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Active ingredient: Aprepitant - Chemisty and Biological Activity

Chemisty and Biological Activity

Chemical Formula

C23H21F7N4O3

Chemical Name

5-[[2-[1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)- morpholin-4-yl]methyl]-1,2-dihydro-1,2,4-triazol-3-one

Chemical Structure

Molecular Weight

534.427 g/mol

Physical State

Solid

Melting Point

Not Available

Water Solubility

Practically insoluble

Isoelectric Point

Not Available

Organisms Affected

Humans and other mammals

Phase 1 Metabolising Enzyme (1-st Step of Metabolism)

CYP3A4

Primary Drug Target
NameP/neurokinin 1 Receptor
Gene NameTACR1
SynonymsSubstance-P receptor; SPR; NK-1 receptor; NK-1R; Tachykinin receptor 1
Specific FunctionThis is a receptor for the tachykinin neuropeptide substance P. It is probably associated with G proteins that activate a phosphatidylinositol-calcium second messenger system. The rank order of affinity of this receptor to tachykinins is: substance P > substance K > neuromedin K.

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