N-(4-HYDROXY-3-METHOXYBENZYL)-8-METHYL-6-NONENAMIDE

General Function:

Cannabinoid receptor activity

Specific Function:

Heterotrimeric G protein-coupled receptor for endocannabinoid 2-arachidonoylglycerol mediating inhibition of adenylate cyclase. May function in inflammatory response, nociceptive transmission and bone homeostasis.

Gene Name:

CNR2

Uniprot ID:

P34972

Molecular Weight:

39680.275 Da

References

1. Appendino G, De Petrocellis L, Trevisani M, Minassi A, Daddario N, Moriello AS, Gazzieri D, Ligresti A, Campi B, Fontana G, Pinna C, Geppetti P, Di Marzo V: Development of the first ultra-potent "capsaicinoid" agonist at transient receptor potential vanilloid type 1 (TRPV1) channels and its therapeutic potential. J Pharmacol Exp Ther. 2005 Feb;312(2):561-70. Epub 2004 Sep 8. [15356216 ]

General Function:

Drug binding

Specific Function:

Involved in cannabinoid-induced CNS effects. Acts by inhibiting adenylate cyclase. Could be a receptor for anandamide. Inhibits L-type Ca(2+) channel current. Isoform 2 and isoform 3 have altered ligand binding.

Gene Name:

CNR1

Uniprot ID:

P21554

Molecular Weight:

52857.365 Da

References

1. Appendino G, Ligresti A, Minassi A, Cascio MG, Allara M, Taglialatela-Scafati O, Pertwee RG, De Petrocellis L, Di Marzo V: Conformationally constrained fatty acid ethanolamides as cannabinoid and vanilloid receptor probes. J Med Chem. 2009 May 14;52(9):3001-9. doi: 10.1021/jm900130m. [19361197 ]

General Function:

Transmembrane signaling receptor activity

Specific Function:

Ligand-activated non-selective calcium permeant cation channel involved in detection of noxious chemical and thermal stimuli. Seems to mediate proton influx and may be involved in intracellular acidosis in nociceptive neurons. Involved in mediation of inflammatory pain and hyperalgesia. Sensitized by a phosphatidylinositol second messenger system activated by receptor tyrosine kinases, which involves PKC isozymes and PCL. Can be activated by endogenous compounds, including 12-hydroperoxytetraenoic acid and bradykinin. Acts as ionotropic endocannabinoid receptor with central neuromodulatory effects. Triggers a form of long-term depression (TRPV1-LTD) mediated by the endocannabinoid anandamine in the hippocampus and nucleus accumbens by affecting AMPA receptors endocytosis (By similarity). Activation by vanilloids, like capsaicin, and temperatures higher than 42 degrees Celsius, exhibits a time- and Ca(2+)-dependent outward rectification, followed by a long-lasting refractory state. Mild extracellular acidic pH (6.5) potentiates channel activation by noxious heat and vanilloids, whereas acidic conditions (pH <6) directly activate the channel.

Gene Name:

TRPV1

Uniprot ID:

Q8NER1

Molecular Weight:

94955.33 Da

References

1. Wikipedia. Capsaicin. Last Updated 16 July 2009. : http://en.wikipedia.org/wiki/Capsaicin [11606325 ]

General Function:

Prostaglandin-endoperoxide synthase activity

Specific Function:

Converts arachidonate to prostaglandin H2 (PGH2), a committed step in prostanoid synthesis. Involved in the constitutive production of prostanoids in particular in the stomach and platelets. In gastric epithelial cells, it is a key step in the generation of prostaglandins, such as prostaglandin E2 (PGE2), which plays an important role in cytoprotection. In platelets, it is involved in the generation of thromboxane A2 (TXA2), which promotes platelet activation and aggregation, vasoconstriction and proliferation of vascular smooth muscle cells.

Gene Name:

PTGS1

Uniprot ID:

P23219

Molecular Weight:

68685.82 Da

References

1. Larsson J, Gottfries J, Bohlin L, Backlund A: Expanding the ChemGPS chemical space with natural products. J Nat Prod. 2005 Jul;68(7):985-91. [16038536 ]

General Function:

Temperature-gated cation channel activity

Specific Function:

Receptor-activated non-selective cation channel involved in detection of pain and possibly also in cold perception and inner ear function (PubMed:25389312, PubMed:25855297). Has a central role in the pain response to endogenous inflammatory mediators and to a diverse array of volatile irritants, such as mustard oil, cinnamaldehyde, garlic and acrolein, an irritant from tears gas and vehicule exhaust fumes (PubMed:25389312, PubMed:20547126). Is also activated by menthol (in vitro)(PubMed:25389312). Acts also as a ionotropic cannabinoid receptor by being activated by delta(9)-tetrahydrocannabinol (THC), the psychoactive component of marijuana (PubMed:25389312). May be a component for the mechanosensitive transduction channel of hair cells in inner ear, thereby participating in the perception of sounds. Probably operated by a phosphatidylinositol second messenger system (By similarity).

Gene Name:

TRPA1

Uniprot ID:

O75762

Molecular Weight:

127499.88 Da

References

1. Lachrymation: http://aok.pte.hu/en/download/index/14785 [21078588 ]

General Function:

Acts as a mediator of transcriptional repression by nuclear hormone receptors via recruitment of histone deacetylases (By similarity). Functions as an estrogen receptor (ER)-selective coregulator that potentiates the inhibitory activities of antiestrogens and represses the activity of estrogens. Competes with NCOA1 for modulation of ER transcriptional activity. Probably involved in regulating mitochondrial respiration activity and in aging.

Specific Function:

Amide binding

Gene Name:

PHB2

Uniprot ID:

Q99623

Molecular Weight:

33296.06 Da