The noncationizable tripeptide Ac-D-Trp-Phe-GlyNH(2) was recently proposed as a novel minimal recognition motif for mu-opioid receptor. The introduction of different substituents (methyl, halogens, nitro, etc.) at the indole of D-Trp significantly influenced receptor affinities and resulted in serum stability and in a measurable effect on central antinociception in mice after ip administration.
De Marco R, Bedini A, Spampinato S, Gentilucci L (2014). Synthesis of tripeptides containing D-Trp substituted at indole ring, and assessment of MOR affinity and in vivo central antinociception. JOURNAL OF MEDICINAL CHEMISTRY, 57, 6861-6866 [10.1021/jm5002925].
Synthesis of tripeptides containing D-Trp substituted at indole ring, and assessment of MOR affinity and in vivo central antinociception.
DE MARCO, ROSSELLA;BEDINI, ANDREA;SPAMPINATO, SANTI MARIO;GENTILUCCI, LUCA
2014
Abstract
The noncationizable tripeptide Ac-D-Trp-Phe-GlyNH(2) was recently proposed as a novel minimal recognition motif for mu-opioid receptor. The introduction of different substituents (methyl, halogens, nitro, etc.) at the indole of D-Trp significantly influenced receptor affinities and resulted in serum stability and in a measurable effect on central antinociception in mice after ip administration.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
