Naftopidil, a new adrenoceptor blocking agent with Ca(2+)-antagonistic properties: interaction with adrenoceptors.

@article{Sponer1992NaftopidilAN,
  title={Naftopidil, a new adrenoceptor blocking agent with Ca(2+)-antagonistic properties: interaction with adrenoceptors.},
  author={Gisbert Sponer and Harald O. Borbe and Bernd M{\"u}ller-Beckmann and P Freud and Burkhard Jakob},
  journal={Journal of cardiovascular pharmacology},
  year={1992},
  volume={20 6},
  pages={1006-13}
}
The interaction of naftopidil with adrenoceptors was studied in comparison to standard drugs. Naftopidil binds specifically to alpha 1-adrenoceptors. The Ki values are 58.3 nM for naftopidil, 0.43 nM for prazosin, and 197 nM for urapidil. The affinities of naftopidil to alpha 2- and beta-adrenoceptor sites are very low (> 6,000 and > 2,500 nM). Naftopidil relaxes aortic strips precontracted with norepinephrine concentration-dependently, and it shifts the concentration-response curve of… CONTINUE READING