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(R)-Terazosin

Names

[ CAS No. ]:
109351-34-0

[ Name ]:
(R)-Terazosin

[Synonym ]:
terazosin
R(+)-2-[4-[(tetrahydro-2-furanyl)carbonyl]-1-piperazinyl]-6,7-dimethoxy-4-quinazolinamine
(+)-(R)-terazosin
R(+)-terazosin

Biological Activity

[Description]:

(R)-Terazosin is the R-enantiomer of Terazosin. (R)-Terazosin is a potent α-adrenoceptor antagonist with Ki values of 6.51 nM, 1.01 nM and 1.97 nM for α1a, α1b and α1d-adrenoceptor, respectively[1].

[Related Catalog]:

Research Areas >> Endocrinology
Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor

[Target]

Ki: 6.51 nM (α1a-adrenoceptor), 1.01 nM (α1b-adrenoceptor) and 1.97 nM (α1d-adrenoceptor)[1]


[In Vitro]

(R)-Terazosin is of low affinity for α2a, α2B and α2c-adrenoceptor with Ki values of 3.85 μM, 0.33 μM and 0.37 μM, respectively[1]. (R)-Terazosin may prove to be a useful probe in understanding the functional role of subtypes of adrenoceptors in various tissues. Because it is a weaker antagonist at α2B sites than its enantiomer, it may be possible to use (R)-Terazosin to differentiate between pharmacological effects mediated by subtypes of α2-adrenoceptors in animal studies[1].

[In Vivo]

(R)-Terazosin shows antagonism of at rat atrial α2B receptor with a pEC30 of 5.69. (R)-Terazosin shows antagonism of at rat vas deferens α1A and α2A receptor with pA2 values of 7.5 and 5.31, respectively[1].

[References]

[1]. Hancock AA, et al. Actions of terazosin and its enantiomers at subtypes of alpha 1- and alpha 2-adrenoceptors in vitro. J Recept Signal Transduct Res. 1995 Sep-Dec;15(7-8):863-85.

Chemical & Physical Properties

[ Molecular Formula ]:
C19H25N5O4

[ Molecular Weight ]:
387.43300

[ Exact Mass ]:
387.19100

[ PSA ]:
103.04000

[ LogP ]:
1.64090

Related Compounds