Agonist-Antagonists and Inverse Agonists

The potential advantages or benefits of allosteric drugs over agonists, antagonists, and inverse agonists may be elaborated as follows. 

Agonists (e.g., prototypic 1,4-benzodiazepines), potentiate GABA-induced Cl flux and are typically characterized by sedative, anxiolytic, and anticonvulsant effects (114). Partial agonists, antagonists, and inverse agonists are also well known (115,116). 

Williams, K., Dawson, V.L., Romano, C., Dichter, M.A. and Molinoff, P.B. (1990). Characterization of polyamines having agonist, antagonist, and inverse agonist effects at the polyamine recognition site of the NMDA receptor. Neuron 5 199-208. 

Fig. 28.1 Agonists, antagonists and inverse agonists active at the benzodiazepine receptor.

Liu, X., Callaerts-Vegh, Z., Evans, K.L., and Bond, R.A. 2002. Chronic infusion of p-adrenoceptor antagonist and inverse agonists decreases elevated protein kinase A activity in transgenic mice with cardiac-specific overexpression of human P2-adrenoceptor. J. Cardiovasc. Pharmacol. 40 448 155. 

Geller E, Halpern P. Benzodiazepine antagonists and inverse agonists. Curr Opin Anaesthesiol 1990 3 568. 

Antihistamines and Histamine H3 receptor antagonists and inverse agonists GSK239512 Latrepirdine (Dimebon)... 

FIGURE 4.1 Mode of action of agonists, neutral antagonists and inverse agonists. 

SR141716A (7) has been shown to act as a competitive antagonist and inverse agonist in host cells transfected with exogenous CBi receptor, as well as in biological preparations endogenously expressing CBi. Bouaboula and co-workers... 

Lempiainen, H., Moln r, F., Macias, G. M., Perakyla, M., and Carlberg, C. (2005) Antagonist- and inverse agonist-driven interactions of the vitamin D receptor and the... 

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