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The tissue distribution and functional characterization of human VR1.
Biochem Biophys Res Commun. 2001 Mar; 281(5):1183-9.BB

Abstract

The irritant action of capsaicin is mediated by the vanilloid receptor, VR1, which is expressed in sensory neurons termed nociceptors. Capsaicin also desensitizes nociceptors and, thus, is useful clinically as an analgesic. Given the potential importance of VR1 in pain, we have cloned the human capsaicin receptor, hVR1, from a human dorsal root ganglia (DRG) cDNA library. Human VR1 protein is 85% identical to the rat VR1 and many of the amino acid differences are concentrated at the amino and carboxyl termini. VR1 is expressed in DRG as an approximately 4.2 kilobase RNA, and is also expressed in the central nervous system and in the kidney. Capsaicin (EC(50) = 853 nM), low pH (<5.5), and noxious heat (44 degrees C) activate hVR1 expressed in Xenopus oocytes. Subthreshold pH (6.4) sensitizes VR1 to capsaicin (EC(50) = 221 nM). This study demonstrates the similarity of human and rat VR1 in integrating multiple noxious stimuli.

Authors+Show Affiliations

Department of Biochemistry, Neurogen Corporation, 35 N.E. Industrial Road, Branford, Connecticut, 06405, USA. dcortright@nrgn.comNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

11243859

Citation

Cortright, D N., et al. "The Tissue Distribution and Functional Characterization of Human VR1." Biochemical and Biophysical Research Communications, vol. 281, no. 5, 2001, pp. 1183-9.
Cortright DN, Crandall M, Sanchez JF, et al. The tissue distribution and functional characterization of human VR1. Biochem Biophys Res Commun. 2001;281(5):1183-9.
Cortright, D. N., Crandall, M., Sanchez, J. F., Zou, T., Krause, J. E., & White, G. (2001). The tissue distribution and functional characterization of human VR1. Biochemical and Biophysical Research Communications, 281(5), 1183-9.
Cortright DN, et al. The Tissue Distribution and Functional Characterization of Human VR1. Biochem Biophys Res Commun. 2001;281(5):1183-9. PubMed PMID: 11243859.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - The tissue distribution and functional characterization of human VR1. AU - Cortright,D N, AU - Crandall,M, AU - Sanchez,J F, AU - Zou,T, AU - Krause,J E, AU - White,G, PY - 2001/3/13/pubmed PY - 2001/5/1/medline PY - 2001/3/13/entrez SP - 1183 EP - 9 JF - Biochemical and biophysical research communications JO - Biochem. Biophys. Res. Commun. VL - 281 IS - 5 N2 - The irritant action of capsaicin is mediated by the vanilloid receptor, VR1, which is expressed in sensory neurons termed nociceptors. Capsaicin also desensitizes nociceptors and, thus, is useful clinically as an analgesic. Given the potential importance of VR1 in pain, we have cloned the human capsaicin receptor, hVR1, from a human dorsal root ganglia (DRG) cDNA library. Human VR1 protein is 85% identical to the rat VR1 and many of the amino acid differences are concentrated at the amino and carboxyl termini. VR1 is expressed in DRG as an approximately 4.2 kilobase RNA, and is also expressed in the central nervous system and in the kidney. Capsaicin (EC(50) = 853 nM), low pH (<5.5), and noxious heat (44 degrees C) activate hVR1 expressed in Xenopus oocytes. Subthreshold pH (6.4) sensitizes VR1 to capsaicin (EC(50) = 221 nM). This study demonstrates the similarity of human and rat VR1 in integrating multiple noxious stimuli. SN - 0006-291X UR - https://www.unboundmedicine.com/medline/citation/11243859/The_tissue_distribution_and_functional_characterization_of_human_VR1_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0006-291X(01)94482-1 DB - PRIME DP - Unbound Medicine ER -