). High constitutive activity of native H3 receptors regulates histamine neurons in brain. Nature 408, 860-4. 

Bakker, R. A., Wieland, K., Timmerman, H. Leurs, R. (2000). Constitutive activity of the histamine H(l) receptor reveals inverse agonism of histamine H(l) receptor antagonists. Eur. J. Pharmacol. 387, R5-7. 

H3-receptor-mediated [35S]GTP gamma[S] binding evidence for constitutive activity of the recombinant and native rat and human H3 receptors. Br. J. Pharmacol. 135, 383-92. 

Wieland, K., Bongers, G., Yamamoto, Y. etal. Constitutive activity of histamine H3 receptors stably expressed in SK-N-MC cells display of agonism and inverse agonism by H3 antagonists. /. Pharmacol. Exp. Ther. 299 908-914, 2001. 

Well-documented cases exist where the estrogens inhibit the expression of some genes. These are usually transcribed by means of the constitutive activity of powerful promoters. The inhibition is a result of the steric interposition of the receptor dimer in the development region of the gene, which thereby recruits corepressors that interrupt the prior instigator effect in the absence of receptor (McKenna et al. 1999 Mester et al. 1995 Smith et al. 1997 Tora et al. 1989). 

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