In‐vivo Binding of (+)‐[3H]PN 200–110 to Peripheral Tissues and Brain of Spontaneously Hypertensive Rats: Effect of Lacidipine
作者： T. MENNINI , C. TADDEI , A. USLENGHI , A. CAGNOTTO , D. MICHELI
DOI: 10.1111/J.2042-7158.1993.TB05570.X
关键词:
摘要: The time-course of dihydropyridine receptor occupancy by lacidipine and its relationship with pharmacological activity has been studied in spontaneously hypertensive rat (SHR), as measured the inhibition specific (+)-[3H]PN 200-110 binding in-vivo. After oral administration doses active reducing blood pressure, did not show tissue target differences respect to sites labelled cerebral cortex, heart, ileum, bladder thoracic aorta. relative receptors heart 60 min after 1 mg kg-1 was 75%. 12 h, when still effective pressure SHR, a low (15%) but detectable proportion occupied drug. percentage decrease linear obtained different lacidipine; that is, there close correspondence between ED25 for (0.33 kg-1) (0.36 kg-1). long-lasting effect on might be explained selective interaction in-vivo 200-110.
elsevier.com
sci-hub.se 参考文章(12)
Seiji Ichida, Takashi Fujisue, Atuhiro Masada, Yasuo Oda, Narihisa Matsuda, Shigeru Aonuma, Characteristics of Specific Bindings of Nitrendipine and PN200–110 to Various Crude Membranes: Induction of Irreversible Bindings by UV Irradiation The Journal of Biochemistry. ,vol. 105, pp. 760- 766 ,(1989) , 10.1093/OXFORDJOURNALS.JBCHEM.A122741
Nicole Morel, Theophile Godfraind, Prolonged depolarization increases the pharmacological effect of dihydropyridines and their binding affinity for calcium channels of vascular smooth muscle. Journal of Pharmacology and Experimental Therapeutics. ,vol. 243, pp. 711- 715 ,(1987)
R. Cort�s, P. Supavilai, M. Karobath, J. M. Palacios, Calcium antagonist binding sites in the rat brain: Quantitative autoradiographic mapping using the 1,4-dihydropyridines [3H]PN 200-110 and [3H]PY 108-068 Journal of Neural Transmission. ,vol. 60, pp. 169- 197 ,(1984) , 10.1007/BF01249092
D. Micheli, A. Collodel, C. Semeraro, G. Gaviraghi, C. Carpi, Lacidipine: a calcium antagonist with potent and long-lasting antihypertensive effects in animal studies. Journal of Cardiovascular Pharmacology. ,vol. 15, pp. 666- 675 ,(1990) , 10.1097/00005344-199004000-00020
Howard R. Lee, William R. Roeske, Henry I. Yamamura, High affinity specific [3H](+)PN 200-110 binding to dihydropyridine receptors associated with calcium channels in rat cerebral cortex and heart. Life Sciences. ,vol. 35, pp. 721- 732 ,(1984) , 10.1016/0024-3205(84)90340-0
C. Dacquet, G. Loirand, L. Rakotoarisoa, C. Mironneau, J. Mironneau, (+)−[3H]‐PN 200–110 binding to cell membranes and intact strips of portal vein smooth muscle: characterization and modulation by membrane potential and divalent cations British Journal of Pharmacology. ,vol. 97, pp. 256- 262 ,(1989) , 10.1111/J.1476-5381.1989.TB11949.X
BalwantS. Tuana, BrianJ. Murphy, Qu Yi, The purified Ca2+ antagonist receptor from skeletal muscle: subunit structure, photoaffinity labeling and endogenous protein kinase activity. Molecular and Cellular Biochemistry. ,vol. 80, pp. 133- 143 ,(1989) , 10.1007/BF00231011
Jean-Louis Pinquier, Saik Urien, Philippe Chaumet-Riffaud, Aime Comte, Jean-Paul Tillement, Binding of [3H]isradipine (PN 200-110) on smooth muscle cell membranes from different bovine arteries. Journal of Cardiovascular Pharmacology. ,vol. 11, pp. 402- 406 ,(1988) , 10.1097/00005344-198804000-00004
Hans Schoemaker, Howard R. Lee, William R. Roeske, Henry I. Yamamura, In vivo identification of calcium antagonist binding sites using [3H]nitrendipine European Journal of Pharmacology. ,vol. 88, pp. 275- 276 ,(1983) , 10.1016/0014-2999(83)90019-5
Toni SCHNEIDER, Franz HOFMANN, The bovine cardiac receptor for calcium channel blockers is a 195-kDa protein. FEBS Journal. ,vol. 174, pp. 369- 375 ,(1988) , 10.1111/J.1432-1033.1988.TB14107.X