Biological description5-HT1B / 1D antagonist (pKi = 8.5), often used in tritiated form as a radiolabelled probe. Shows approx. 100-fold selectivity over other 5-HT receptors and shows CNS and oral activity.
Storage instructionsStore at +4°C. Store under desiccating conditions. The product can be stored for up to 12 months.
Solubility overviewSoluble in ethanol to 25 mM
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
Millan MJ et al. Specific labelling of serotonin 5-HT(1B) receptors in rat frontal cortex with the novel, phenylpiperazine derivative, [3H]GR125,743. A pharmacological characterization. Pharmacol Biochem Behav71:589-98 (2002).
Read more (PubMed: 11888550) »
Audinot V et al. Binding profile of the novel 5-HT1B/1D receptor antagonist, [3H]GR 125,743, in guinea-pig brain: a comparison with [3H]5-carboxamidotryptamine. Eur J Pharmacol327:247-56 (1997).
Read more (PubMed: 9200567) »
Doménech T et al. Characterization of human serotonin 1D and 1B receptors using [3H]-GR-125743, a novel radiolabelled serotonin 5HT1D/1B receptor antagonist. Naunyn Schmiedebergs Arch Pharmacol356:328-34 (1997).
Read more (PubMed: 9303569) »