Design and synthesis of new potent, silent 5-HT1A antagonists by covalent coupling of aminopropanol derivatives with selective serotonin reuptake inhibitors.

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Perez M, Pauwels PJ, Pallard-Sigogneau I, Fourrier C, Chopin P, Palmier C, Colovray V, Halazy S

Design and synthesis of new potent, silent 5-HT1A antagonists by covalent coupling of aminopropanol derivatives with selective serotonin reuptake inhibitors.

Bioorg Med Chem Lett. 1998 Dec 1;8(23):3423-8.

PubMed ID

9873746 [ View in PubMed

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Abstract

Hybrid molecules built up by covalent coupling of aminopropanol derivatives (especially pindolol) with antidepressant drugs like fluoxetine, paroxetine or milnacipran were found to be potent and silent 5-HT1A antagonists (KB < 1 nM for 7c and 9a).

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Pindolol	5-hydroxytryptamine receptor 1A	Ki (nM)	110	N/A	N/A	Details