CP 99,994 (hydro<wbr/>chloride)

CP 99,994 (hydrochloride)

CAT N°: 27669
Price:

48.00 40.80

CP 99,994 is a nonpeptide neurokinin-1 (NK1) receptor antagonist (Ki = 0.25 nM in a radioligand binding assay).{46649} It is selective for NK1 over NK2 and NK3 receptors (Kis = >10 ?M for both) as well as dopamine D1 and D2, ?1-, ?2- and ?-adrenergic, serotonin, histamine H1, muscarinic and nicotinic acetylcholine, ?-opioid, glutamate, benzodiazepine, and ?-aminobutyric acid (GABA) receptors (IC50s = >1 ?M for all). In vitro, CP 99,994 inhibits excitation of guinea pig locus coeruleus cells induced by substance P (Item No. 24035; IC50 = 25 nM). It inhibits increases in horizontal locomotor activity induced by the NK1 agonist [Sar9,Met(O2)11]-substance P in guinea pigs (ID50 = 0.59 mg/kg). CP 99,994 inhibits aerosolized capsaicin-induced plasma extravasation in guinea pig lung (ID50 = 4 mg/kg). It exhibits anti-emetic effects in ferret models of emesis induced by copper sulfate, loperamide, or cisplatin (Item No. 13119) when administered at doses of 0.3 and 1 mg/kg.{46650}

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