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Description
There are four major Adrenergic Receptor (AR) subtypes (alpha1, alpha2, beta1, beta2). Each of the subtypes has been classified by their unique responses to agonists and antagonists. Adrenergic receptors belong to the family of guanine nucleotide-binding, regulatory protein-coupled receptors (GPCR) which transverse the plasma membrane seven times. The transmembrane regions are hydrophobic and are interconnected by hydrophilic loops . beta2-Adrenergic Receptor (beta2AR) is the most studied receptor of the catecholamine system. beta2AR stimulation occurs through the catecholamines epinephrine (adrenaline) and norepinephrine (noradrenaline) acting as neuromodulators in the central nervous system and as hormones in the vascular system. beta2AR activation results in coupling to heterotrimeric G proteins and activation of the second messengers cAMP and phosphatidylinositol, ultimately leading to changes in cellular physiology. GPCR kinases (GRKs) terminate beta2AR signaling through phosphorylation of the GPCR and by recruiting beta-arrestin. beta-arrestin binding uncouples the receptor from the G protein, thereby terminating G proteini?1/2mediated signaling (desensitization), and initiating clathrin-mediated endocytosis (internalization) of beta2AR . beta-adrenergic blocking agents (beta blockers) are drugs that block catecholamines from binding to betaAR and are prescribed for cardiac arrhythmias, cardioprotection after myocardial infarction (heart attack), and hypertension . Synonyms: ADRB2R, ADRBR, B2AR, BAR, BETA2AR,