Alpha-1A adrenergic receptor (ADRA1A) (ADRA1A)

The Alpha-1A adrenergic receptor (ADRA1A) is a G protein-coupled receptor (GPCR) that mediates the signaling of catecholamines like norepinephrine and epinephrine (UniProt, P35348). It is primarily located in the smooth muscle of the prostate, bladder neck, and urethra, where its activation leads to contraction via the Gq/11-phospholipase C pathway (NCBI Gene, 148). This receptor plays a critical role in the pathophysiology of benign prostatic hyperplasia (BPH) and lower urinary tract symptoms (LUTS) (StatPearls, NBK538498). Therapeutic targeting of ADRA1A involves the use of selective antagonists, such as tamsulosin and silodosin, which relax the smooth muscle to alleviate urinary obstruction (DrugBank, DB00706). Beyond the urinary tract, ADRA1A is also involved in vascular tone regulation and has been implicated in cardiac hypertrophy and central nervous system functions (PubMed, 21892148). Safety concerns for drugs targeting this receptor include orthostatic hypotension and intraoperative floppy iris syndrome (StatPearls, NBK538498).

Other names

Alpha-1A adrenoceptorAlpha-1C adrenoceptorADRA1CAlpha-1A adrenoreceptor

Antagonism of the receptor leads to relaxation of smooth muscle in the prostate and bladder neck, improving urine flow (StatPearls, NBK538498). Agonism leads to smooth muscle contraction and vasoconstriction (UniProt, P35348).