geoscience.net logo
+ Resolve Article
+ Follow Us
Follow on FacebookFollow on Facebook
Follow on TwitterFollow on Twitter

+ Translate
+ Subscribe to Site Feed
GeoScience Most Shared ContentMost Shared Content

Quantitative evaluation of the beta 2-adrenoceptor affinity of phenoxypropanolamines and phenylethanolamines


, : Quantitative evaluation of the beta 2-adrenoceptor affinity of phenoxypropanolamines and phenylethanolamines. Journal of Medicinal Chemistry 28(9): 1328-1334

The influence of the aromatic moiety of beta-adrenoceptor ligands on the affinity for the beta 2-adrenoceptor has been studied. Three classes of ligands have been examined, viz. N-isopropyl- and N-tert-butylphenylethanolamines and N-isopropylphenoxypropanolamines. Computer-assisted analysis of the inhibition by any of these ligands of the specific (-)-[3H]dihydroalprenolol binding to the beta 2-adrenoceptors of a bovine skeletal muscle preparation in the presence of GppNHp (10(-4) M) yielded the affinities of these ligands at pH 7.5. The obtained values were adjusted for the amounts of cations present at this pH value. A significant correlation was found between the calculated lipophilicities and the experimentally determined affinities in the three classes. Furthermore, steric factors seem to play an important role, as these correlations were improved by the introduction of steric parameters for the aromatic substituents in the regression analyses. From the established equations it is concluded that the phenoxypropanolamine derivatives bind to the beta 2-adrenoceptor in a way different from that of the ligands in both ethanolamine classes.

US$29.90

PMID: 2993621


Other references

Forman, L.; Matouskova, E.; Pech, Z.; Teply, M.; Dolezalek, J.; Vondruska, V., 1978: Method for the manufacture of whipped butter and whipped flavoured products based on butter. Butter is tempered to 12-40 deg C to soften or melt it and is then whipped to 130-220% overrun in a continuous scraped-surface cooler in an atmosphere of air or an inert gas. Optionally, flavouring substances, such as cocoa, honey or ham are added...

Bernat Adell, M.Desamparados., 2005: Thoughts after the SEEIUC Presidence. Enfermeria Intensiva 16(3): 97-99

Plakhotnik, V.V.; Onis' kova, M.G., 1986: Sources of resistance in breeding spring barley for immunity to loose smut. Over several years in northern Kazakhstan, 550 accessions from the collection of the Vavilov Institute of Plant Industry (VIR) were evaluated for resistance to Ustilago segetum var. nuda by vacuum inoculation of the ear with a spore suspension. Mo...

Obiedzinski, M.W., 2002: Health claims on food and food ingredients. This article discusses the health aspects of food and food ingredients. The importance of determining the health claims of food and food ingredients in order to have a proper diet, is also discussed.

Yoo, J.Gyu.; Demers, S-Pierre.; Lian, L.; Smith, L.C., 2007: Developmental arrest and cytoskeletal anomalies of rat embryos reconstructed by somatic cell nuclear transfer. Many factors influence success rates in animal cloning by somatic cell nuclear transfer (SCNT), including cell cycle stage of donor cells and recipient oocytes, the procedure of micromanipulation, and the activation protocol. This study was condu...

Mckenzie, K.; Jodari, F.G.deaux, A.P.llingue, R.G.stavson, B., 1984: Developing improved rice varieties for Louisiana. Annual progress report Louisiana Agricultural Experiment Station: 6th) 5-43

Churikova T.G., 1994: Crystallization differentiation of the basaltic magma of the Ploskie Sopky Volcano (Kamchatka). Pages (unpaginated 1994

Misra, D.; Prasad, R.B.an, S., 1969: Impact of soil conservation practices on crop production in India. Journal of soil and water conservation in India: 17 (1 2) 52-57

Anonymous, 1976: Spain: a good year despite soaring prices. Eurofruit 4 (12) 12-14

Browning, E.Hyatt, K.H., 1958: Scorpiones, Uropygi, Araneae, Opiliones and Scolopendromorph Chilopoda from Rennell Island. Natural History of Rennell lslands. 1957( ); 2: 71-81