Sympathomimetics structure-activity relationship

Knowledge of structure-activity relationships has permitted the synthesis of sympathomimetics that display a high degree of selectivity at adrenoceptor subtypes. 

I. Structure-activity relationships of halogenated sympathomimetic amines... 

Structure-activity relationships (SAR) in sympathomimetic amines must then deal with the effect of molecular structure on ... 

It had been recognized early on (71) that there were similarities between the effects of administration adrenal gland extracts and stimulation of the sympathetic nervous system. Elliot (72) suggested that adrenaline might be released by sympathetic nerve stimulation and over the years the term adrenergic nerves became effectively synonymous with sympathetic nerves. In 1910 Barger and Dale (73) reported a detailed structure-activity relationship study of epinephrine analogs and introduced the term sympathomimetic for chemicals that mimicked the effects of sympathetic nerve stimulation, but they also noted some important differences between the effects of administered adrenaline and stimulation of sympathetic nerves. It was not until... 

Structure activity relationships for a series of sympathomimetic amines having a carbostyril moiety (11) have been reported.35 The most potent (11, R3=H, R4=t-butyl) is 22,400 x isoproterenol in relaxation of guinea pig trachea, and is also more fi-2 selective than 4. Order of activity Rg H>Me>Et, R4 t-butyl>i-Pr>CMe2CH20> Bz>H.35 Another analog (11, R3=Et, R4=CHMe9) (OPC 2009) is claimed to be more active and more selective... 

Non-Phenethylamine Derivatives - The search for compounds which bear no structural relationship to phenethylamlnes and have anorectic properties continues. Current studies on Wy-5244 (XIV) show it to possess only weak sympathomimetic activity in isolated cat atria and rabbity aortic strips however the compound apparently does alter adrenergic receptor mechanisms since the actions of substances such as norepinephrine, d-amphetamine, phenoxybenzamine, and Imlpramine were profoundly influenced by Wy-5244.31 The synthesis of (XIV) and related compounds has been described.32... 

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