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More specifically, it may interact with N-methyl-D-aspartate (NMDA) receptors, gamma-aminobutyric acid (GABA) receptors, and alpha 1-adrenergic receptors in the central nervous system [1, 2]

Compound 22 , a hybrid with the N-terminal from 21 and the C-terminal from 16 demonstrated a further enhanced potency (Ki = 23 nM) and a high selectivity for IRAP over AP-N ( 16 , devoid of a macrocyclic ring system in the N-terminal is not selective and inhibits both IRAP and AP-N activity, suggesting that introduction of proper conformational constrains in the N-terminal by macrocyclization improves selectivity ( 15 and Ang IV seem to adopt a -turn at the C-terminal when binding to IRAP, while in the case of 21 , a less well-defined turn conformation is adopted at the N-terminal

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Inflammation res: Off J Eur Histamine Res Soc

& Finglas, P