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. Author manuscript; available in PMC: 2015 Feb 15.
Published in final edited form as: Biochem Pharmacol. 2013 Dec 16;87(4):547–561. doi: 10.1016/j.bcp.2013.11.020

Table 1.

List of structures of select ligands and their known specificity to the various receptors.

Structure Name Chemical name Properties References
graphic file with name nihms550347t1.jpg (R,R′)-Fenoterol (Fen) 5-[(1R)-1-hydroxy-2-{[(2R)-1-(4-hydroxyphenyl) propan-2-yl]amino}ethyl] benzene-1,3-diol
  • β2-AR agonist

    Ki = 0.35 and 14.8 μM for β2-AR and β1-AR, respectively

[1]
graphic file with name nihms550347t2.jpg (R,R′)-4-methoxy-1-naphthylfenoterol (MNF) 5-[(1R)-1-hydroxy-2-{[(2R)-1-(4-methoxynaphthalen-1-yl)propan-2-yl]amino} ethyl]benzene-1,3-diol
  • Selective β2-AR agonist

    Ki = 0.28 and 160.5 μM for β2-AR and β1-AR, respectively

[2]
  • Involved in CB receptors signaling

[4]
graphic file with name nihms550347t3.jpg AM251 N-(Piperidin-1-yl)-5-(4-iodophenyl)--1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide
  • Selective CB1 receptor antagonist

    Ki = 7.5 nM

[20]
  • GPR55 agonist

    EC50 GTPγS = 39 nM

[21]
graphic file with name nihms550347t4.jpg rimonabant, SR 141716 N-(Piperidin-1-yl)-5-(4-chloropheny-l)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide
  • Selective CB1 receptor antagonist

    Ki = 1.98 nM

[22]
graphic file with name nihms550347t5.jpg AM630 6-Iodo-2-methyl-1-[2-(4-morpholinyl-)ethyl]-1H-indol-3-yl](4-methoxy phenyl)methanone
  • Selective CB2 receptor antagonist

    Ki = 31.2 nM

[23]
graphic file with name nihms550347t6.jpg WIN 55,212-2 (R)-(+)-[2,3-Dihydro-5-methyl-3-(4--morpholinylmethyl) pyrrolo[1,2,3-de]-1,4-benzoxazin--6-yl]-1-naphthalenylmethanone
  • CB receptor agonist

    Ki = 62.3 and 3.3 nM for CB1 and CB2 receptors, respectively

[24]
graphic file with name nihms550347t7.jpg O-1602 5-Methyl-4-[(1R,6R)-3-methyl-6-(1-c-yclohexen-1-yl]-1,3-benzenediol
  • Selective GPR55 receptor agonist

    EC50 GTPγS = 13, > 30000 and > 30000 nM for GPR55, CB1 and CB2 receptors, respectively

[21]
graphic file with name nihms550347t8.jpg L-α-Lysophosphatidyl inositol (LPI) 1-Acyl-sn-glycero-3-phospho-(1-D-myo-inositol)
  • Endogenous GPR55 receptor agonist

[25]
graphic file with name nihms550347t9.jpg CP 55,940 (−)-cis-3-[2-Hydroxy-4-(1,1-dimethy-lheptyl)phenyl]-trans-4-(3-hydroxypropyl) cyclohexanol
  • CB1 and CB2 receptors agonist

    Ki = 0.6 – 5.0 and 0.7 – 2.6 nM for CB1 and CB2, respectively

[26]
  • GPR55 antagonist

[11]