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- W2067945941 abstract "Abstract The α adrenergic agonistic activity of a number of imidazolines was measured on the α adrenergic receptors of the isolated rabbit intestine. A number of imidazolines were full agonists having an intrinsic activity constant equal to 1 in relation to noradrenaline as a standard. Some other derivatives had only partial agonist activity. The affinities of the imidazolines for these adrenergic receptors was assessed using pD 2 values. The pD 2 values were correlated with a number of physicochemical parameters of the drugs, i.e. pK a , the molar volume and the apparent and true partition coefficients (APC and TPC respectively) by stepwise regression analysis. Results indicate that pD 2 was correlated with pK a primarily, whereas molar volume also was a factor determining agonistic activity at the peripheral α adrenergic receptor. Central α adrenergic receptor stimulating properties of the imidazolines were determined by measuring bradycardia induced by these agents after intrahypothalamic injection into rats. Although it was not possible to correlate central α adrenergic activity with any of the physicochemical parameters due to the lack of action of a number of imidazolines, results show that structural requirements for central α adrenergic activity clearly differ from those for peripheral α adrenergic activity. These data are discussed in view of the mechanism of action of the antihypertensive imidazoline clonidine." @default.
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- W2067945941 title "Structure activity relationship for central and peripheral alpha adrenergic activities of imidazoline derivatives" @default.
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- W2067945941 doi "https://doi.org/10.1016/0024-3205(75)90487-7" @default.
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