Erowid References Database
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Glennon RA, Kier LB.
“LSD Analogs as Serotonin Antagonists: a Molecular Connectivity SAR analysis”.
Europ. J. Med. Chem.. 1978;13(3):219-222.
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Abstract
The serotonin (5-HT) antagonist activity of 16 LSD analogs was analysed by a molecular connectivity approach using anti-5HT data reported previously, (Cerletti and Doopiner J.Pharmacol,Exp. Ther. 1958, 122, 124). The biological activity of the 16 analogues of LSD was converted to a logarithm of relative biological response and this related well to 3 connectivity indices. The equation evolved accounted for 880f the variation in activity and, excluding the isopropyl amides 6 and 7, can account for 970f the variance in activity. The 5-HT antagonistic activity of LSD analogues is influenced by the amide substitutents and is optimal for LSD itself. It is proposed that compounds (1 ; R = Pr; R1 = Et) and (1; R = Me; R = Pr) should haye high potency. (SEE CHART WITH PAPER)
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