An NK1 receptor antagonist (Ki = 0.95 nM); selective for human NK1 over human NK2 and NK3 and rat NK1 (Kis = >1

Netupitant – 25 mg

Brand:
Cayman
CAS:
290297-26-6
Storage:
-20
UN-No:
Non-Hazardous - /

Netupitant is an insurmountable antagonist of the neurokinin-1 (NK1) receptor (Ki = 0.95 nM in CHO cells expressing the human recombinant receptor).{37265} It is selective for human NK1 over human NK2 and NK3 and rat NK1 (Kis = >1,500 nM) and over 50 G protein-coupled receptors, monoamine transporters, and ion channels when used in the nanomolar range.{37266} Netupitant decreases the maximal response to substance P-induced contractions in isolated guinea pig ileum with long-lasting effects. It also dose-dependently inhibits the substance P-induced scratching, biting, and licking response in mice when used at doses ranging from 1-10 mg/kg and decreases NK agonist-induced foot tapping in gerbils (ID50s = 1.5 mg/kg, i.p., or 0.5 mg/kg, oral). Formulations containing netupitant have been used in the treatment of chemotherapy-induced nausea and vomiting.  

 

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Description

An NK1 receptor antagonist (Ki = 0.95 nM); selective for human NK1 over human NK2 and NK3 and rat NK1 (Kis = >1,500 nM); selective for NK1 over 50 G protein-coupled receptors, monoamine transporters, and ion channels when used in the nanomolar range; decreases the maximal response to substance P in isolated guinea pig ileum; inhibits substance P-induced scratching, biting, and licking in mice at doses of 1-10 mg/kg; decreases NK agonist-induced foot tapping in gerbils (ID50s = 1.5 mg/kg, i.p., or 0.5 mg/kg, oral).

Formal name: N,α,α-trimethyl-N-[4-(2-methylphenyl)-6-(4-methyl-1-piperazinyl)-3-pyridinyl]-3,5-bis(trifluoromethyl)-benzeneacetamide

Synonyms:  Ro 67-31898/000

Molecular weight: 578.6

CAS: 290297-26-6

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Neuroscience|Pain Research

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