Cannabinoid
Based on phylogenetic analysis, the family of cannabinoid receptors is separated into two different classes of the rhodopsin-like family of GPCRs. While CB1 and CB2 receptors share a group together with lysophospholipid (LPL) and melanocortin receptors (GPCR-A13), the newly recognized GPR55, GPR119, and GPR18 receptors are officially member of another group (GPCR-A15), together with protein activated receptors (PAR) and other LPL receptors[1]. Two orphan GPCRs have recently been implicated as novel cannabinoid receptors; these are GPR119, which has been proposed as a receptor for oleoylethanolamide, and GPR55 which has been proposed as a receptor activated by multiple different cannabinoid ligands. GPR55 has been demonstrated to interact with chemically unrelated cannabinoid ligands, in both mammalian and non-mammalian recombinant expression systems, and by independent research groups. Clearly, there is some relationship between the ligand-binding sites of GPR55 and CB1/CB2; however, the endogenous agonist and physiological relevance of GPR55 are not yet clear. Studies have suggested that L-α-lysophosphatidylinositol (LPI), which activates GPR55 but not CB1 or CB2 receptors, could be its endogenous ligand. Conversely, cannabidiol (CBD, Axon 1234) is a GPR55 antagonist[2]. GPR119 is strongly implicated in the regulation of energy balance and body weight. However, further corroborating data of the activity of acylethanolamides at GPR119 will be required before it can be regarded unequivocally as a cannabinoid receptor[3].
[1] P. Joost, A. Methner. Phylogenetic analysis of 277 human G-protein-coupled receptors as a tool for the prediction of orphan receptor ligands. Gen. Biol. 2002, 3, 0063.
[2] S. Sylantyev et al. Cannabinoid- and lysophosphatidylinositol-sensitive receptor GPR55 boosts neurotransmitter release at central synapses.Proc. Nat. Acad. Sci. USA 2013, 110, 5193-5198.
[3] A.J. Brown. Novel cannabinoid receptors. Br. J. Pharmacol. 2007, 152, 567-575.
Axon ID | Name | Description | From price | |
---|---|---|---|---|
1714 | (R)-(+)-SLV 319 | Inactive enantiomer of SLV 319 | €95.00 | |
1235 | Abnormal cannabidiol | Cannabinoid agonist | €135.00 | |
1218 | AM 251 | CB1 antagonist | €95.00 | |
1219 | AM 281 | CB1 antagonist | €95.00 | |
2791 | AM 4113 | CB1 antagonist | €105.00 | |
2541 | APD 597 | Orally bioavailable selective GPR119 agonist | €125.00 | |
2380 | APD 668 | Potent and selective, orally active GPR119 agonist | €125.00 | |
1572 | AR 231453 | Cannabinoid GPR119 agonist | €80.00 | |
3430 | AS1269574 | Selective and orally available GPR119 agonist | €90.00 | |
1234 | Cannabidiol | GPR55 antagonist | €105.00 | |
3955 | CB2R PAM C2 | First synthetic, potent and orally active CB2 receptor PAM | €120.00 | |
2015 | CP 945598 | CB1 antagonist | €135.00 | |
2119 | CP 945598 hydrochloride | CB1 antagonist | €135.00 | |
3097 | DBPR211 | Potent and selective peripherally restricted CB1 antagonist/inverse agonist | €125.00 | |
3632 | Genistein | CB1 antagonist | €70.00 | |
1925 | GW 842166X | Cannabinoid CB2 receptor agonist | €110.00 | |
1440 | HU 308 | CB2 agonist | €140.00 | |
1574 | Iodopravadoline | CB2 antagonist | €75.00 | |
1418 | JWH 133 | CB2 agonist | €110.00 | |
2092 | MBX 2982 | Potent and selective GPR119 agonist | €125.00 | |
1550 | MK 0364 | CB1 antagonist/inverse agonist | €95.00 | |
3028 | ML184 | Potent and selective GPR55 agonist | €120.00 | |
4125 | ML193 | Highly potent and selective GPR55 antagonist | €90.00 | |
1211 | Palmitoylethanolamide | Endocannabinoid; GPR55 agonist | €75.00 | |
1565 | PSNCBAM 1 | CB1 antagonist (allosteric) | €85.00 | |
1712 | rac-(±)-SLV 319 | Racemate of CB1 antagonist Ibipinabant (Axon 1713) | €110.00 | |
1713 | SLV 319 | CB1 antagonist | €105.00 | |
1220 | SR 141716 hydrochloride | CB1 antagonist | €70.00 | |
1924 | SR 144528 | CB2 receptor antagonist and/or an inverse agonist | €95.00 | |
2543 | ZCZ 011 | Brain penetrant CB1 positive allosteric modulator (PAM) | €90.00 |