Unknown

Dataset Information

0

The endogenous lipid anandamide is a full agonist at the human vanilloid receptor (hVR1).


ABSTRACT: The endogenous cannabinoid anandamide was identified as an agonist for the recombinant human VR1 (hVR1) by screening a large array of bioactive substances using a FLIPR-based calcium assay. Further electrophysiological studies showed that anandamide (10 or 100 microM) and capsaicin (1 microM) produced similar inward currents in hVR1 transfected, but not in parental, HEK293 cells. These currents were abolished by capsazepine (1 microM). In the FLIPR anandamide and capsaicin were full agonists at hVR1, with pEC(50) values of 5. 94+/-0.06 (n=5) and 7.13+/-0.11 (n=8) respectively. The response to anandamide was inhibited by capsazepine (pK(B) of 7.40+/-0.02, n=6), but not by the cannabinoid receptor antagonists AM630 or AM281. Furthermore, pretreatment with capsaicin desensitized the anandamide-induced calcium response and vice versa. In conclusion, this study has demonstrated for the first time that anandamide acts as a full agonist at the human VR1.

SUBMITTER: Smart D 

PROVIDER: S-EPMC1571834 | biostudies-literature | 2000 Jan

REPOSITORIES: biostudies-literature

altmetric image

Publications

The endogenous lipid anandamide is a full agonist at the human vanilloid receptor (hVR1).

Smart D D   Gunthorpe M J MJ   Jerman J C JC   Nasir S S   Gray J J   Muir A I AI   Chambers J K JK   Randall A D AD   Davis J B JB  

British journal of pharmacology 20000101 2


The endogenous cannabinoid anandamide was identified as an agonist for the recombinant human VR1 (hVR1) by screening a large array of bioactive substances using a FLIPR-based calcium assay. Further electrophysiological studies showed that anandamide (10 or 100 microM) and capsaicin (1 microM) produced similar inward currents in hVR1 transfected, but not in parental, HEK293 cells. These currents were abolished by capsazepine (1 microM). In the FLIPR anandamide and capsaicin were full agonists at  ...[more]

Similar Datasets

| S-EPMC7589233 | biostudies-literature
| S-EPMC1573364 | biostudies-other
| S-EPMC1574087 | biostudies-other
| S-EPMC5512168 | biostudies-literature
| S-EPMC6959550 | biostudies-literature
| S-EPMC8483473 | biostudies-literature
2016-12-01 | GSE75603 | GEO
| S-EPMC1774428 | biostudies-literature
| S-EPMC4735867 | biostudies-literature
| S-EPMC2974571 | biostudies-literature