These tools will no longer be maintained as of December 31, 2024. Archived website can be found here. PubMed4Hh GitHub repository can be found here. Contact NLM Customer Service if you have questions.


Pubmed for Handhelds

PUBMED FOR HANDHELDS

Search MEDLINE/PubMed

  • Title: Pharmacological properties of YM-15430-1, a 1,4-dihydropyridine derivative with beta 1-adrenoceptor-blocking activity.
    Author: Shibasaki K, Uchida W, Shirai Y, Inagaki O, Asano M, Takenaka T.
    Journal: Arch Int Pharmacodyn Ther; 1994; 328(2):213-24. PubMed ID: 7710306.
    Abstract:
    The pharmacological properties of YM-15430-1 and its stereoisomers (YM-15430-2, YM-15430-3 and YM-15430-4) were evaluated in in vitro experiments. In the rabbit isolated aorta, all compounds antagonized the CaCl2-induced contraction with a negative logarithm of the dissociation constant in calcium antagonism of 8.51, 7.13, 8.68 and 7.16, respectively. In the rat isolated right atrium, YM-15430-1 produced a competitive antagonism of the isoprenaline-induced tachycardia with a pA2 value of 7.59. YM-15430-2, YM-15430-3 and YM-15430-4 also antagonized the isoprenaline-induced tachycardia, with pA2 values of 7.91, 7.09 and 6.24, respectively. Because it was the most active of the 4 stereoisomers, YM-15430-1 was particularly studied. YM-15430-1 showed an about 100-fold greater selectivity for beta 1- than for beta 2-adrenoceptors, and had no intrinsic sympathomimetic activity. These results suggest that YM-15430-1 is a hybrid compound which combines calcium entry-blocking and selective beta 1-adrenoceptor-blocking activities in one molecule.
    [Abstract] [Full Text] [Related] [New Search]