Indoloxypropanolamine analogues as 5-HT(1A) receptor antagonists.

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Krushinski JH Jr, Schaus JM, Thompson DC, Calligaro DO, Nelson DL, Luecke SH, Wainscott DB, Wong DT

Indoloxypropanolamine analogues as 5-HT(1A) receptor antagonists.

Bioorg Med Chem Lett. 2007 Oct 15;17(20):5600-4. Epub 2007 Aug 22.

PubMed ID

17804228 [ View in PubMed

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Abstract

Analogues of pindolol, 1-(1H-indol-4-yloxy)-3-isopropylamino-propan-2-ol, were synthesized and evaluated as 5-HT(1A) receptor antagonists. The structural features required for optimal binding to the 5-HT1A receptor are as follows: S-2-propanol linker, 4-indoloxy substituent, and a large lipophilic cyclic amine substituent.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Pindolol	5-hydroxytryptamine receptor 1A	Ki (nM)	22.4	N/A	N/A	Details
Pindolol	5-hydroxytryptamine receptor 1A	Ki (nM)	81.1	N/A	N/A	Details
Pindolol	Beta-1 adrenergic receptor	Ki (nM)	0.52	N/A	N/A	Details