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 Indazole-3- carboxamides Indole-3-carboxamides Indole-3-carboxylates Naphthoylindazoles Naphthoylindoles Naphthoylpyrroles Naphthylmethylindenes Naphthylmethylindoles Phenylacetylindoles Pyrazolecarboxamides Tetramethylcyclo- propanoylindazoles Tetramethylcyclo- propanoylindoles 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)