Conformationally constrained tachykinins: N-methylated analogues of neurokinin A
โ Scribed by P. Rovero; V. Pestellini; R. Patacchini; P. Santicioli; C. A. Maggi; A. Meli
- Book ID
- 101719667
- Publisher
- Wiley (John Wiley & Sons)
- Year
- 1989
- Tongue
- English
- Weight
- 193 KB
- Volume
- 28
- Category
- Article
- ISSN
- 0006-3525
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โฆ Synopsis
Limited conformational constraints have been introduced in the sequence of the C-terminal fragment of the peptide neurotransmitter neurokinin A by N-methylation of individual peptide bonds, and the biological activities of the peptides thus obtained were evaluated in order to assess the effect of such conformational constraint on receptor selectivity. The analogue methylated in position 7 shows enhanced selectivity toward NK-1 receptor.
๐ SIMILAR VOLUMES
Conformationally Constrained NO Synthase Inhibitors: Rigid Analogues of L-N-Iminoethylornithine. -Three series of type (VI), (XI), and (XII) are prepared with the aim to create novel nitric oxide synthase inhibitors. Derivatives of type (VI) show desired activity. The most potent derivatives are fo