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.
| Cell Experiment | |
|---|---|
| Cell lines | CHO cells expressing the h5-HT1B or h5-HT1D receptors |
| Preparation method | [35S]GTPγS binding studies. [35S]GTPγS binding studies in CHO cells expressing the h5-HT1B or h5-HT1D receptors are performed. In brief, membranes from 1 × 106 cells are preincubated at 30°C for 30 minutes, in HEPES buffer (HEPES [20 mM], MgCl2 [3 mM], NaCl [100 mM], ascorbate [0.2 mM]), containing GDP (10 µ M), with or without BRL-15572. Starting the reaction by the addition of 10 µL of [35S]GTPγS (100 pM, assay concentration) followed by a further 30 minutes incubation at 30°C. Determing Non-specific binding by addition of unlabelled GTPγS (10 µM), prior to the addition of cells. Stoping the reaction by rapid filtration using Whatman GF/B grade filters followed by five washes with ice-cold HEPES buffer. Determining radioactivity by liquid scintillation spectrometry |
| Concentrations | 0 μM -10 μM |
| Incubation time | 30 minutes |
| Animal Experiment | |
|---|---|
| Animal models | Male Wistar rats with diabetes |
| Formulation | 20% propylene glycol |
| Dosages | 1 mg/kg, 2 mg/kg |
| Administration | Administered via i.v. |
| Molecular Weight | 479.87 |
| Formula | C25H27ClN2O.2HCl |
| CAS Number | 193611-72-2 |
| Solubility (25°C) | DMSO >100 mg/mL |
| Storage | 4°C, dry, sealed |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[3] C Roberts, et al. Ligands for the investigation of 5-HT autoreceptor function
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