Synthesis and Pharmacological Characterization of a Series of Geometrically Constrained 5-HT2A/2C Receptor Ligands

JJ Chambers, JC Parrish, NH Jensen… - Journal of medicinal …, 2003 - ACS Publications
In studies of the SAR of phenethylamine-type serotonin 5-HT2A receptor agonists,
substituted conformationally constrained tetrahydronaphthofurans were designed to …

Structural determinants of 5-HT1A versus 5-HT1D receptor binding site selectivity

MA Harrington, AJ Sleight, J Pitha… - European journal of …, 1991 - Elsevier
A structure-activity analysis was used to identify selective 5-HT 1A versus 5-HT 1D receptor
agents. An analysis of published data identified 13 drugs which display nanomolar affinity …

MDL 72832: a potent and stereoselective ligand at central and peripheral 5-HT1A receptors

AK Mir, M Hibert, MD Tricklebank… - European journal of …, 1988 - Elsevier
In receptor binding assays (±) MDL 72832, 8-[4-(1, 4-benzodioxan-2-ylmethylamino) butyl] 8-
azaspiro [4, 5] decane-7, 9-dione, was a potent (pIC 50 9.1), selective and stereospecific …

Structural Combination of Established 5‐HT2A Receptor Ligands: New Aspects of the Binding Mode

V Kramer, MM Herth, MA Santini… - Chemical biology & …, 2010 - Wiley Online Library
MH. MZ, MDL 100907, and altanserin are structurally similar 4‐benzoyl‐piperidine
derivatives and are well accommodated to receptor interaction models. We combined …

[PDF][PDF] A Novel (Benzodifuranyl)aminoalkane with Extremely Potent Activity at the 5-HT2A Receptor

MA Parker, D Marona-Lewicka, VL Lucaites… - Journal of medicinal …, 1998 - thevespiary.org
A major focus of our research for a number of years has been to understand the structure-
activity relationship (SAR) of classical hallucinogens and their derivatives, the …

Molecular interaction of serotonin 5-HT2A receptor residues Phe339 (6.51) and Phe340 (6.52) with superpotent N-benzyl phenethylamine agonists

MR Braden, JC Parrish, JC Naylor, DE Nichols - Molecular pharmacology, 2006 - ASPET
Experiments were conducted to examine the molecular basis for the high affinity and
potency of a new class of 5-HT2A receptor agonists, N-benzyl phenethylamines …

Enantiospecific Synthesis and Pharmacological Evaluation of a Series of Super-Potent, Conformationally Restricted 5-HT2A/2C Receptor Agonists

JJ Chambers, DM Kurrasch-Orbaugh… - Journal of medicinal …, 2001 - ACS Publications
The affinity of ligands for either the 5-HT2A or 5-HT2C agonist binding site was enhanced by
modification of the 2, 5-oxygen substituents that are found in typical hallucinogenic …

Molecular Design of Novel Ligands for 5-HT1A Receptors

AA Hancock, MD Meyer… - Journal of receptor …, 1991 - Taylor & Francis
Abstract Serotonin (5-HT) is a potent bioactive substance known to function through a
number of different receptor types and subtypes. In our attempt to develop new agents that …

Novel Potent and Selective Central 5-HT3 Receptor Ligands Provided with Different Intrinsic Efficacy. 2. Molecular Basis of the Intrinsic Efficacy of Arylpiperazine Derivatives at …

A Cappelli, M Anzini, S Vomero, L Canullo… - Journal of medicinal …, 1999 - ACS Publications
Novel 5-HT3 receptor ligands were designed and synthesized with the aim of obtaining
deeper insight into the molecular basis of the intrinsic efficacy of arylpiperazines interacting …

The role of lipophilicity in determining binding affinity and functional activity for 5-HT2A receptor ligands

MA Parker, DM Kurrasch, DE Nichols - Bioorganic & medicinal chemistry, 2008 - Elsevier
The lipophilicity of a set of 5-HT2A ligands was determined using immobilized-artificial-
membrane chromatography, a method that generates values well correlated with octanol …