N Almaula

2 papers in the library · 147 citations · publishing 1996

Papers

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Contribution of a helix 5 locus to selectivity of hallucinogenic and nonhallucinogenic ligands for the human 5-hydroxytryptamine2A and 5-hydroxytryptamine2C receptors: direct and indirect effects on ligand affinity mediated by the same locus.

Molecular Pharmacology July 1, 1996 N Almaula, Barbara J. Ebersole, J A Ballesteros et al.

An important determinant of the neurobehavioral responses induced by a drug is its relative receptor selectivity. The molecular basis of ligand selectivity of hallucinogenic and nonhallucinogenic compounds of varying structural classes for the human 5-hydroxytryptamine (5-HT)2A and 5-HT2C receptors was investigated with the use of reciprocal site-directed mutagenesis. Because these two closely...

DOI: 10.1016/s0026-895x(25)09149-7 Lysergic acid diethylamide Cell line Animals Humans +22

Mapping the binding site pocket of the serotonin 5-Hydroxytryptamine2A receptor. Ser3.36(159) provides a second interaction site for the protonated amine of serotonin but not of lysergic acid diethylamide or bufotenin.

Journal of Biological Chemistry June 21, 1996 N Almaula, Barbara J. Ebersole, D Zhang et al. 147 citations

Like other amine neurotransmitters that activate G-protein-coupled receptors, 5-hydroxytryptamine (5-HT) binds to the 5-HT2A receptor through the interaction of its cationic primary amino group with the conserved Asp3.32(155) in transmembrane helix 3. Computational experiments with a 5-HT2A receptor model suggest that the same functional group of 5-hydroxytryptamine also forms a hydrogen bond...

DOI: 10.1074/jbc.271.25.14672 Full text