Description
Terazosin hydrochloride is a highly water-soluble antihypertensive agent with a
structure and profile closely related to that of prazosin.
Uses
An α-1-adrenergicblocker related to prazosin.
Uses
Terazosin hydrochloride has been used for orthogonality and similarity analysis using reversed-phase chromatographic studies
5. Furthermore, terazosin has also been used for the evaluation of chemometric techniques to determine orthogonality and similarity in chromatographic methods
6.
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
