108456-08-2Relevant articles and documents
Use of Molecular Modeling to Design Selective NTS2 Neurotensin Analogues
Fanelli, Roberto,Floquet, Nicolas,Besserer-Offroy, élie,Delort, Bartholomé,Vivancos, Mélanie,Longpré, Jean-Michel,Renault, Pedro,Martinez, Jean,Sarret, Philippe,Cavelier, Florine
, p. 3303 - 3313 (2017)
Neurotensin exerts potent analgesia by acting at both NTS1 and NTS2 receptors, whereas NTS1 activation also results in other physiological effects such as hypotension and hypothermia. Here, we used molecular modeling approach to design highly selective NT
Synthesis of new substance P analogues releasing histamine from rat peritoneal mast cells
Chen,Mousli,Thoret,Fischer,Landry,Michelot
, p. 931 - 937 (2007/10/02)
New analogues of the N-terminal fragment of substance P [Arg-Pro-Lys-Pro, SP(1-4)] were synthesized and their activities on histamine release from rat peritoneal mast cells were compared. The potency of these compounds decreases in the following order (in abbreviation): SP(1-4)C12 > C'12-SP(1-4)-OCH3 > C'12-SP(1-4)-OH, H-Lys-Pro-C12 and SP. Benzalkonium chloride, a competitive antagonist of peptide-induced histamine release from rat mast cells, inhibits the effect of SP and SP analogues with IC50 in the range of micromolar concentrations. SP(1-4)-C12 and C'12-SP(1-4)-OCH3 have been found to be 10-fold more active than SP on the GTPase activity of purified G proteins (G(o)/G(i)). The lack of clear structural relationships for agonist activities supports a receptor-less mechanism for histamine release by SP and its analogs. This effect could be elicited by a direct stimulation of G proteins.