Description
Terazosin hydrochloride is a highly water-soluble antihypertensive agent with a
structure and profile closely related to that of prazosin.
Brand name
Terazosin
is INN and BAN;HEITRIN.
General Description
Terazosin hydrochloride, 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-(tetrahydro-2-furoyl)piperazine monohydrochloride (Hytrin), is a structuralcongener of prazosin hydrochloride. It possessessimilar selective properties of specifically inhibiting 1-adrenergic receptors. The drug is slightly less potent thanprazosin hydrochloride. Terazosin hydrochloride has a halflifeof approximately 12 hours, which is much longer thanthat of prazosin. This lends itself to a once-daily dose tocontrol hypertension in many patients.
Biological Activity
α 1 - and α 2B -adrenoceptor antagonist (K i values are 3.3, 0.7, 1.1, 7.7, 1510 and 78.2 nM for α 1A , α 1B , α 1D , α 2B , α 2A and α 2C receptors respectively). Antihypertensive following oral or intravenous administration in vivo .
Biochem/physiol Actions
α1-adrenoceptor antagonist.
References
References/Citations
1) Hancock et al. (1995), Actions of terazosin and its enantiomers at subtypes of alpha-1 and alpha-2 adrenoceptors in vitro; Recept. Signal Transduct. Res., 15 863
2) Kyncl et al. (1986), Pharmacology of terazosin; Am. J. Med., 80 12
3) Shionoiri et al. (1994), Long-term therapy with terazosin may improve glucose and lipid metabolism in hypertensives: a multicenter prospective study; Am. J. Med. Sci., 307 Suppl 1 S91
4) Pan et al. (2003), Identification of apoptotic and antiangiogenic activities of terazosin in human prostate cancer and endothelial cells; J. Urol., 169 724
5) Chen et al. (2015), Terazosin activates Pgk1 and HSP90 to promote stress resistance; Nat. Chem. Biol., 11 19
