A nonpeptide NK1 receptor antagonist (Ki = 0.25 nM in a radioligand binding assay); selective for NK1 over NK2 and NK3 receptors (Kis = >10 μM for both); inhibits excitation of guinea pig locus coeruleus cells induced by substance P in vitro (IC50 = 25 nM); inhibits increases in horizontal locomotor activity induced by [Sar9

CP 99,994 (hydrochloride) – 1 mg

Brand:
Cayman
CAS:
145148-39-6
Storage:
-20
UN-No:
De Minimis - 3077 / 9

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 μM for both) as well as dopamine D1 and D2, α1-, α2- and β-adrenergic, serotonin, histamine H1, muscarinic and nicotinic acetylcholine, μ-opioid, glutamate, benzodiazepine, and γ-aminobutyric acid (GABA) receptors (IC50s = >1 μM 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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SKU: 27669 - 1 mg Category:

Description

A nonpeptide NK1 receptor antagonist (Ki = 0.25 nM in a radioligand binding assay); selective for NK1 over NK2 and NK3 receptors (Kis = >10 μM for both); inhibits excitation of guinea pig locus coeruleus cells induced by substance P in vitro (IC50 = 25 nM); inhibits increases in horizontal locomotor activity induced by [Sar9,Met(O2)11]-substance P in guinea pigs (ID50 = 0.59 mg/kg); inhibits aerosolized capsaicin-induced plasma extravasation in guinea pig lung (ID50 = 4 mg/kg); exhibits anti-emetic effects in ferret models of emesis induced by copper sulfate, loperamide, or cisplatin at 0.3 and 1 mg/kg

Formal name: (2S,3S)-N-[(2-methoxyphenyl)methyl]-2-phenyl-3-piperidinamine, dihydrochloride

Synonyms: 

Molecular weight: 369.3

CAS: 145148-39-6

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Immunology & Inflammation|Pulmonary Diseases||Research Area|Neuroscience

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