1,4-Dihydropyridine activators in the tiamdipine series. 1990

F Galletti, and E Luchowski, and D J Triggle
Department of Biochemical Pharmacology, School of Pharmacy, State University of New York, Buffalo 14260.

The pharmacologic and radioligand binding properties of 5-nitro analogs of the 1,4-dihydropyridine Ca2+ channel antagonist, tiamdipine (2-(2-aminoethylthio)methyl-3-carbomethoxy-5-carbomethoxy-6-m ethyl-4-(3-nitrophenyl)-1,4-dihydropyridine) and its N-formyl derivative have been measured in rat tail artery, guinea pig ileum and rat heart. The enantiomers of both analogs showed activator and antagonist properties, the latter being exhibited at lower concentrations.

UI MeSH Term Description Entries
D007082 Ileum The distal and narrowest portion of the SMALL INTESTINE, between the JEJUNUM and the ILEOCECAL VALVE of the LARGE INTESTINE.
D008297 Male Males
D009119 Muscle Contraction A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments. Inotropism,Muscular Contraction,Contraction, Muscle,Contraction, Muscular,Contractions, Muscle,Contractions, Muscular,Inotropisms,Muscle Contractions,Muscular Contractions
D009130 Muscle, Smooth Unstriated and unstriped muscle, one of the muscles of the internal organs, blood vessels, hair follicles, etc. Contractile elements are elongated, usually spindle-shaped cells with centrally located nuclei. Smooth muscle fibers are bound together into sheets or bundles by reticular fibers and frequently elastic nets are also abundant. (From Stedman, 25th ed) Muscle, Involuntary,Smooth Muscle,Involuntary Muscle,Involuntary Muscles,Muscles, Involuntary,Muscles, Smooth,Smooth Muscles
D009131 Muscle, Smooth, Vascular The nonstriated involuntary muscle tissue of blood vessels. Vascular Smooth Muscle,Muscle, Vascular Smooth,Muscles, Vascular Smooth,Smooth Muscle, Vascular,Smooth Muscles, Vascular,Vascular Smooth Muscles
D009206 Myocardium The muscle tissue of the HEART. It is composed of striated, involuntary muscle cells (MYOCYTES, CARDIAC) connected to form the contractile pump to generate blood flow. Muscle, Cardiac,Muscle, Heart,Cardiac Muscle,Myocardia,Cardiac Muscles,Heart Muscle,Heart Muscles,Muscles, Cardiac,Muscles, Heart
D010069 Oxadiazoles Compounds containing five-membered heteroaromatic rings containing two carbons, two nitrogens, and one oxygen atom which exist in various regioisomeric forms. Oxadiazole
D011189 Potassium Chloride A white crystal or crystalline powder used in BUFFERS; FERTILIZERS; and EXPLOSIVES. It can be used to replenish ELECTROLYTES and restore WATER-ELECTROLYTE BALANCE in treating HYPOKALEMIA. Slow-K,Chloride, Potassium
D011869 Radioligand Assay Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders). Protein-Binding Radioassay,Radioreceptor Assay,Assay, Radioligand,Assay, Radioreceptor,Assays, Radioligand,Assays, Radioreceptor,Protein Binding Radioassay,Protein-Binding Radioassays,Radioassay, Protein-Binding,Radioassays, Protein-Binding,Radioligand Assays,Radioreceptor Assays
D011921 Rats, Inbred WKY A strain of Rattus norvegicus used as a normotensive control for the spontaneous hypertensive rats (SHR). Rats, Wistar Kyoto,Wistar Kyoto Rat,Rats, WKY,Inbred WKY Rat,Inbred WKY Rats,Kyoto Rat, Wistar,Rat, Inbred WKY,Rat, WKY,Rat, Wistar Kyoto,WKY Rat,WKY Rat, Inbred,WKY Rats,WKY Rats, Inbred,Wistar Kyoto Rats

Related Publications

F Galletti, and E Luchowski, and D J Triggle
December 1989, Trends in pharmacological sciences,
F Galletti, and E Luchowski, and D J Triggle
September 2009, Journal of medicinal chemistry,
F Galletti, and E Luchowski, and D J Triggle
May 1989, Canadian journal of physiology and pharmacology,
F Galletti, and E Luchowski, and D J Triggle
June 1998, Bioorganic & medicinal chemistry,
F Galletti, and E Luchowski, and D J Triggle
February 2011, European journal of medicinal chemistry,
F Galletti, and E Luchowski, and D J Triggle
November 2010, Indian journal of pharmaceutical sciences,
F Galletti, and E Luchowski, and D J Triggle
June 2018, Royal Society open science,
F Galletti, and E Luchowski, and D J Triggle
July 2013, Magnetic resonance in chemistry : MRC,
Copied contents to your clipboard!