At least 55 types of GPCRs are known to directly mediate neuronal and endocrine regulation of cardiac and vascular responses, and many more influence cardiovascular functions indirectly. In spite of this apparent abundance of potential GPCR drug targets, currently only p-adrenoceptor antagonists (p-blockers) and antagonists of angiotensin II type 1 receptors (AT1 antagonists) are in widespread use in clinical cardiovascular therapeutics. In addition, some other types of receptors for mono-amine neurotransmitters and vasoactive peptides are targets for certain classical cardiovascular drugs such as atropine and for newer drug classes with precisely targeted actions such as sumatriptan and related agents that have changed clinical practices in the treatment of migraine. Approximately ten additional types of GPCRs are currently targeted by new drug candidates that are in various phases of clinical development. The genome project and concomitant advances in molecular medicine have, however, recently uncovered new potential drug targets: receptor subtypes with possibilities for drug actions with improved benefit:harm ratios; regulatory mechanisms influencing receptor gene expression and receptor functions; and genetic receptor variants offering opportunities for patient selection, risk profiling, and individualized therapy. More than 100 orphan GPCRs await characterization, and some of them may turn out to be valid cardiovascular drug targets.

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