From Wikipedia, the free encyclopedia
Type of cannabinoidergic drug
An endocannabinoid enhancer (eCBE ) is a type of
cannabinoidergic
[1]
drug that enhances the activity of the
endocannabinoid system by increasing
extracellular
concentrations of
endocannabinoids .
[2]
[3]
[4]
[5] Examples of different types of eCBEs include
fatty acid amide hydrolase (FAAH)
inhibitors ,
monoacylglycerol lipase (MAGL)
inhibitors , and
endocannabinoid transporter (eCBT) inhibitors (or "
endocannabinoid reuptake inhibitors " ("eCBRIs")).
[2]
[3]
[4]
[5] An example of an actual eCBE is
AM404 , the
active metabolite of the
analgesic
paracetamol (acetaminophen; Tylenol) and a dual FAAH inhibitor and eCBRI.
[6]
[7]
[8]
See also
References
^ George I. Papakostas; Maurizio Fava (2010).
Pharmacotherapy for Depression and Treatment-resistant Depression . World Scientific. pp. 323–.
ISBN
978-981-4287-59-3 .
^
a
b Bambico, Francis Rodriguez;
Gobbi, Gabriella (2008). "The cannabinoid CB1 receptor and the endocannabinoid anandamide: possible antidepressant targets". Expert Opinion on Therapeutic Targets . 12 (11): 1347–1366.
doi :
10.1517/14728222.12.11.1347 .
ISSN
1472-8222 .
PMID
18851692 .
S2CID
86111417 .
^
a
b Di Marzo, Vincenzo (2008). "Targeting the endocannabinoid system: to enhance or reduce?". Nature Reviews Drug Discovery . 7 (5): 438–455.
doi :
10.1038/nrd2553 .
ISSN
1474-1776 .
PMID
18446159 .
S2CID
21081378 .
^
a
b Saito, Viviane M.; Wotjak, Carsten T.; Moreira, Fabrício A. (2010).
"Pharmacological exploitation of the endocannabinoid system: new perspectives for the treatment of depression and anxiety disorders?" . Rev Bras Psiquiatr . 32 (1): 57–514.
doi :
10.1590/S1516-44462010000500004 .
ISSN
1516-4446 .
PMID
20512266 .
^
a
b Micale, Vincenzo; Di Marzo, Vincenzo; Sulcova, Alexandra; Wotjak, Carsten T.; Drago, Filippo (2013). "Endocannabinoid system and mood disorders: Priming a target for new therapies". Pharmacology & Therapeutics . 138 (1): 18–37.
doi :
10.1016/j.pharmthera.2012.12.002 .
ISSN
0163-7258 .
PMID
23261685 .
^ Giuffrida A, Beltramo M, Piomelli D (2001). "Mechanisms of endocannabinoid inactivation: biochemistry and pharmacology". J. Pharmacol. Exp. Ther . 298 (1): 7–14.
PMID
11408519 .
^ Anderson BJ (2008).
"Paracetamol (Acetaminophen): mechanisms of action" . Paediatr Anaesth . 18 (10): 915–21.
doi :
10.1111/j.1460-9592.2008.02764.x .
PMID
18811827 .
S2CID
17115356 .
^ Bertolini A, Ferrari A, Ottani A, Guerzoni S, Tacchi R, Leone S (2006).
"Paracetamol: new vistas of an old drug" . CNS Drug Rev . 12 (3–4): 250–75.
doi :
10.1111/j.1527-3458.2006.00250.x .
PMC
6506194 .
PMID
17227290 .
Phytocannabinoids (
comparison )
Cannabibutols Cannabichromenes Cannabicyclols Cannabidiols Cannabielsoins Cannabigerols Cannabiphorols Cannabinols Cannabitriols Cannabivarins Delta-8-tetrahydrocannabinols Delta-9-tetrahydrocannabinols Delta-10-Tetrahydrocannabinols Miscellaneous cannabinoids Active metabolites
Endocannabinoids
Synthetic cannabinoid receptor agonists / neocannabinoids
Classical cannabinoids (dibenzopyrans) Non-classical cannabinoids Adamantoylindoles Benzimidazoles Benzoylindoles Cyclohexylphenols
Eicosanoids
Hydrocarbons Indazole carboxamides Indazole-3- carboxamides Indole-3-carboxamides Indole-3-carboxylates Naphthoylindazoles
Naphthoylindoles Naphthoylpyrroles Naphthylmethylindenes Naphthylmethylindoles Phenylacetylindoles Pyrazolecarboxamides Pyrrolobenzoxazines Quinolinyl esters Tetramethylcyclo- propanoylindazoles Tetramethylcyclo- propanoylindoles Tetramethylcyclo- propylindoles Others
Allosteric
CBR Tooltip Cannabinoid receptor
ligands
Endocannabinoid enhancers (inactivation inhibitors)
Anticannabinoids (antagonists/inverse agonists/antibodies)
Receptor (
ligands )
CB1 Tooltip Cannabinoid receptor type 1
Agonists(abridged,
full list ) Inverse agonists Antagonists
CB2 Tooltip Cannabinoid receptor type 2
Agonists
2-AG
2-AGE (noladin ether)
3,3'-Diindolylmethane
4-O-Methylhonokiol
α-Amyrin · β-Amyrin
A-796,260
A-834,735
A-836,339
AM-1172
AM-1221
AM-1235
AM-1241
AM-2232
Anandamide
AZ-11713908
Cannabinol
Caryophyllene
CB-13
CBS-0550
CP 55,940
GW-405,833 (L-768,242)
GW-842,166X
HU-308
JTE 7-31
JWH-007
JWH-015
JWH-018
JWH-73
JWH-133
L-759,633
L-759,656
Lenabasum (anabasum)
Magnolol
MDA-19
Nabitan
NADA
Olorinab (APD-371)
PF-03550096
S-444,823
SER-601
Serinolamide A
UR-144
Tedalinab
THC (dronabinol)
THCV
Tetrahydromagnolol
Virodhamine
Antagonists
NAGly (
GPR18 )
GPR55
GPR119
Transporter (
modulators )
eCBTs Tooltip Endocannabinoid transporter
Enzyme (
modulators )
Others
Others:
2-PG (directly potentiates activity of 2-AG at CB1 receptor)
ARN-272 (FAAH-like anandamide transporter inhibitor)