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[3H]A-778317 [1-((R)-5-tert-butyl-indan-1-yl)-3-isoquinolin-5-yl-urea]: a novel, stereoselective, high-affinity antagonist is a useful radioligand for the human transient receptor potential vanilloid-1 (TRPV1) receptor.
Bianchi BR, El Kouhen R, Neelands TR, Lee CH, Gomtsyan A, Raja SN, Vaidyanathan SN, Surber B, McDonald HA, Surowy CS, Faltynek CR, Moreland RB, Jarvis MF, Puttfarcken PS. Bianchi BR, et al. J Pharmacol Exp Ther. 2007 Oct;323(1):285-93. doi: 10.1124/jpet.107.124305. Epub 2007 Jul 27. J Pharmacol Exp Ther. 2007. PMID: 17660385
1-((R)-5-tert-butyl-indan-1-yl)-3-isoquinolin-5-yl-urea (A-778317) is a novel, stereoselective, competitive antagonist that potently blocks transient receptor potential vanilloid-1 (TRPV1) receptor-mediated changes in intracellular calcium conce …
1-((R)-5-tert-butyl-indan-1-yl)-3-isoquinolin-5-yl-urea (A-778317) is a novel, stereoselective, competitive anta …
Conformational analysis and structural comparisons of (1R,3S)-(+)- and (1S,3R)-(-)-tefludazine, (S)-(+)- and (R)-(-)-octoclothepin, and (+)-dexclamol in relation to dopamine receptor antagonism and amine-uptake inhibition.
Liljefors T, Bøgesø KP. Liljefors T, et al. J Med Chem. 1988 Feb;31(2):306-12. doi: 10.1021/jm00397a006. J Med Chem. 1988. PMID: 2892932
Conformational analysis with molecular mechanics (MM2(85] and molecular superimposition studies of (1R,3S)-(+)- and (1S,3R)-(-)-4-[3-(4-fluorophenyl)-6-(trifluoromethyl)indan-1-yl]-1- piperazineethanol (tefludazine) and (S)-(+)- and (R)-(-)-octo …
Conformational analysis with molecular mechanics (MM2(85] and molecular superimposition studies of (1R,3S)-(+)- and (1S,3R)-(-)-4-[3- …
Binding of [(3)H]A-778317 to native transient receptor potential vanilloid-1 (TRPV1) channels in rat dorsal root ganglia and spinal cord.
Bianchi BR, El Kouhen R, Chen J, Puttfarcken PS. Bianchi BR, et al. Eur J Pharmacol. 2010 May 10;633(1-3):15-23. doi: 10.1016/j.ejphar.2010.02.004. Epub 2010 Feb 11. Eur J Pharmacol. 2010. PMID: 20153316
A-778317 (1-((R)-5-tert-butyl-indan-1-yl)-3-isoquinolin-5-yl-urea) is a potent antagonist of human and rat transient receptor potential vanilloid-1 (TRPV1) receptors. ...
A-778317 (1-((R)-5-tert-butyl-indan-1-yl)-3-isoquinolin-5-yl-urea) is a potent antagonist of human and rat trans …