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 [ ]
Cannabinoid receptor
Synthetic cannabinoid
Cannabinoid receptor antagonist
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 .
Pharmacomodulation
Types
♦ Receptor : Agonist
Partial agonist
Antagonist
Inverse agonist
Positive allosteric modulator (PAM)
Negative allosteric modulator (NAM)
♦ Miscellaneous: Precursor
Cofactor
Classes
Enzyme see Enzyme inhibition
Ion channel See Ion channel modulators
Receptor &transporter
BA /M
Adrenergic Dopaminergic
Dopamine receptor agonist
Dopamine receptor antagonist
Dopamine reuptake inhibitor (DRI)
Histaminergic Serotonergic
AA
Cholinergic
Acetylcholine receptor agonist (Muscarinic
Nicotinic )
Acetylcholine receptor antagonist (Muscarinic
Nicotinic (Ganglionic
Muscular ))
Cannabinoidergic Opioidergic
Opioid modulator
Opioid receptor agonist
Opioid receptor antagonist
Enkephalinase inhibitor
Other
Miscellaneous
Cofactor (see Enzyme cofactors )
Precursor (see Amino acids )
Cannabinoids
Phytocannabinoids
Cannabichromenes Cannabicyclols Cannabidiols Cannabielsoins Cannabigerols Cannabinols and cannabinodiols Cannabitriols Delta-8-tetrahydrocannabinols Delta-9-tetrahydrocannabinols
Delta-9-THC (THC)
THCH
THCP
THCV
Miscellaneous cannabinoids Active metabolites
Endocannabinoids
Arachidonoyl ethanolamide (AEA; anandamide)
2-Arachidonoylglycerol (2-AG)
2-Arachidonyl glyceryl ether (2-AGE; noladin ether)
2-Oleoylglycerol (2-OG)
N-Arachidonoyl dopamine (NADA)
N-Arachidonylglycine (NAGly)
N-Arachidonoyl serotonin (AA-5-HT)
Docosatetraenoylethanolamide (DEA)
Lysophosphatidylinositol (LPI)
Oleamide
Oleoylethanolamide (OEA)
Palmitoylethanolamide (PEA)
RVD-Hpα
Stearoylethanolamide (SEA)
O-Arachidonoyl ethanolamine (O-AEA; virodhamine)
Synthetic cannabinoid receptor agonists / neocannabinoids
Classical cannabinoids (dibenzopyrans) Non-classical cannabinoids Adamantoylindoles Benzimidazoles Benzoylindoles
AM-630
AM-679
AM-694
AM-1241
AM-2233
GW-405,833 (L-768,242)
Pravadoline
RCS-4
WIN 54,461
Cyclohexylphenols Eicosanoids
ACEA
ACPA
Methanandamide (AM-356)
O-1812
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
A-796,260
A-834,735
FUB-144
UR-144
XLR-11
XLR-12
Tetramethylcyclo- propylindoles Others
Allosteric CBR ligands Endocannabinoid enhancers (inactivation inhibitors) Anticannabinoids (antagonists/inverse agonists/antibodies)
AM-251
AM-630
AM-6545
BML-190
Drinabant (AVE1625)
Hemopressin
Ibipinabant (SLV319)
JTE-907
LY-320,135
MK-9470
NESS-0327
O-1918
O-2050
Otenabant (CP-945,598)
PF-514273
PipISB
PSB-SB-487
Rimonabant (SR141716)
Rosonabant (E-6776)
SR-144,528
Surinabant (SR147778)
Taranabant (MK-0364)
TM-38837
VCHSR
See also: Cannabinoid receptor modulators (cannabinoids by pharmacology)
List of: AM cannabinoids
JWH cannabinoids
Designer drugs § Synthetic cannabimimetics
Receptor (ligands )
CB1
Agonists (abridged; see here for more) : 2-AG
2-AGE (noladin ether)
11-Hydroxy-THC
α-Amyrin · β-Amyrin
AB-CHMINACA
AM-1220
AM-1221
AM-1235
AM-2201
AM-2232
Anandamide
AZ-11713908
Cannabinol
CB-13
CP 47,497
CP 55,940
Dimethylheptylpyran
DEA
ECG
EGCG
Epicatechin
Gallocatechol (gallocatechin)
Honokiol
HU-210
JWH-007
JWH-015
JWH-018
JWH-073
Kavain
L-759,633
Levonantradol
Menabitan
Nabilone
Nabitan
NADA
O-1812
Oleamide
Pravadoline
Serinolamide A
THC (dronabinol)
UR-144
WIN 55,212-2
Yangonin
Antagonists: AM-251
AM-6545
Cannabidiol
Cannabigerol
Drinabant
Falcarinol (carotatoxin)
Hemopressin
Ibipinabant
LY-320,135
MK-9470
NESS-0327
O-2050
Otenabant
PF-514273
PipISB
Rimonabant
Rosonabant
Surinabant
Taranabant
THCV
TM-38837
VCHSR
Virodhamine
CB2
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-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-133
L-759,633
L-759,656
Magnolol
MDA-19
Nabitan
NADA
Olorinab (APD-371)
PF-03550096
S-444,823
SER-601
Serinolamide A
UR-144
Tedalinab
THC (dronabinol)
THCV
Virodhamine
Antagonists: 4-O-Methylhonokiol
AM-630
BML-190
Cannabidiol
Honokiol
JTE-907
SR-144,528
WIN 54,461
WIN 56,098
NAGly (GPR18 )
Agonists: Abnormal cannabidiol
ACPA
AM251
Anandamide
Cannabidiol
NADGly
THC (dronabinol)
O-1602
GPR55
Agonists: 2-AGE (noladin ether)
Abnormal cannabidiol
AM-251
CP 55,940
Lysophosphatidylinositol
O-1602
Oleoylethanolamide
Palmitoylethanolamide
THC (dronabinol)
GPR119 Unsorted
Transporter (modulators )
eCBTs
Inhibitors:
AM-404
Arachidonoyl serotonin
Cannabidiol
Guineensine
LY-2183240
Paracetamol (acetaminophen)
URB-597
VDM-11
Enzyme (modulators )
FAAH MAGL
Inhibitors:
IDFP
JZL-184
JZL-195
MAFP
URB-602
ABHD6 ABHD12
Inhibitors: Betulinic acid
Maslinic acid
MAFP
Oleanolic acid
Orlistat (tetrahydrolipstatin)
Ursolic acid
Others
Precursors: Phosphatidylethanolamine
NAPE
Diacylglycerol
Others: (directly potentiates activity of 2-AG at CB1 receptor)
(FAAH-like anandamide transporter inhibitor)
See also
Receptor/signaling modulators
Cannabinoids (cannabinoids by structure)