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LPI 805

Target nature : NK2R tachykinin receptor
CAS n° : 634888-88-3
Mecanism of action : inhibits cAMP responses, potentiates calcium responses
Physico-chemical properties : allosteric effector of the tachykinin NK2 receptor
Probe availability : national chemical library
Princeps reference : Maillet E, N. Pellegrini, C Valant, B. Bucher, M. Hibert, J.J. Bourguignon and J.L. Galzi. (2007). A novel conformation-specific allosteric inhibitor of the tachykinin NK2 receptor with functionally selective properties FASEB J. vol 21, 2124-2134.
More bibliography : Palanche, T., Ilien, B., Zoffmann, S., Reck, M.P., Bucher, B., Edelstein, S., Galzi, J.L.(2001) Dual responses and desensitization of the NK2 tachykinin receptor are mediated by multiple conformational states as revealed by rapid kinetic measurements. J.Biol. Chem 276, 34853-34861 Europe patent n° 1 514 112 (6 september 2006) and French patent n° 2 840 993 (8 april 2005) : « new process to identify allosteric effectors», inventors: Galzi, J.L., Maillet, E., Hibert, M., Bourguignon, J.J.
Other available information on the probe : weakly soluble, never used in vivo
Other information on the target : The NK2R is a valuable model of Gq-coupled receptors. Very few applications in health due to significant differences in tissue distribution among species and variability of affinity for drugs
Selectivity profile : LPI 805 is active on NK1R. Other receptors were not tested
In vivo data : none
In vitro data : speeds up dissociation of bound agonist. The dissociation follows a two step process, with a rapid and a slow step. LPI 805 speeds up dissociation by increasing the amplitude of the rapid dissociation process ans correlatively reducing that of the slow dissociation step. The resulting functional consequence is that calcium responses and potentiated while cAMP responses are reduced up to full blockade. La résultante est fonctionnelle: les réponses calciques sont amplifiées (elles sont liée à l'occupation du site de faible affinité, voir palanché et al. 2001) tandis que les réponse de production de cAMP sont réduites
Toxicity : unknown
Chaine SMILES : N#CCN(Cc1ccccc1)Cc3ccc2ccccc2c3
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