Journal of Medicinal Chemistry p. 463 - 467 (1986)
Update date:2022-08-17
Topics:
DeBernardis, John F.
Kyncl, John J.
Basha, Fatima Z.
Arendsen, David L.
Martin, Yvonne C.
et al.
The synthesis and pharmacology of 2-(5,6-dihydroxy-1,2,3,4-tetrahydro-1-naphthyl)imidazoline (A-54741, 4), a very potent α-adrenergic agonist, are described.The change in biological activity resulting from variation of the carboxylic ring size of 4 from four through seven members (2-5) is presented, as well as an explanation that accounts for this change in activity by considering the "exactness of fit" of these compounds to both the α1- and α2-adrenergic receptors.Compound 4 was found in vitro to be a full agonist with greater potency at the α2 receptor (ED50 norepinephrine (NE)/ED50 4 = 188 +/- 22) than at the α1 receptor (ED50 NE/ED50 4 = 13 +/- 2).
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