All AbMole products are for research use only, cannot be used for human consumption.
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 |
[3] C Roberts, et al. Ligands for the investigation of 5-HT autoreceptor function
| Related 5-HT Receptor Products |
|---|
| AS19
AS19 is a potent, selective 5-HT7 receptor agonist with an IC50 value of 0.83 nM and a Ki of 0.6 nM. |
| CP94253
CP94253 is a selective, orally active agonist for serotonin receptor 1B (5-HT1B), through competitive binding with iodocyanopindolol (ICP) to the 5-HT1 receptor. |
| RS 39604
RS 39604 is a potent, selective, and orally active 5-HT4 receptor antagonist with a pKi of 9.1 in guinea pig striatal membranes. |
| GR127935
GR127935 is a selective 5-HT1D receptor antagonist. |
| SB-699551
SB-699551 is a potent and selective 5-HT5A antagonist with a pKi of 8.3. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2024 AbMole BioScience. All Rights Reserved.
