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Synthesis and characterization of an aryl-azidoparoxetine. A novel photo-affinity probe for serotonin-transporter.
- Source :
-
Biochemical pharmacology [Biochem Pharmacol] 1995 Oct 12; Vol. 50 (8), pp. 1211-5. - Publication Year :
- 1995
-
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.
- Subjects :
- Binding Sites
Blood Platelets metabolism
Humans
Kinetics
Paroxetine chemical synthesis
Paroxetine metabolism
Photochemistry
Serotonin metabolism
Serotonin Plasma Membrane Transport Proteins
Affinity Labels
Carrier Proteins analysis
Membrane Glycoproteins analysis
Membrane Transport Proteins
Nerve Tissue Proteins
Paroxetine analogs & derivatives
Selective Serotonin Reuptake Inhibitors chemical synthesis
Subjects
Details
- Language :
- English
- ISSN :
- 0006-2952
- Volume :
- 50
- Issue :
- 8
- Database :
- MEDLINE
- Journal :
- Biochemical pharmacology
- Publication Type :
- Academic Journal
- Accession number :
- 7488236
- Full Text :
- https://doi.org/10.1016/0006-2952(95)00260-7