- Structure-activity relationship studies of CNS agents. Part 9: 5-HT(1A) and 5-HT2 receptor affinity of some 2- and 3-substituted 1,2,3,4-tetrahydro-β-carbolines
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The 5-HT(1A) and 5-HT2 receptor affinity of 2- and 3-substituted 1,2,3,4-tetrahydro-β-carbolines 1-8, 10 and 12-15 has been determined. It has been found that the specific 5-HT(1A) affinity of the protonated form (K(i)(AH+)) of 2-n-hexyl derivatives 4, 8, 14 and (+)-LSD is of the same order. It has been shown by means of molecular modelling methods that pharmacophores of all the active compounds can adopt a common position at the 5-HT(1A) receptor model. The model also offers an explanation for the observed stereoselectivity of chiral compounds.
- Bojarski,Cegla,Charakchieva-Minol,Mokrosz,Mackowiak,Misztal,Mokrosz
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p. 289 - 294
(2007/10/02)
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