A highly selective NK-2 tachykinin receptor antagonist containing D-tryptophan

  • Eur J Pharmacol. 1990 Jan 3;175(1):113-5. doi: 10.1016/0014-2999(90)90161-x.
P Rovero  1 ,  V Pestellini ,  C A Maggi ,  R Patacchini ,  D Regoli ,  A Giachetti
Affiliations
  • 1. Peptide Synthesis Laboratory, Chemistry Department, A. Menarini Pharmaceuticals, Firenze, Italy.
PMID: 2157594 DOI: 10.1016/0014-2999(90)90161-x
Abstract

The classical approach used in the development of substance P (SP) antagonists, i.e. the introduction of multiple D-tryptophan (D-Trp), was successfully extended to neurokinin A (NKA). Thus, a new NK-2-selective tachykinin receptor antagonist, namely [Tyr5, D-Trp6,8,9, Arg10]NKA-(4-10), was developed that had pA2 values of 5.2, 7.9 and 4.9 in three monoreceptor in vitro assays for NK-1, NK-2 and NK-3 tachykinin receptors, respectively.

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