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G protein-coupled receptors
G protein-coupled receptors (GPCR) represent the largest group among the receptors of both hormones and neuro-transmitters, and accordingly have a prominent role as drug targets. The percentage of all drugs in use today that act on one or the other GPCR is given in the literature as 25-50%, and it is likely to increase in the future1. Examples are:
• Muscarinic acetylcholine receptors (several types)
• Catecholamine receptors
• Serotonin receptors 5-HT 1,2,4,6
• GABAB receptor
• `Metabotropic' glutamate receptors (11 subtypes)
• Purine receptors (P2Y): Adenosine, AMP, ADP, ATP
• Peptide hormone receptors
As noted before, most of the presently used drugs target receptors of small hormone and transmitter molecules, to which they are structurally related. The number of drugs that target receptors for peptide mediators is very limited. Notable examples are the opioids (derivatives and analogs of morphine) and the the angiotensin receptor blocker val-sartan (cf. the introductory chapter). However, peptide re-ceptors are very much in the focus of current drug develop-ment efforts, and it seems likely that in the future a substan-tial number of new drugs that target currently inaccessible receptors will become available.
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