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Allosteric Cannabinoid Receptor 1 (CB1) Ligands Reduce Ocular Pain and Inflammation.

Thapa D, Cairns EA, Szczesniak AM, Kulkarni PM, Straiker AJ, Thakur GA, Kelly MEM.

Molecules. 2020 Jan 20;25(2). pii: E417. doi: 10.3390/molecules25020417.


Application of Fluorine- and Nitrogen-Walk Approaches: Defining the Structural and Functional Diversity of 2-Phenylindole Class of Cannabinoid 1 Receptor Positive Allosteric Modulators.

Garai S, Kulkarni PM, Schaffer PC, Leo LM, Brandt AL, Zagzoog A, Black T, Lin X, Hurst DP, Janero DR, Abood ME, Zimmowitch A, Straiker A, Pertwee RG, Kelly M, Szczesniak AM, Denovan-Wright EM, Mackie K, Hohmann AG, Reggio PH, Laprairie RB, Thakur GA.

J Med Chem. 2020 Jan 23;63(2):542-568. doi: 10.1021/acs.jmedchem.9b01142. Epub 2020 Jan 3.


Cannabinoid receptor-mediated modulation of inhibitory inputs to mitral cells in the main olfactory bulb.

Wang ZJ, Hu SS, Bradshaw HB, Sun L, Mackie K, Straiker A, Heinbockel T.

J Neurophysiol. 2019 Aug 1;122(2):749-759. doi: 10.1152/jn.00100.2018. Epub 2019 Jun 19.


Evidence for a GPR18 Role in Chemotaxis, Proliferation, and the Course of Wound Closure in the Cornea.

Murataeva N, Daily L, Taylor X, Dhopeshwarkar A, Hu SS, Miller S, McHugh D, Oehler O, Li S, Bonanno JA, Mackie K, Straiker A.

Cornea. 2019 Jul;38(7):905-913. doi: 10.1097/ICO.0000000000001934.


Cannabinoid CB2R receptors are upregulated with corneal injury and regulate the course of corneal wound healing.

Murataeva N, Miller S, Dhopeshwarkar A, Leishman E, Daily L, Taylor X, Morton B, Lashmet M, Bradshaw H, Hillard CJ, Romero J, Straiker A.

Exp Eye Res. 2019 May;182:74-84. doi: 10.1016/j.exer.2019.03.011. Epub 2019 Mar 21.


Δ9-Tetrahydrocannabinol and Cannabidiol Differentially Regulate Intraocular Pressure.

Miller S, Daily L, Leishman E, Bradshaw H, Straiker A.

Invest Ophthalmol Vis Sci. 2018 Dec 3;59(15):5904-5911. doi: 10.1167/iovs.18-24838.


Synthesis and evaluation of potent and selective MGL inhibitors as a glaucoma treatment.

Alapafuja SO, Malamas MS, Shukla V, Zvonok A, Miller S, Daily L, Rajarshi G, Miyabe CY, Chandrashekhar H, Wood J, Tyukhtenko S, Straiker A, Makriyannis A.

Bioorg Med Chem. 2019 Jan 1;27(1):55-64. doi: 10.1016/j.bmc.2018.11.003. Epub 2018 Nov 3.


Inflammation and CB2 signaling drive novel changes in the ocular lipidome and regulate immune cell activity in the eye.

Toguri JT, Leishman E, Szczesniak AM, Laprairie RB, Oehler O, Straiker AJ, Kelly MEM, Bradshaw HB.

Prostaglandins Other Lipid Mediat. 2018 Nov;139:54-62. doi: 10.1016/j.prostaglandins.2018.09.004. Epub 2018 Sep 16.


Revisiting cannabinoid receptor 2 expression and function in murine retina.

Borowska-Fielding J, Murataeva N, Smith B, Szczesniak AM, Leishman E, Daily L, Toguri JT, Hillard CJ, Romero J, Bradshaw H, Kelly MEM, Straiker A.

Neuropharmacology. 2018 Oct;141:21-31. doi: 10.1016/j.neuropharm.2018.08.007. Epub 2018 Aug 16.


Controlled-Deactivation CB1 Receptor Ligands as a Novel Strategy to Lower Intraocular Pressure.

Miller S, Kulkarni S, Ciesielski A, Nikas SP, Mackie K, Makriyannis A, Straiker A.

Pharmaceuticals (Basel). 2018 May 22;11(2). pii: E50. doi: 10.3390/ph11020050.


Cannabidiol Inhibits Endocannabinoid Signaling in Autaptic Hippocampal Neurons.

Straiker A, Dvorakova M, Zimmowitch A, Mackie K.

Mol Pharmacol. 2018 Jul;94(1):743-748. doi: 10.1124/mol.118.111864. Epub 2018 Apr 18.


Enantiomer-specific positive allosteric modulation of CB1 signaling in autaptic hippocampal neurons.

Mitjavila J, Yin D, Kulkarni PM, Zanato C, Thakur GA, Ross R, Greig I, Mackie K, Straiker A.

Pharmacol Res. 2018 Mar;129:475-481. doi: 10.1016/j.phrs.2017.11.019. Epub 2017 Nov 20.


The In Vivo Effects of the CB1-Positive Allosteric Modulator GAT229 on Intraocular Pressure in Ocular Normotensive and Hypertensive Mice.

Cairns EA, Szczesniak AM, Straiker AJ, Kulkarni PM, Pertwee RG, Thakur GA, Baldridge WH, Kelly MEM.

J Ocul Pharmacol Ther. 2017 Oct;33(8):582-590. doi: 10.1089/jop.2017.0037. Epub 2017 Jul 18.


Discovery and characterization of two novel CB1 receptor splice variants with modified N-termini in mouse.

Ruehle S, Wager-Miller J, Straiker A, Farnsworth J, Murphy MN, Loch S, Monory K, Mackie K, Lutz B.

J Neurochem. 2017 Aug;142(4):521-533. doi: 10.1111/jnc.14099. Epub 2017 Jul 18.


A GPR119 Signaling System in the Murine Eye Regulates Intraocular Pressure in a Sex-Dependent Manner.

Miller S, Hu SS, Leishman E, Morgan D, Wager-Miller J, Mackie K, Bradshaw HB, Straiker A.

Invest Ophthalmol Vis Sci. 2017 Jun 1;58(7):2930-2938. doi: 10.1167/iovs.16-21330.


Two Janus Cannabinoids That Are Both CB2 Agonists and CB1 Antagonists.

Dhopeshwarkar A, Murataeva N, Makriyannis A, Straiker A, Mackie K.

J Pharmacol Exp Ther. 2017 Feb;360(2):300-311. doi: 10.1124/jpet.116.236539. Epub 2016 Dec 7.


Evidence for a GPR18 Role in Diurnal Regulation of Intraocular Pressure.

Miller S, Leishman E, Oehler O, Daily L, Murataeva N, Wager-Miller J, Bradshaw H, Straiker A.

Invest Ophthalmol Vis Sci. 2016 Nov 1;57(14):6419-6426. doi: 10.1167/iovs.16-19437.


Harnessing the Endocannabinoid 2-Arachidonoylglycerol to Lower Intraocular Pressure in a Murine Model.

Miller S, Leishman E, Hu SS, Elghouche A, Daily L, Murataeva N, Bradshaw H, Straiker A.

Invest Ophthalmol Vis Sci. 2016 Jun 1;57(7):3287-96. doi: 10.1167/iovs.16-19356.


Where's my entourage? The curious case of 2-oleoylglycerol, 2-linolenoylglycerol, and 2-palmitoylglycerol.

Murataeva N, Dhopeshwarkar A, Yin D, Mitjavila J, Bradshaw H, Straiker A, Mackie K.

Pharmacol Res. 2016 Aug;110:173-180. doi: 10.1016/j.phrs.2016.04.015. Epub 2016 Apr 23.


Broad impact of deleting endogenous cannabinoid hydrolyzing enzymes and the CB1 cannabinoid receptor on the endogenous cannabinoid-related lipidome in eight regions of the mouse brain.

Leishman E, Cornett B, Spork K, Straiker A, Mackie K, Bradshaw HB.

Pharmacol Res. 2016 Aug;110:159-172. doi: 10.1016/j.phrs.2016.04.020. Epub 2016 Apr 22.


Aiming for allosterism: Evaluation of allosteric modulators of CB1 in a neuronal model.

Straiker A, Mitjavila J, Yin D, Gibson A, Mackie K.

Pharmacol Res. 2015 Sep;99:370-6. doi: 10.1016/j.phrs.2015.07.017. Epub 2015 Jul 23.


Cannabinoid-induced chemotaxis in bovine corneal epithelial cells.

Murataeva N, Li S, Oehler O, Miller S, Dhopeshwarkar A, Hu SS, Bonanno JA, Bradshaw H, Mackie K, McHugh D, Straiker A.

Invest Ophthalmol Vis Sci. 2015 May;56(5):3304-13. doi: 10.1167/iovs.14-15675.


Cannabinoid receptor-interacting protein 1a modulates CB1 receptor signaling and regulation.

Smith TH, Blume LC, Straiker A, Cox JO, David BG, McVoy JR, Sayers KW, Poklis JL, Abdullah RA, Egertová M, Chen CK, Mackie K, Elphick MR, Howlett AC, Selley DE.

Mol Pharmacol. 2015 Apr;87(4):747-65. doi: 10.1124/mol.114.096495. Epub 2015 Feb 5.


AM841, a covalent cannabinoid ligand, powerfully slows gastrointestinal motility in normal and stressed mice in a peripherally restricted manner.

Keenan CM, Storr MA, Thakur GA, Wood JT, Wager-Miller J, Straiker A, Eno MR, Nikas SP, Bashashati M, Hu H, Mackie K, Makriyannis A, Sharkey KA.

Br J Pharmacol. 2015 May;172(9):2406-18. doi: 10.1111/bph.13069. Epub 2015 Feb 27.


Cannabinoid and lipid-mediated vasorelaxation in retinal microvasculature.

MacIntyre J, Dong A, Straiker A, Zhu J, Howlett SE, Bagher A, Denovan-Wright E, Yu DY, Kelly ME.

Eur J Pharmacol. 2014 Jul 15;735:105-14. doi: 10.1016/j.ejphar.2014.03.055. Epub 2014 Apr 18.


Mutation of putative GRK phosphorylation sites in the cannabinoid receptor 1 (CB1R) confers resistance to cannabinoid tolerance and hypersensitivity to cannabinoids in mice.

Morgan DJ, Davis BJ, Kearn CS, Marcus D, Cook AJ, Wager-Miller J, Straiker A, Myoga MH, Karduck J, Leishman E, Sim-Selley LJ, Czyzyk TA, Bradshaw HB, Selley DE, Mackie K.

J Neurosci. 2014 Apr 9;34(15):5152-63. doi: 10.1523/JNEUROSCI.3445-12.2014.


Parsing the players: 2-arachidonoylglycerol synthesis and degradation in the CNS.

Murataeva N, Straiker A, Mackie K.

Br J Pharmacol. 2014 Mar;171(6):1379-91. doi: 10.1111/bph.12411. Review.


Diacylglycerol lipaseα (DAGLα) and DAGLβ cooperatively regulate the production of 2-arachidonoyl glycerol in autaptic hippocampal neurons.

Jain T, Wager-Miller J, Mackie K, Straiker A.

Mol Pharmacol. 2013 Aug;84(2):296-302. doi: 10.1124/mol.113.085217. Epub 2013 Jun 7.


Fmr1 deletion enhances and ultimately desensitizes CB(1) signaling in autaptic hippocampal neurons.

Straiker A, Min KT, Mackie K.

Neurobiol Dis. 2013 Aug;56:1-5. doi: 10.1016/j.nbd.2013.04.002. Epub 2013 Apr 9.


GPR55, a G-protein coupled receptor for lysophosphatidylinositol, plays a role in motor coordination.

Wu CS, Chen H, Sun H, Zhu J, Jew CP, Wager-Miller J, Straiker A, Spencer C, Bradshaw H, Mackie K, Lu HC.

PLoS One. 2013;8(4):e60314. doi: 10.1371/journal.pone.0060314. Epub 2013 Apr 2.


A GPR18-based signalling system regulates IOP in murine eye.

Caldwell MD, Hu SS, Viswanathan S, Bradshaw H, Kelly ME, Straiker A.

Br J Pharmacol. 2013 Jun;169(4):834-43. doi: 10.1111/bph.12136.


The CB2-preferring agonist JWH015 also potently and efficaciously activates CB1 in autaptic hippocampal neurons.

Murataeva N, Mackie K, Straiker A.

Pharmacol Res. 2012 Nov;66(5):437-42. doi: 10.1016/j.phrs.2012.08.002. Epub 2012 Aug 14.


CB₂ cannabinoid receptors inhibit synaptic transmission when expressed in cultured autaptic neurons.

Atwood BK, Straiker A, Mackie K.

Neuropharmacology. 2012 Sep;63(4):514-23. doi: 10.1016/j.neuropharm.2012.04.024. Epub 2012 May 8.


Sticking out of the crowd: the molecular identity and development of cholecystokinin-containing basket cells.

Keimpema E, Straiker A, Mackie K, Harkany T, Hjerling-Leffler J.

J Physiol. 2012 Feb 15;590(4):703-14. doi: 10.1113/jphysiol.2011.224386. Epub 2012 Jan 4. Review.


CB₂: therapeutic target-in-waiting.

Atwood BK, Straiker A, Mackie K.

Prog Neuropsychopharmacol Biol Psychiatry. 2012 Jul 2;38(1):16-20. doi: 10.1016/j.pnpbp.2011.12.001. Epub 2011 Dec 9. Review.


The endocannabinoid N-arachidonoyldopamine (NADA) exerts neuroprotective effects after excitotoxic neuronal damage via cannabinoid receptor 1 (CB(1)).

Grabiec U, Koch M, Kallendrusch S, Kraft R, Hill K, Merkwitz C, Ghadban C, Lutz B, Straiker A, Dehghani F.

Neuropharmacology. 2012 Mar;62(4):1797-807. doi: 10.1016/j.neuropharm.2011.11.023. Epub 2011 Dec 13.


Functional selectivity in CB(2) cannabinoid receptor signaling and regulation: implications for the therapeutic potential of CB(2) ligands.

Atwood BK, Wager-Miller J, Haskins C, Straiker A, Mackie K.

Mol Pharmacol. 2012 Feb;81(2):250-63. doi: 10.1124/mol.111.074013. Epub 2011 Nov 7.


Differential signalling in human cannabinoid CB1 receptors and their splice variants in autaptic hippocampal neurones.

Straiker A, Wager-Miller J, Hutchens J, Mackie K.

Br J Pharmacol. 2012 Apr;165(8):2660-71. doi: 10.1111/j.1476-5381.2011.01744.x.


The CB1 cannabinoid receptor C-terminus regulates receptor desensitization in autaptic hippocampal neurones.

Straiker A, Wager-Miller J, Mackie K.

Br J Pharmacol. 2012 Apr;165(8):2652-9. doi: 10.1111/j.1476-5381.2011.01743.x.


Indirect sympatholytic actions at β-adrenoceptors account for the ocular hypotensive actions of cannabinoid receptor agonists.

Hudson BD, Beazley M, Szczesniak AM, Straiker A, Kelly ME.

J Pharmacol Exp Ther. 2011 Dec;339(3):757-67. doi: 10.1124/jpet.111.185769. Epub 2011 Sep 1.


COX-2 and fatty acid amide hydrolase can regulate the time course of depolarization-induced suppression of excitation.

Straiker A, Wager-Miller J, Hu SS, Blankman JL, Cravatt BF, Mackie K.

Br J Pharmacol. 2011 Nov;164(6):1672-83. doi: 10.1111/j.1476-5381.2011.01486.x.


CP47,497-C8 and JWH073, commonly found in 'Spice' herbal blends, are potent and efficacious CB(1) cannabinoid receptor agonists.

Atwood BK, Lee D, Straiker A, Widlanski TS, Mackie K.

Eur J Pharmacol. 2011 Jun 1;659(2-3):139-45. doi: 10.1016/j.ejphar.2011.01.066. Epub 2011 Feb 16.


Expression of G protein-coupled receptors and related proteins in HEK293, AtT20, BV2, and N18 cell lines as revealed by microarray analysis.

Atwood BK, Lopez J, Wager-Miller J, Mackie K, Straiker A.

BMC Genomics. 2011 Jan 7;12:14. doi: 10.1186/1471-2164-12-14.


Architecture of cannabinoid signaling in mouse retina.

Hu SS, Arnold A, Hutchens JM, Radicke J, Cravatt BF, Wager-Miller J, Mackie K, Straiker A.

J Comp Neurol. 2010 Sep 15;518(18):3848-66. doi: 10.1002/cne.22429.


JWH018, a common constituent of 'Spice' herbal blends, is a potent and efficacious cannabinoid CB receptor agonist.

Atwood BK, Huffman J, Straiker A, Mackie K.

Br J Pharmacol. 2010 Jun;160(3):585-93. doi: 10.1111/j.1476-5381.2009.00582.x. Epub 2010 Jan 22.


Monoacylglycerol lipase limits the duration of endocannabinoid-mediated depolarization-induced suppression of excitation in autaptic hippocampal neurons.

Straiker A, Hu SS, Long JZ, Arnold A, Wager-Miller J, Cravatt BF, Mackie K.

Mol Pharmacol. 2009 Dec;76(6):1220-7. doi: 10.1124/mol.109.059030. Epub 2009 Sep 18.


Cannabinoid signaling in inhibitory autaptic hippocampal neurons.

Straiker A, Mackie K.

Neuroscience. 2009 Sep 29;163(1):190-201. doi: 10.1016/j.neuroscience.2009.06.004. Epub 2009 Jun 6.


Cannabinoid CB1 receptor-dependent long-term depression in autaptic excitatory neurons.

Kellogg R, Mackie K, Straiker A.

J Neurophysiol. 2009 Aug;102(2):1160-71. doi: 10.1152/jn.00266.2009. Epub 2009 Jun 3.


Incensole acetate, an incense component, elicits psychoactivity by activating TRPV3 channels in the brain.

Moussaieff A, Rimmerman N, Bregman T, Straiker A, Felder CC, Shoham S, Kashman Y, Huang SM, Lee H, Shohami E, Mackie K, Caterina MJ, Walker JM, Fride E, Mechoulam R.

FASEB J. 2008 Aug;22(8):3024-34. doi: 10.1096/fj.07-101865. Epub 2008 May 20.


Metabotropic suppression of excitation in murine autaptic hippocampal neurons.

Straiker A, Mackie K.

J Physiol. 2007 Feb 1;578(Pt 3):773-85. Epub 2006 Nov 16.

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