The activity of anandamide at vanilloid VR1 receptors requires facilitated transport across the cell membrane and is limited by intracellular metabolism

L De Petrocellis, T Bisogno, M Maccarrone… - Journal of Biological …, 2001 - ASBMB
The endogenous ligand of CB 1 cannabinoid receptors, anandamide, is also a full agonist at
vanilloid VR1 receptors for capsaicin and resiniferatoxin, thereby causing an increase in …

[HTML][HTML] Overlap between the ligand recognition properties of the anandamide transporter and the VR1 vanilloid receptor: inhibitors of anandamide uptake with …

L De Petrocellis, T Bisogno, JB Davis, RG Pertwee… - FEBS letters, 2000 - Elsevier
Some synthetic agonists of the VR1 vanilloid (capsaicin) receptor also inhibit the facilitated
transport into cells of the endogenous cannabinoid anandamide (arachidonoylethanolamide …

Structure‐activity relationship for the endogenous cannabinoid, anandamide, and certain of its analogues at vanilloid receptors in transfected cells and vas deferens

RA Ross, TM Gibson, HC Brockie… - British journal of …, 2001 - Wiley Online Library
This study was directed at exploring the structure‐activity relationship for anandamide and
certain of its analogues at the rat VR1 receptor in transfected cells and at investigating the …

Anandamide: some like it hot

V Di Marzo, T Bisogno, L De Petrocellis - Trends in pharmacological …, 2001 - cell.com
Anandamide was the first endogenous ligand of cannabinoid receptors to be discovered in
1992. Yet, this compound also efficiently activates receptors specific for capsaicin, known as …

Unsaturated long-chain N-acyl-vanillyl-amides (N-AVAMs): vanilloid receptor ligands that inhibit anandamide-facilitated transport and bind to CB1 cannabinoid …

D Melck, T Bisogno, L De Petrocellis, H Chuang… - Biochemical and …, 1999 - Elsevier
We investigated the effect of changing the length and degree of unsaturation of the fatty acyl
chain of N-(3-methoxy-4-hydroxy)-benzyl-cis-9-octadecenoamide (olvanil), a ligand of …

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

D Smart, MJ Gunthorpe, JC Jerman… - British journal of …, 2000 - Wiley Online Library
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 …

The vanilloid receptor (VR1)‐mediated effects of anandamide are potently enhanced by the cAMP‐dependent protein kinase

L De Petrocellis, S Harrison, T Bisogno… - Journal of …, 2001 - Wiley Online Library
The endogenous cannabinoid receptor ligand, anandamide (AEA), is a full agonist of the
vanilloid receptor type 1 (VR1) for capsaicin. Here, we demonstrate that the potency and …

Anandamide: an endogenous activator of the vanilloid receptor

D Smart, JC Jerman - Trends in pharmacological sciences, 2000 - cell.com
Anandamide: an endogenous activator of the vanilloid receptor Page 1 134 TiPS – April 2000
(Vol. 21) LETTERS Two recent articles1,2 have discussed whether the cannabinoid …

New perspectives on enigmatic vanilloid receptors

A Szallasi, V Di Marzo - Trends in neurosciences, 2000 - cell.com
In spite of the rapid advances in our understanding of vanilloid-receptor pharmacology in the
PNS, the function of vanilloid receptors in the brain has remained elusive. Recently, the …

[HTML][HTML] Palmitoylethanolamide enhances anandamide stimulation of human vanilloid VR1 receptors

L De Petrocellis, JB Davis, V Di Marzo - FEBS letters, 2001 - Elsevier
In human embryonic kidney cells over-expressing the human vanilloid receptor type 1
(VR1), palmitoylethanolamide (PEA, 0.5–10 μM) enhanced the effect of …