77799-96-3Relevant academic research and scientific papers
Molecular properties of the adrenergic α-receptor. 4. Topographical and structural differences between tissue-specific binding sites as revealed by benextramine and analogues
Melchiorre,Giannella,Brasili,et al.
, p. 111 - 114 (2007/10/02)
Until recently, it has been tacitly assumed that the postsynaptic or α1-adrenoreceptors of diverse biological origins are pharmacologically similar. Quantitative evidence is now available that significant differences may exist between the α1-receptors of different tissues and species. α1-receptor authors submit experimental evidence which demonstrates that the α.1-receptor binding sites of the rat vas deferens and rabbit aorta or left atrium exhibit stereochemical and structural differences. Furthermore, the topographical dualism underlying the respective effects of Benextramine and N,N'-bis(8-amino-n-octyl)cystamine on rat vas deferens apply also to rabbit aorta. In addition, the tetramine disulfides incorporating catechol nuclei showed high potency toward the α1-receptors of both rat vas deferens and rabbit aorta. Optimum activity was sharply associated on both tissues with those 3',4'-dihydroxybenzyl compounds having a six- and eight-carbon chains. The mechanistic and topographical significance of this dualism is discussed.
