Top Abstract Purchase Related
Home
>
Node
>
Subnode

Pharmacological properties of YM-15430-1, a 1,4-dihydropyridine derivative with beta 1-adrenoceptor-blocking activity

Shibasaki, K.; Uchida, W.; Shirai, Y.; Inagaki, O.; Asano, M.; Takenaka, T.

Archives Internationales de Pharmacodynamie et de Therapie 328(2): 213-224

1994

ISSN/ISBN: 0003-9780
PMID: 7710306
Document Number: 431998
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.

Document emailed within 1 workday
Secure & encrypted payments

Asano, M.; Uchida, W.; Shibasaki, K.; Terai, M.; Inagaki, O.; Takenaka, T.; Matsumoto, Y.; Fujikura, T. 1990: Pharmacological profiles of YM-16151-1 and its optical isomers: a novel calcium entry blocking and selective beta-1 adrenoceptor blocking agent Journal of Pharmacology and Experimental Therapeutics 254(1): 204-211
Armah, B.I.; Hofferber, E.; Stenzel, W. 1988: Pharmacological properties of the positive inotropic and alpha 1-adrenoceptor blocking agent saterinone Arzneimittel-Forschung 38(9): 1287-1292
Miyagishi, A.; Nakahara, H.; Hara, Y. 1984: Adrenoceptor blocking effects of arotinolol, a new combined alpha- and beta-adrenoceptor blocking agent Archives Internationales de Pharmacodynamie et de Therapie 271(2): 249-262
Hellenbrecht, D.; Gortner, L. 1976: Correlations between hydrophobicity and non-specific pharmacological effects of beta-adrenoceptor blocking agents Polish Journal of Pharmacology and Pharmacy 28(6): 625-630
Hellenbrecht, D.; Enenkel, J. 1984: Estimation of the nonspecific cardiovascular toxicity of beta-adrenoceptor blocking drugs with different hydrophobic properties in the cat Arzneimittel-Forschung 34(9): 980-983
Conde, S.; Corral, C.; Lissavetzky; Darias, V.; Martin, D. 1986: Synthesis and beta-adrenoceptor blocking activity of thiophenic analogues of metoprolol Il Farmaco; Edizione Scientifica 41(1): 80-88
Yamamoto, N.; Nomura, M.; Okubo, K.; Maeda, K.; Goto, T. 1999: Pharmacologic characterization of FR172516: a new combined calcium channel-blocking and beta-adrenoceptor-blocking agent Journal of Cardiovascular Pharmacology 33(4): 587-594
Hara, Y.; Sato, E.; Miyagishi, A.; Aono, S.; Nakatani, H. 1979: Pharmacological properties of dl-2-(3'-t-butylamino-2'-hydroxypropylthio)-4-(5'-carbamoyl-2'-thienyl) thiazole hydrochloride (S-596), a new beta-adrenergic blocking agent Nihon Yakurigaku Zasshi. Folia Pharmacologica Japonica 75(7): 707-720
Shanks, R.G. 1981: Review of a review. Partial agonist activity of beta-adrenoceptor blocking drugs European Heart Journal 2(3): 253-255
Nakayama, K.; Kurihara, J.; Miyajima, Y.; Ishii, K.; Kato, H. 1985: Calcium antagonistic properties of nicardipine, a dihydropyridine derivative assessed in isolated cerebral arteries and cardiac muscle Arzneimittel-Forschung 35(4): 687-693
Conway, J. 1980: The antihypertensive action of beta-adrenoceptor blocking agents Archives Internationales de Pharmacodynamie et de Therapie Suppl: 83-91
Lorimer, A.R.; Jones, J.V.; Clark, B.; Dunn, F.G.; Melville, D.; Lawrie, T.D. 1976: Indications for beta-adrenoceptor blocking drugs in hypertension Postgraduate Medical Journal 52(Suppl 4): 81-85
Di Luzio, V.; Purcaro, A.; Curzi, G.; Di Segni, E.; Chiesa, R.; Di Giuseppe, F. 1972: Effects on the contractile state of the myocardium and anti-arrhythmic properties of practolol, a beta-blocking agent with cardioselective activity Bollettino Della Societa Italiana di Cardiologia 17(3): 179-187
Mostaghim, R.; Maddox, Y.T.; Ramwell, P.W. 1986: Endothelial potentiation of relaxation response to beta adrenoceptor blocking agents Journal of Pharmacology and Experimental Therapeutics 239(3): 797-801
Schneider, R.E.; Bishop, H.; Kendall, M.J.; Quarterman, C.P. 1981: Effect of inflammatory disease on plasma concentrations of three beta-adrenoceptor blocking agents International Journal of Clinical Pharmacology Therapy and Toxicology 19(4): 158-162
Keith, R.A.; Hwang, T.F.; Murthy, V.S.; Kau, S.T.; Salama, A.I.; Giles, R.E. 1989: ICi 147,798: a slowly dissociable beta adrenoceptor antagonist that causes insurmountable beta-1 and surmountable beta-2 adrenoceptor antagonism in isolated tissues Journal of Pharmacology and Experimental Therapeutics 248(1): 240-248
Elonen, E. 1975: Effect of beta-adrenoceptor blocking drugs, physostigmine, and atropine on the toxicity of doxepin in mice Medical Biology 53(4): 231-237
Hamilton, T.C.; Parkes, M.W. 1977: Bufuralol, a new beta-adrenoceptor blocking agent in a series of benzofuran-2-ethanolamines. Part 2: pharmacology Arzneimittel-Forschung 27(7): 1410-1417
Takenaka, T.; Usuda, S.; Nomura, T.; Maeno, H.; Sado, T. 1976: Vasodilator profile of a new 1,4-dihydropyridine derivative, 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid 3-[2-(N-benzyl-N-methylamino)]-ethyl ester 5-methyl ester hydrochloride (YC-93) Arzneimittel-Forschung 26(12): 2172-2178
Batrak, G.E.; Zlenko, E.T.; Khrustalev, S.I.; Khmel', M.P.; Malinovskiĭ, M.S. 1979: Pharmacological properties of a new benzimidazole derivative Farmakologiia i Toksikologiia 42(5): 511-515