Terazosin is a Competitive and Orally Active α1-Adrenoceptor Antagonist

α1 Adrenergic receptor is a G protein-coupled receptor (GPCR) associated with GQ heterotrimeric G protein. Besides, α1-adrenergic receptors are including three highly homologous subtypes, namely α1A-, α1B -, and α1D adrenergic receptors subtype. The main factors involved in sympathetic control of blood pressure α1-adrenoceptor is α1D- and α1A adrenoceptor, which mediates peripheral vasoconstriction. Moreover, the α1A adrenoceptor may function mainly by entering Ca2+ through the L-type channel. And α1D adrenoceptors may function mainly through T-type channels and depleted Ca2+ storage. The α1-adrenergic receptor is a G protein-coupled receptor. Furthermore, it regulates the sympathetic nervous system by binding and activating the neurotransmitter norepinephrine and the neurohormone epinephrine.

Meanwhile, postsynaptic α1-adrenoceptor produces physiological effects by activating phospholipase C. Phospholipase C activates protein kinase C by increasing the concentration of inositol 1,4,5-triphosphate and diglyceride to mobilize intracellular calcium. Specifically, α1-adrenoceptors also activate other pathways, such as the mitogen-activated protein kinase pathway. Here, we will introduce an α1-adrenoceptor antagonist, Terazosin.

Terazosin is a Competitive and Orally Active α1-Adrenoceptor Antagonist.

At first, Terazosin is a quinazoline derivative and a competitive and orally active α1-adrenoceptor antagonist. Nonetheless, Terazosin works by relaxing blood vessels and the opening of the bladder. Importantly, Terazosin has the potential for benign prostatic hyperplasia (BPH) and high blood pressure treatment.

Next, Terazosin does not discriminate against cloned α1-adrenoceptor subtypes transiently expressed in COS cells. Particularly, Terazosin can promote stone discharge in the treatment of ureteral stones. Terazosin is reportedly safe and effective in the treatment of distal ureteral stones, especially stones >5 mm

Finally, Terazosin is a competitive and orally active α1-adrenoceptor antagonist.


Ju M, et al. J Int Med Res. 2020 Apr;48(4):300060520904851.