Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UNIPROT:P46098 (5-HT3 receptor)
 2,290 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Serotonergic abnormalities have been identified in the brain of suicide victims independent of psychiatric diagnosis. We report the first study of serotonin 5-HT3 receptors in the brain of suicide victims. There were no differences in the number (Bmax) or affinity (KD) of 5-HT3 receptors in the temporal cortex of suicide victims compared to matched controls. There was a negative correlation between brain serotonin levels and receptor number (r = -0.5, p = 0.04) in both groups. This study indicates that alterations in serotonergic function in the brain of suicide victims do not appear to directly involve the 5-HT3 receptor.
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PMID:Serotonin 5-HT3 receptor binding kinetics in the cortex of suicide victims are normal. 902 70

Ligand-gated ion channels (LGICs) are considered as attractive protein targets in the search for new therapeutic agents. Nowadays, this strategy involves the capability to screen large chemical libraries. We present a new Tag-lite ligand binding assay targeting LGICs on living cells. This technology combines the use of suicide enzyme tags fused to channels of interest with homogeneous time-resolved fluorescence (HTRF) as the detection readout. Using the 5-HT3 receptor as system model, we showed that the pharmacology of the HALO-5HT3 receptor was identical to that of the native receptor. After validation of the assay by using 5-HT3 agonists and antagonists of reference, a pilot screen enabled us to identify azelastine, a well-known histamine H1 antagonist, as a potent 5-HT3 antagonist. This interesting result was confirmed with electrophysiological experiments. The method described here is easy to implement and could be applicable for other LGICs, opening new ways for the screening of chemical libraries.
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PMID:Design and validation of a homogeneous time-resolved fluorescence cell-based assay targeting the ligand-gated ion channel 5-HT3A. 2599 4