Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)

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Chemical Compound Review:

GR-64349 (3S)-3-[[(1S)-1-[[(1S)-1- [[(1S)-1-[[(3R)-1...

Synonyms: AC1MI0IH, GR 64349, 136218-59-2, 136548-07-7, 137593-52-3

Ciccocioppo, R. et al., Renzetti, A.R. et al., Julia, V. et al.

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High impact information on GR 64349

Chinese hamster ovary cells stably transfected with the wild-type or Tyr289Phe mutant NK2 receptor both bound neurokinin A (NKA) and the synthetic NK2 receptor-selective agonists, GR 64349 and [betaAla8]NKA(4-10), with high and even affinities [1].
The NK1 selective agonist [Sar9,Met(O2)11]substance P and the NK2 selective agonist GR 64349 did not At doses that inhibited alcohol intake, the NK3 agonists did not modify water intake; total fluid intake was significantly reduced only following 500 ng/rat of [Asp5.6,MePhe8]substance P(5-11) [2].
GR-73632 reduced gastric emptying, and GR-64349 increased abdominal response [3].

References

Defects of tyrosine289phenylalanine mutation on binding and functional properties of the human tachykinin NK2 receptor stably expressed in chinese hamster ovary cells. Renzetti, A.R., Catalioto, R.M., Carloni, C., Criscuoli, M., Cucchi, P., Giolitti, A., Zappitelli, S., Rotondaro, L., Maggi, C.A. Biochem. Pharmacol. (1999) [Pubmed]
Selective agonists at NK3 tachykinin receptors inhibit alcohol intake in Sardinian alcohol-preferring rats. Ciccocioppo, R., Panocka, I., Pompei, P., De Caro, G., Massi, M. Brain Res. Bull. (1994) [Pubmed]
Tachykininergic mediation of viscerosensitive responses to acute inflammation in rats: role of CGRP. Julia, V., Buéno, L. Am. J. Physiol. (1997) [Pubmed]

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