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. doi:10.1016/S0022-3565(24)29345-9. 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.
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Phytocannabinoids (comparison) | Cannabibutols | |
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Cannabichromenes | |
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Cannabicyclols | |
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Cannabidiols | |
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Cannabielsoins | |
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Cannabigerols | |
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Cannabiphorols | |
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Cannabinols | |
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Cannabitriols | |
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Cannabivarins | |
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Delta-3-tetrahydrocannabinols | |
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Delta-4-tetrahydrocannabinols | |
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Delta-7-tetrahydrocannabinols | |
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Delta-8-tetrahydrocannabinols | |
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Delta-9-tetrahydrocannabinols | |
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Delta-10-Tetrahydrocannabinols | |
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Delta-11-Tetrahydrocannabinols | |
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Miscellaneous cannabinoids | |
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Active metabolites | |
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Endocannabinoids | |
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Synthetic cannabinoid receptor agonists / neocannabinoids | Classical cannabinoids (dibenzopyrans) | |
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Non-classical cannabinoids | |
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Adamantoylindoles | |
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Benzimidazoles | |
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Benzoylindoles | |
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Cyclohexylphenols | |
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Eicosanoids | |
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Indazole-3- carboxamides | |
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Indole-3-carboxamides | |
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Indole-3-carboxylates | |
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Naphthoylindazoles | |
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Naphthoylindoles | |
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Naphthoylpyrroles | |
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Naphthylmethylindenes | |
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Naphthylmethylindoles | |
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Phenylacetylindoles | |
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Pyrazolecarboxamides | |
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Tetramethylcyclo- propanoylindazoles | |
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Tetramethylcyclo- propanoylindoles | |
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Others | |
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Allosteric CBRTooltip Cannabinoid receptor ligands | |
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Endocannabinoid enhancers (inactivation inhibitors) | |
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Anticannabinoids (antagonists/inverse agonists/antibodies) | |
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Receptor (ligands) | CB1Tooltip Cannabinoid receptor type 1 | Agonists (abridged, full list) | |
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Inverse agonists | |
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Antagonists | |
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CB2Tooltip 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
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Antagonists | |
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NAGly (GPR18) | |
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GPR55 | |
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GPR119 | |
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Transporter (modulators) | eCBTsTooltip Endocannabinoid transporter | |
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Enzyme (modulators) | |
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Others |
- Others: 2-PG (directly potentiates activity of 2-AG at CB1 receptor)
- ARN-272 (FAAH-like anandamide transporter inhibitor)
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