![[Feedback]](/icons/banner/feedbackACT.gif){kind=icon}
![[For Subscribers]](/icons/banner/subscriberACT.gif){kind=icon}
![[Archive]](/icons/banner/archiveACT.gif){kind=icon}
![[Search]](/icons/banner/searchACT.gif){kind=icon}
![[Contents]](/icons/banner/tocACT.gif){kind=icon}
|
|
|
|
|
||
A Szallasi, NE Lewin and PM Blumberg
Molecular Mechanisms of Tumor Promotion Section, National Cancer Institute, Bethesda, Maryland.
We have used the vanilloid (capsaicin) receptor assay to search for modulators of binding activity. We report here that both capsaicin and its ultrapotent analog, resiniferatoxin (RTX), bind to the plasma protein alpha-1-acid glycoprotein (AGP) with high affinity (10.5 and 0.3 microM, respectively). AGP seems to be the dominant vanilloid (capsaicin/RTX) binding protein in serum. [3H] RTX binding to AGP is inhibited by chlorpromazine and by Trisbutoxyethylphosphate, indicating that vanilloids compete for a well-characterized drug binding domain on the AGP molecule. The 35-fold difference in the affinity of AGP for RTX and capsaicin may result in differences in the pharmacodynamics and pharmacokinetics of these two compounds; the contribution of AGP binding to the unique spectra of action of RTX or to the marked species differences in vanilloid actions, however, remains to be determined. An important practical application of AGP is its inclusion in the [3H]RTX binding assay utilizing sensory ganglion membranes to reduce nonspecific binding by up to 5-fold.
This article has been cited by other articles:
|
|
 |
|
  B. R. Bianchi, R. El Kouhen, T. R. Neelands, C.-H. Lee, A. Gomtsyan, S. N. Raja, S. N. Vaidyanathan, B. Surber, H. A. McDonald, C. S. Surowy, 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., October 1, 2007; 323(1): 285 - 293. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 J. Lazar, D. C. Braun, A. Toth, Y. Wang, L. V. Pearce, V. A. Pavlyukovets, P. M. Blumberg, S. H. Garfield, S. Wincovitch, H.-K. Choi, et al. Kinetics of Penetration Influence the Apparent Potency of Vanilloids on TRPV1 Mol. Pharmacol., April 1, 2006; 69(4): 1166 - 1173. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 J. Jung, J. S. Shin, S.-Y. Lee, S. W. Hwang, J. Koo, H. Cho, and U. Oh Phosphorylation of Vanilloid Receptor 1 by Ca2+/Calmodulin-dependent Kinase II Regulates Its Vanilloid Binding J. Biol. Chem., February 20, 2004; 279(8): 7048 - 7054. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
J. Jung, S.-Y. Lee, S. W. Hwang, H. Cho, J. Shin, Y.-S. Kang, S. Kim, and U. Oh Agonist Recognition Sites in the Cytosolic Tails of Vanilloid Receptor 1 J. Biol. Chem., November 8, 2002; 277(46): 44448 - 44454. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
Y. Wang, T. Szabo, J. D. Welter, A. Toth, R. Tran, J. Lee, S. U. Kang, Y.-G. Suh, P. M. Blumberg, and J. Lee High Affinity Antagonists of the Vanilloid Receptor Mol. Pharmacol., October 1, 2002; 62(4): 947 - 956. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 E. V. Kuzhikandathil, H. Wang, T. Szabo, N. Morozova, P. M. Blumberg, and G. S. Oxford Functional Analysis of Capsaicin Receptor (Vanilloid Receptor Subtype 1) Multimerization and Agonist Responsiveness Using a Dominant Negative Mutation J. Neurosci., November 15, 2001; 21(22): 8697 - 8706. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
A. Szallasi, P. M. Blumberg, L. L. Annicelli, J. E. Krause, and D. N. Cortright The Cloned Rat Vanilloid Receptor VR1 Mediates Both R-Type Binding and C-Type Calcium Response in Dorsal Root Ganglion Neurons Mol. Pharmacol., September 1, 1999; 56(3): 581 - 587. [Abstract] [Full Text]
|
|
|
|
 |
|
 A. Szallasi and P. M. Blumberg Vanilloid (Capsaicin) Receptors and Mechanisms Pharmacol. Rev., June 1, 1999; 51(2): 159 - 212. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 T. Biro, M. Maurer, S. Modarres, N. E. Lewin, C. Brodie, G. Acs, P. Acs, R. Paus, and P. M. Blumberg Characterization of Functional Vanilloid Receptors Expressed by Mast Cells Blood, February 15, 1998; 91(4): 1332 - 1340. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
G. Acs, T. Biro, P. Acs, S. Modarres, and P. M. Blumberg Differential Activation and Desensitization of Sensory Neurons by Resiniferatoxin J. Neurosci., July 15, 1997; 17(14): 5622 - 5628. [Abstract] [Full Text] [PDF]
|
|
 |
 |
 |
|
 |
 |
 |
