Table 1.
Receptor system | Mechanism | Potential therapeutic application | References |
---|---|---|---|
eCB | FAAH inhibitor | Intestinal motility; augmenting eCB tone; addiction; depression | Bisogno et al. 2001, Ligresti et al. 2006, Capasso et al. 2008, Leweke et al. 2012, Campos et al. 2013, Panlilio et al. 2013, Blanco et al. 2014, Chauvet et al. 2014 |
AEA uptake inhibitor | Augmenting eCB tone; addiction; depression | Rakhshan et al. 2000, Bisogno et al. 2001, Ligresti et al. 2006, Scherma et al. 2008, Gamaleddin et al. 2011, Leweke et al. 2012, Campos et al. 2013 | |
Antagonist of CB1/CB2 receptor agonists | Reduction of THC effects | Thomas et al. 2007, Pertwee 2008 | |
Expanded eCB | GPR55 antagonist | To be determined | Pertwee 2007, Ryberg et al. 2007, Rahimi et al. 2015 |
TRPV1 agonist | Schizophrenia; analgesia | Costa et al. 2007, De Petrocellis et al. 2008, Santos et al. 2008, Terzian et al. 2009, Adamczyk et al. 2012, Heng et al. 2014 | |
TRPV2 agonist | Vasodilation | Qin et al. 2008 | |
TRPA1 agonist | Analgesia | De Petrocellis et al. 2008 | |
TRPM8 antagonist | Analgesia; prostate cancer | De Petrocellis et al. 2008 | |
Serotonin | 5-HT1A agonist | Addiction; anxiety; depression; schizophrenia | Russo et al. 2005, Alex & Pehek 2007, Campos & Guimarães 2008, Resstel et al. 2009 |
5-HT2A agonist | Addiction; schizophrenia | Russo et al. 2005, Alex & Pehek 2007 | |
5-HT3 agonist | Addiction | Alex & Pehek 2007, Xiong et al. 2012 | |
Tryptophan degradation inhibitor | Addiction; anxiety; depression; pain; inflammation | Jenny et al. 2009, Ross 2009 | |
Adenosine | Adenosine uptake inhibitor and indirect A2A agonist | Addiction; inflammation | Carrier et al. 2006, Liou et al. 2008, Ferré et al. 2010 |
Opioid | Mu-opioid ligand | Addiction; pain | Pertwee et al. 2002 |
Mu- and delta-opioid positive allosteric modulator | Addiction; pain | Kathmann et al. 2006 | |
Dopamine | D2 allosteric modulator | Addiction | Bloom & Hillard 1985 |
Dopamine transporter inhibitor | Addiction; depression | Pandolfo et al. 2011 | |
Other | GABAA positive allosteric modulator | Addiction | Long et al. 2012 |
Alpha-1 and alpha-1-beta glycine receptor positive allosteric modulator | Pain; inflammation | Ahrens et al. 2009 | |
Regulator of intracellular calcium | Epilepsy; neuroprotection | Drysdale et al. 2006, Ryan et al. 2006 | |
T-type calcium channel inhibitor | Epilepsy; neuroprotection; pain | Ross 2009 | |
PPARγ agonist | Vasorelaxation; addiction | O’Sullivan et al. 2009, Enayatfard et al. 2013, Panlilio et al. 2013, de Guglielmo et al. 2014 |
Abbreviations: 5-HT, 5-hydroxytryptamine; AEA, N-arachidonoylethanolamine; CB1 and CB2, cannabinoid receptor type 1 and 2; eCB, endocannabinoid; FAAH, fatty acid amide hydrolase; PPARγ, peroxisome proliferator-activated receptor gamma; THC, Δ9-tetrahydrocannabinol; TRPA1, transient receptor potential cation channel A1; TRPM8, transient receptor potential cation channel M8; TRPV1 and TRPV2, transient receptor potential cation channel V1 and V2.