Interaction of a beta-adrenergic partial agonist with its receptor in guinea-pig taenia caecum. 1984

K Koike, and I Takayanagi

Beta-adrenoceptor mechanisms in guinea-pig taenia caecum were studied by means of a receptor-binding technique. Hill plots of test drugs obtained from inhibition curves were linear with slopes which were equal to 1.00. pKi-values of isoprenaline and desisopropylprocaterol were in agreement with those pD2-values. pKi-value of carteolol was in agreement with its pA2-value. The beta-adrenoceptor is suggested to have two different sites; one can interact with the agonist and partial agonist and the other can interact with the antagonist and partial agonist.

UI MeSH Term Description Entries
D007545 Isoproterenol Isopropyl analog of EPINEPHRINE; beta-sympathomimetic that acts on the heart, bronchi, skeletal muscle, alimentary tract, etc. It is used mainly as bronchodilator and heart stimulant. Isoprenaline,Isopropylarterenol,4-(1-Hydroxy-2-((1-methylethyl)amino)ethyl)-1,2-benzenediol,Euspiran,Isadrin,Isadrine,Isopropyl Noradrenaline,Isopropylnoradrenaline,Isopropylnorepinephrine,Isoproterenol Hydrochloride,Isoproterenol Sulfate,Isuprel,Izadrin,Norisodrine,Novodrin,Hydrochloride, Isoproterenol,Noradrenaline, Isopropyl,Sulfate, Isoproterenol
D008297 Male Males
D008861 Microsomes Artifactual vesicles formed from the endoplasmic reticulum when cells are disrupted. They are isolated by differential centrifugation and are composed of three structural features: rough vesicles, smooth vesicles, and ribosomes. Numerous enzyme activities are associated with the microsomal fraction. (Glick, Glossary of Biochemistry and Molecular Biology, 1990; from Rieger et al., Glossary of Genetics: Classical and Molecular, 5th ed) Microsome
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
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
D011943 Receptors, Adrenergic, beta One of two major pharmacologically defined classes of adrenergic receptors. The beta adrenergic receptors play an important role in regulating CARDIAC MUSCLE contraction, SMOOTH MUSCLE relaxation, and GLYCOGENOLYSIS. Adrenergic beta-Receptor,Adrenergic beta-Receptors,Receptors, beta-Adrenergic,beta Adrenergic Receptor,beta-Adrenergic Receptor,beta-Adrenergic Receptors,Receptor, Adrenergic, beta,Adrenergic Receptor, beta,Adrenergic beta Receptor,Adrenergic beta Receptors,Receptor, beta Adrenergic,Receptor, beta-Adrenergic,Receptors, beta Adrenergic,beta Adrenergic Receptors,beta-Receptor, Adrenergic,beta-Receptors, Adrenergic
D002354 Carteolol A beta-adrenergic antagonist used as an anti-arrhythmia agent, an anti-angina agent, an antihypertensive agent, and an antiglaucoma agent. Carteolol Hydrochloride,Carteolol Monohydrochloride,OPC-1085,Hydrochloride, Carteolol,Monohydrochloride, Carteolol,OPC 1085,OPC1085
D002432 Cecum The blind sac or outpouching area of the LARGE INTESTINE that is below the entrance of the SMALL INTESTINE. It has a worm-like extension, the vermiform APPENDIX. Cecums
D004082 Dihydroalprenolol Hydrogenated alprenolol derivative where the extra hydrogens are often tritiated. This radiolabeled form of ALPRENOLOL, a beta-adrenergic blocker, is used to label the beta-adrenergic receptor for isolation and study. 1-((Methylethyl)amino)-3-(2-propylphenoxy)-2-propanol
D004983 Ethanolamines AMINO ALCOHOLS containing the ETHANOLAMINE; (-NH2CH2CHOH) group and its derivatives. Aminoethanols

Related Publications

K Koike, and I Takayanagi
June 1979, Japanese journal of pharmacology,
K Koike, and I Takayanagi
August 1976, Canadian journal of physiology and pharmacology,
K Koike, and I Takayanagi
December 1969, Japanese journal of pharmacology,
K Koike, and I Takayanagi
September 1969, European journal of pharmacology,
K Koike, and I Takayanagi
August 1972, European journal of pharmacology,
K Koike, and I Takayanagi
April 1988, Japanese journal of pharmacology,
K Koike, and I Takayanagi
July 1966, The Journal of physiology,
K Koike, and I Takayanagi
February 1966, The Journal of physiology,
Copied contents to your clipboard!