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Development of 2-Aminotetralin-Type Serotonin 5-HT₁ Agonists: Molecular Determinants for Selective Binding and Signaling at 5-HT_1A, 5-HT_1B, 5-HT_1D, and 5-HT_1F Receptors.

ABSTRACT: The serotonin (5-hydroxytryptamine, 5-HT) 5-HT₁ G-protein coupled receptor subtypes (5-HT_{1A/1B/1D/1E/1F}) share a high sequence homology, confounding development of subtype-specific ligands. This study used a 5-HT₁ structure-based ligand design approach to develop subtype-selective ligands using a 5-substituted-2-aminotetralin (5-SAT) chemotype, leveraging results from pharmacological, molecular modeling, and mutagenesis studies to delineate molecular determinants for 5-SAT binding and function at 5-HT₁ subtypes. 5-SATs demonstrated high affinity (K_i ≤ 25 nM) and at least 50-fold stereoselective preference ([2S] > [2R]) at 5-HT_1A, 5-HT_1B, and 5-HT_1D receptors but essentially nil affi

SUBMITTER: McGlynn RP

PROVIDER: S-EPMC10797628 | biostudies-literature | 2024 Jan

REPOSITORIES: biostudies-literature

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Dataset Information

Development of 2-Aminotetralin-Type Serotonin 5-HT₁ Agonists: Molecular Determinants for Selective Binding and Signaling at 5-HT_1A, 5-HT_1B, 5-HT_1D, and 5-HT_1F Receptors.

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Development of 2-Aminotetralin-Type Serotonin 5-HT1 Agonists: Molecular Determinants for Selective Binding and Signaling at 5-HT1A, 5-HT1B, 5-HT1D, and 5-HT1F Receptors.

OmicsDI is part of the ELIXIR infrastructure

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Development of 2-Aminotetralin-Type Serotonin 5-HT₁ Agonists: Molecular Determinants for Selective Binding and Signaling at 5-HT_1A, 5-HT_1B, 5-HT_1D, and 5-HT_1F Receptors.