The dipeptide neurokinin-1 receptor antagonist S19752 is a potent and long-acting inhibitor of bronchoconstriction when administered by aerosol to the guinea pig in vivo
✍ Scribed by Jean-Luc Fauchère; Nathalie Kucharczyk; Edgar Jacoby; Michel Lonchampt; Pascale Robineau; Catherine Dacquet; Domenico Regoli; Emmanuel Canet
- Book ID
- 104364747
- Publisher
- Elsevier Science
- Year
- 1997
- Tongue
- English
- Weight
- 268 KB
- Volume
- 7
- Category
- Article
- ISSN
- 0960-894X
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✦ Synopsis
The K+ salt of Tbi-Hyp-Trp -OTfb (S19572, Tbi = 1-[4-(2H-tetrazol-5-yl)butyl]-lH-indole-3-carbonyl; Tfb = 3,5-di-trifluoromethyl-benzyl) is a chemically modified, water-soluble derivative designed from prolyl-tryptophan using N-and Cterminal substitutions to confer on the analogs receptor selectivity and water solubility. The new NK-1 selective receptor antagonist is both highly potent in binding and bioassays in vitro, and long-acting when administered by aerosol to the guinea-pig in vivo. Molecular modeling of the antagonist in the seven transmembrane NK-1 receptor model offers a rationale for the observed water solubility and yet retained binding affinity.