Prazosin binding site

E Brunner and W. E. Muller, Prazosin binding to human aj-add glycoprotein (orosmucoid), human serum albumin, and human serum. Further characterisation of the single drug binding site of orosmucoid, /. Pkarm. Pharmacd.. 37 305 (1985). 

Ishiguro M, Futabayashi Y, Ohnuki T, Ahmed M, Muramatsu I, Nagatomo T. Identification of binding sites of prazosin, tamsulosin and KMD-3213 with a,-adrenergic receptor subtypes by molecular modeling. Life Sci 2002 71 2531-2541. 

Shapiro, A.B., K. Fox, P. Lam and V. Ling. Stimulation of P-glycoprotein-mediated drug transport by prazosin and progesterone. Evidence for a third drug-binding site. Eur. J. Biochem. 259 841-850, 1999. 

We chose to examine the receptor subtype selectivity of selected tetraamines 3,5-9 by employing receptor binding assays. [ HJPrazosin was used to label uia and aiB-adrenoreceptors binding sites of rat submaxillary gland and liver homogenates, respectively. Prazosin, benextramine and the aiB-selective antagonist spiperone [11] were used as the standard compounds. 

The compound bearing an A, A -dimethyl-1,6-hexane-diamine moiety (2) was the most active of the series, being more potent than prazosin (Giardinh et al., 1989). The chain length effect on potency allowed us to postulate that the rat vas deferens a,-adrenoreceptor incorporates a lipophilic area, located between the binding sites for the quinazoline and the furan rings of prazosin, which can optimally accommodate an hexane spacer. 

Displaces warfarin from plasma protein binding sites. Reduces natriuretic and diuretic effects of furosemide and antihypertensive effects of thiazides, beta blockers, prazosin, and captopril. 

It has been advanced that benextramine and prazosin may interact with the very same site where norepinephrine binds. On the basis of substituents effects and taking advantage of the finding that norepinephrine at a relatively low concentration (30 pM) afforded complete protection of aortic ai-adrenoreceptors... 

---