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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| Types |
- ♦ Miscellaneous: Precursor
- Cofactor
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| Classes | | Enzyme | see Enzyme inhibition |
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| Ion channel | See Ion channel modulators |
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Receptor & transporter | |
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| Miscellaneous |
- Cofactor (see Enzyme cofactors)
- Precursor (see Amino acids)
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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 |
- CBN
- CBNA
- CBN-C1
- CBN-C2
- CBN-C4
- CBNM
- CBND
- CBNP
- CBVD
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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 |
- 1-Butyl-3-(2-methoxybenzoyl)indole
- 1-Butyl-3-(4-methoxybenzoyl)indole
- 1-Pentyl-3-(2-methoxybenzoyl)indole
- AM-630
- AM-679
- AM-694
- AM-1241
- AM-2233
- GW-405,833 (L-768,242)
- Pravadoline
- RCS-4
- WIN 54,461
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| Cyclohexylphenols | |
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| Eicosanoids |
- AM-883
- AM-1346
- ACEA
- ACPA
- Methanandamide (AM-356)
- O-585
- O-689
- O-1812
- O-1860
- O-1861
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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 |
- JWH-030
- JWH-031
- JWH-032
- JWH-033
- JWH-036
- JWH-044
- JWH-045
- JWH-145
- JWH-146
- JWH-147
- JWH-150
- JWH-156
- JWH-243
- JWH-244
- JWH-245
- JWH-246
- JWH-292
- JWH-293
- JWH-307
- JWH-308
- JWH-309
- JWH-346
- JWH-347
- JWH-348
- JWH-363
- JWH-364
- JWH-365
- JWH-366
- JWH-367
- JWH-368
- JWH-369
- JWH-370
- JWH-371
- JWH-372
- JWH-373
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| Naphthylmethylindenes | |
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| Naphthylmethylindoles |
- JWH-175
- JWH-184
- JWH-185
- JWH-192
- JWH-194
- JWH-195
- JWH-196
- JWH-197
- JWH-199
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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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(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) | | FAAHTooltip Fatty acid amide hydrolase | |
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| MAGL | |
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| ABHD6 |
- Inhibitors: JZP-169
- JZP-430
- KT182
- KT185
- KT195
- KT203
- LEI-106
- ML294
- ML295
- ML296
- UCM710
- WWL-70
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| ABHD12 | |
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| Others |
- Precursors: Phosphatidylethanolamine
- NAPE
- Diacylglycerol
- Others: 2-PG (directly potentiates activity of 2-AG at CB1 receptor)
- ARN-272 (FAAH-like anandamide transporter inhibitor)
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- See also
- Receptor/signaling modulators
- Cannabinoids (cannabinoids by structure)
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