Biological descriptionPotent and selective 5-HT1B/1D receptor antagonist (pKi = 8.5 for both 5-HT1D in rat and 5-HT1D in guinea pig). 100-fold selectivity over 5-HT1A, 5-HT1E, and 5-HT2C. Displays centrally mediated effects upon systemic administration.
Chemical nameN-[4-Methoxy-3-(4-methyl-1-piperazinyl)phenyl]-2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)-1,1'-biphenyl-4-carboxamide hydrochloride
Storage instructionsStore at +4°C. Store under desiccating conditions. The product can be stored for up to 12 months.
Solubility overviewSoluble in water 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.
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Yu XJ et al. The 5-HT1D receptor antagonist GR-127,935 prevents inhibitory effects of sumatriptan but not CP-122,288 and 5-CT on neurogenic plasma extravasation within guinea pig dura mater. Neuropharmacology36:83-91 (1997).
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Lucas JJ et al. 5-Hydroxytryptamine1B receptors modulate the effect of cocaine on c-fos expression: converging evidence using 5-hydroxytryptamine1B knockout mice and the 5-hydroxytryptamine1B/1D antagonist GR127935. Mol Pharmacol51:755-63 (1997).
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Hidiroglou M et al. Effects of level of dietary sulfur on the growth performance and blood mineral profile of sheep fed urea-supplemented corn silage. Int J Vitam Nutr Res47:284-91 (1977).
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