Parallel synthesis of 3-aryloxy-2-propanolamines and evaluation as dual affinity 5-HT(1A) and 5-HT re-uptake ligands.

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van Niel MB, Beer MS, Castro JL, Cheng SK, Evans DC, Heald A, Hitzel L, Hunt P, Mortishire-Smith R, O'Connor D, Watt AP, MacLeod AM

Parallel synthesis of 3-aryloxy-2-propanolamines and evaluation as dual affinity 5-HT(1A) and 5-HT re-uptake ligands.

Bioorg Med Chem Lett. 1999 Nov 15;9(22):3243-8.

PubMed ID

10576696 [ View in PubMed

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Abstract

A solution phase synthesis for the preparation of 3-aryloxy-2-propanolamine libraries has been developed. This resulted in the identification of 5 as a ligand with dual affinity for 5-HT1A and serotonin reuptake receptors which shows excellent pharmacokinetic parameters.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Pindolol	5-hydroxytryptamine receptor 1A	EC 50 (nM)	27	N/A	N/A	Details
Pindolol	5-hydroxytryptamine receptor 1A	Ki (nM)	24	N/A	N/A	Details