158654-83-2Relevant articles and documents
COMPOUNDS FOR TREATING HUNTINGTON'S DISEASE
-
Page/Page column 186, (2020/12/01)
The present description relates to compounds, forms, and pharmaceutical compositions thereof and methods of using such compounds, forms, or compositions thereof for treating or ameliorating Huntington's disease. In particular, the present description relates to substituted monocyclic heteroaryl compounds of Formula (I), Formula (II), or Formula (III), forms and pharmaceutical compositions thereof and methods of using such compounds, forms, or compositions thereof for treating or ameliorating Huntington's disease.
Stability against enzymatic hydrolysis of endomorphin-1 analogues containing β-proline
Cardillo, Giuliana,Gentilucci, Luca,Tolomelli, Alessandra,Calienni, Maria,Qasem, Ahmed R.,Spampinato, Santi
, p. 1498 - 1502 (2007/10/03)
The enantiomer of endomorphin-1 (Tyr-Pro-Trp-PheNH2) and the analogues containing (S)-or (R)-β-proline have been synthesized, and their affinities towards μ-opioid receptors have been measured. As expected, the incubations of the different peptides with some commercially available enzymes showed that the presence of D-residues gave strong resistance towards digestion. The presence of β-proline alone is sufficient to confer good resistance against the hydrolysis of the biologically strategic Pro-Trp bond.
Synthesis and binding activity of endomorphin-1 analogues β-amino acids
Cardillo, Giuliana,Gentilucci, Luca,Melchiorre, Paolo,Spampinato, Santi
, p. 2755 - 2758 (2007/10/03)
Endomorphin-1 (Tyr-Pro-Trp-PheNH2) has been proposed as the most potent endogenous ligand of the μ-opioid receptors. In this paper, we describe the synthesis of some endomorphin-1 based tetrapeptides in which a residue of the sequence Tyr-Pro-Trp-PheNH2 is replaced by the corresponding β-isomer. These novel peptides showed different affinities for the opioid receptors labeled with [3H]-DAMGO in rat brain membranes, depending on the β-amino acid. In particular, the tetrapeptide containing β-Pro (Tyr-β-(R)-Pro-Trp-PheNH2) displayed a higher affinity than endogenous endomorphin-1, as revealed by their K(i) values (0.33 and 11.1 nM, respectively). (C) 2000 Elsevier Science Ltd.
Constrained β-alanine based GpIIb/IIIa antagonists
Klein, Scott I.,Czekaj, Mark,Molino, Bruce F.,Valeria, Chu
, p. 1773 - 1778 (2007/10/03)
The concepts of centrally constrained and peptide based fibrinogen receptor antagonists have been successfully combined into a single series of analogs which have been demonstrated to be potent inhibitors of platelet aggregation.