Endocannabinoid enhancer
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.
- 1 2 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.
- 1 2 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.
- 1 2 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.
- 1 2 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.
- ↑ 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.
- ↑ 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. PMID 17227290.
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| Types | |
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| Classes | | see Enzyme inhibition |
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| Miscellaneous | |
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| Receptor (ligands) | |
- Antibodies: Brizantin (Бризантин)
- Dietressa (Диетресса)
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- 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
- Magnolol
- MDA-19
- Nabitan
- NADA
- PF-03550096
- S-444,823
- SER-601
- Serinolamide A
- UR-144
- Tedalinab
- THC (dronabinol)
- THCV
- Tetrahydromagnolol
- Virodhamine
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| Transporter (modulators) | |
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| Enzyme (modulators) | | |
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- Inhibitors: JZP-169
- JZP-430
- KT182
- KT185
- KT195
- KT203
- LEI-106
- ML294
- ML295
- ML296
- UCM710
- WWL-70
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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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- See also: Cannabinoids (cannabinoids by structure)
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