Target Information
Adrenergic receptors (ARs) are members of the 7-transmembrane domain G-protein-coupled receptor superfamily that bind the endogenous catecholamines epinephrine and norepinephrine. Pharmacological, structural, and molecular cloning data indicate significant heterogeneity within this receptor family. Nine receptor subtypes have been identified thus far including three alpha-1 AR subtypes (1A/D, 1B, and 1C), three alpha-2 ARs (2A, 2B, and 2C), and three beta AR subtypes (1, 2, and 3). ARs participate in either the onset or maintenance of several disease states including hypertension, cardiac dysfunction (congestive heart failure, ischemia, arrhythmias), diabetes, glaucoma, depression, and impotence. A1AR subtypes are found in numerous tissues and have been shown to be involved in the regulation of blood pressure due to changes in vascular tone and cardiac output. Effects on uterine contraction, hepatic glucose metabolism, heat shock protein 70 (HSP70), proto-oncogene expression, and mitogenesis have been linked to A1AR activation. Norepinephrine can increase nitric oxide synthase (NOS) levels in the hypothalamus by activating alpha-1 AR which may indirectly suppress the release of luteinizing hormone (LH), the androgens, estrogen, and progesterone.
Synonyms
ADA1; adra1a; adra1aa; Adra1c; ADRA1L1; adrenergic alpha 1c receptor; adrenergic receptor alpha 1c subtype; adrenergic receptor, alpha 1a; adrenergic receptor, alpha 1c; adrenergic, alpha-1A-, receptor; adrenergic, alpha-1Aa, receptor; adrenoceptor alpha 1A; adrenoceptor alpha 1Aa; alpha 1A-adrenoceptor; alpha 1A-adrenoreceptor; alpha 1C-adrenergic receptor; alpha-1A adrenergic receptor; Alpha-1A adrenoceptor; alpha-1A adrenoreceptor; ALPHA1AAR; Alpha-1C adrenergic receptor; Alpha1C-AR; Alpha-adrenergic receptor 1c; fc18h12; G protein coupled receptor; wu:fc18h12