Citation
Bianchi, Bruce R., et al. "[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." The Journal of Pharmacology and Experimental Therapeutics, vol. 323, no. 1, 2007, pp. 285-93.
Bianchi BR, El Kouhen R, Neelands TR, et al. [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. J Pharmacol Exp Ther. 2007;323(1):285-93.
Bianchi, B. R., El Kouhen, R., Neelands, T. R., Lee, C. H., Gomtsyan, A., Raja, S. N., Vaidyanathan, S. N., Surber, B., McDonald, H. A., Surowy, C. S., Faltynek, C. R., Moreland, R. B., Jarvis, M. F., & Puttfarcken, P. S. (2007). [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. The Journal of Pharmacology and Experimental Therapeutics, 323(1), 285-93.
Bianchi BR, et al. [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. J Pharmacol Exp Ther. 2007;323(1):285-93. PubMed PMID: 17660385.
TY - JOUR
T1 - [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.
AU - Bianchi,Bruce R,
AU - El Kouhen,Rachid,
AU - Neelands,Torben R,
AU - Lee,Chih-Hung,
AU - Gomtsyan,Arthur,
AU - Raja,Shirish N,
AU - Vaidyanathan,Sriajan N,
AU - Surber,Bruce,
AU - McDonald,Heath A,
AU - Surowy,Carol S,
AU - Faltynek,Connie R,
AU - Moreland,Robert B,
AU - Jarvis,Michael F,
AU - Puttfarcken,Pamela S,
Y1 - 2007/07/27/
PY - 2007/7/31/pubmed
PY - 2007/11/6/medline
PY - 2007/7/31/entrez
SP - 285
EP - 93
JF - The Journal of pharmacology and experimental therapeutics
JO - J Pharmacol Exp Ther
VL - 323
IS - 1
N2 - 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 concentrations (pIC50 = 8.31 +/- 0.13). The (S)-stereoisomer, 1-((S)-5-tert-butyl-indan-1-yl)-3-isoquinolin-5-yl-urea (A-778316), is 6.8-fold less potent (pIC50 = 7.47 +/- 0.07). A-778317 also potently blocks capsaicin and acid activation of native rat TRPV1 receptors in dorsal root ganglion neurons. A-778317 was tritiated ([3H]A-778317; 29.3 Ci/mmol) and used to study recombinant human TRPV1 (hTRPV1) receptors expressed in Chinese ovary cells (CHO) cells. [3H]A-778317 labeled a single class of binding sites in hTRPV1-expressing CHO cell membranes with high affinity (KD = 3.4 nM; Bmax = 4.0 pmol/mg protein). Specific binding of 2 nM [3H]A-778317 to hTRPV1-expressing CHO cell membranes was reversible. The rank-order potency of TRPV1 receptor antagonists to inhibit binding of 2 nM [3H]A-778317 correlated well with their functional potencies in blocking TRPV1 receptor activation. The present data demonstrate that A-778317 blocks polymodal activation of the TRPV1 receptor by binding to a single high-affinity binding site and that [3H]A-778317 possesses favorable binding properties to facilitate further studies of hTRPV1 receptor pharmacology.
SN - 0022-3565
UR - https://www.unboundmedicine.com/medline/citation/17660385/
L2 - https://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=17660385
DB - PRIME
DP - Unbound Medicine
ER -
