| Literature DB >> 7488236 |
J Chudzik1, D McCarthy, D Bakish, A Ravindran, P D Hrdina.
Abstract
Paroxetine is an effective antidepressant drug and potent serotonin (5-HT) uptake inhibitor. It selectively labels 5-HT transporter on platelets and neurons. We report here the synthesis of an aryl-azido derivative of paroxetine, which is a novel photoactive and irreversible ligand for the [3H]paroxetine binding site on the platelet 5-HT transporter. The compound inhibited [3H]paroxetine binding (IC50, 55 nM) and 5-HT uptake (IC50, 12 nM) at equilibrium conditions and inactivated 10-20% of [3H]paroxetine binding sites upon irradiation at 320 nm. SDS-PAGE of platelet protein extract labelled with the radioactive analogue of the synthesized probe revealed the presence of four radioactive bands of which the 71-kDa one was the most prominent.Entities:
Mesh：
Substances：
Year: 1995 PMID： 7488236 DOI： 10.1016/0006-2952(95)00260-7
Source DB: PubMed Journal: Biochem Pharmacol ISSN： 0006-2952 Impact factor: 5.858