BRL-15572

BRL-15572 is a hydrochloride salt form of BRL-15572 which is a selective  serotonin receptor subtype 5-HT1D antagonist with an IC50 of 260 μM.  BRL-15572 indicates 60-fold selectivity over h5-HT1B, and displays little or no affinity for a range of other receptor types. In the presence of the 5-HT1D antagonist BRL15572 at a dose of 10 μM triggered a significant reduction in evoked IPSC (inhibitory postsynaptic currents) amplitude. Additionally, the antianti-migraine agent sumatriptan (1 μM) produced a striking reduction in evoked IPSC amplitude in the presence of BRL15572 (10 μM) which was not significantly different to that produced in its absence. For a comparison, sumatriptan (1 μM) did not produce a marked reduction in evoked IPSC amplitude in the presence of both NAS181 (10 μM) and BRL15572 (10 μM). In addition, it was observed that the prevention of GABAergic synaptic transmission produced by 5-HT was abolished by the 5-HT1B antagonist NAS181, but not by the 5-HT1A and 5-HT1D antagonists WAY100135 and BRL15572, while that produced by sumatriptan was only abolished in the combined presence of NAS181 and BRL15572.