Pharmacological characterization of tachykinin tetrabranched derivatives.

ABSTRACT:

Background and purpose

Peptide welding technology (PWT) is a novel chemical strategy that allows the synthesis of multibranched peptides with high yield, purity and reproducibility. Using this technique, we have synthesized and pharmacologically characterized the tetrabranched derivatives of the tachykinins, substance P (SP), neurokinin A (NKA) and B (NKB).

Experimental approach

The following in vitro assays were used: calcium mobilization in cells expressing human recombinant NK receptors, BRET studies of G-protein - NK1 receptor interaction, guinea pig ileum and rat urinary bladder bioassays. Nociceptive behavioural response experiments were performed in mice following intrathecal injection of PWT2-SP.

Key results

In calcium mobilization studies, PWT tachykinin deri

SUBMITTER: Ruzza C 

PROVIDER: S-EPMC4243984 | biostudies-literature | 2014 Sep

REPOSITORIES: biostudies-literature