NAS-181 free base is a potent and selective antagonist of the rat 5-HT1B receptor, exhibiting a Ki value of 47 nM. This compound demonstrates a 13-fold selectivity for the rat 5-HT1B over the bovine 5-HT1B receptor, which has a Ki of 630 nM. NAS-181 free base effectively enhances serotonin turnover and increases synaptic serotonin levels by inhibiting the terminal rat 5-HT1B autoreceptors, making it a valuable tool for research in neuropharmacology and serotonergic signaling.
NAS-181 free base is a potent and selective antagonist of the rat 5-HT1B receptor, exhibiting a Ki value of 47 nM. This compound demonstrates a 13-fold selectivity for the rat 5-HT1B over the bovine 5-HT1B receptor, which has a Ki of 630 nM. NAS-181 free base effectively enhances serotonin turnover and increases synaptic serotonin levels by inhibiting the terminal rat 5-HT1B autoreceptors, making it a valuable tool for research in neuropharmacology and serotonergic signaling.
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