Agonists are a class of chemicals that bind to certain receptors of a cell and trigger a series of responses. A selective agonist is specific for a certain type of receptor. Agonists can be classified as full agonists or partial agonists. Full agonists bind and activate a receptor, displaying full efficacy at that receptor. Partial agonists also bind and activate a given receptor, but has only partial efficacy at that receptor.[1] Agonists are widely used in the clinical setting. Four members of 5-hydroxytryptamine1B/1D (5-HT1B/1D) receptor agonists have been developed for the treatment of migraine headaches and approved for general clinical use in the United States.[2] Dopamine agonists are first-line agents for the treatment of Parkinson’s disease.[3] Increasing preclinical and clinical literature suggests that GABAB receptor agonists promote abstinence and reduce the use of cocaine, heroin, alcohol and nicotine.[4]

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[1] [2] Fox AW. Comparative tolerability of oral 5-HT1B/1D agonists. Headache. 2000, 40(7): 521-527. [3] Schade R, et al. Dopamine agonists and the risk of cardiac-valve regurgitation. N Engl J Med. 2007, 356(1): 29-38. [4] Cousins MS, et al. GABA(B) receptor agonists for the treatment of drug addiction: a review of recent findings. Drug Alcohol Depend. 2002, 65(3): 209-220.

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