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The Alpha1A-adrenoceptor (α1A-adrenoreceptor), also known as ADRA1A, is a subtype of the alpha-1 adrenergic receptor family. This receptor is a G protein-coupled receptor (GPCR) that primarily couples to the Gq/11 family of G proteins, leading to activation of phospholipase C and increases in intracellular calcium. It is involved in vasoconstriction, smooth muscle contraction, and neurotransmission, and is a therapeutic target for conditions like hypertension and benign prostatic hyperplasia. Endogenous ligands include norepinephrine and epinephrine.
Agonists cause vasoconstriction and smooth muscle contraction by activating Gq/11 signaling, increasing IP3 and DAG, leading to calcium release. Antagonists block this activation, causing vasodilation and smooth muscle relaxation.
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