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Items: 1 to 50 of 87

1.

Polyamidoamine dendrimers-based nanomedicine for combination therapy with siRNA and chemotherapeutics to overcome multidrug resistance.

Pan J, Palmerston Mendes L, Yao M, Filipczak N, Garai S, Thakur GA, Sarisozen C, Torchilin VP.

Eur J Pharm Biopharm. 2019 Jan 8. pii: S0939-6411(18)31217-7. doi: 10.1016/j.ejpb.2019.01.006. [Epub ahead of print]

PMID:
30633973
2.

B-973, a Novel α7 nAChR Ago-PAM: Racemic and Asymmetric Synthesis, Electrophysiological Studies, and in Vivo Evaluation.

Garai S, Raja KS, Papke RL, Deschamps JR, Damaj MI, Thakur GA.

ACS Med Chem Lett. 2018 Oct 11;9(11):1144-1148. doi: 10.1021/acsmedchemlett.8b00407. eCollection 2018 Nov 8.

PMID:
30429960
3.

Macroscopic and Microscopic Activation of α7 Nicotinic Acetylcholine Receptors by the Structurally Unrelated Allosteric Agonist-Positive Allosteric Modulators (ago-PAMs) B-973B and GAT107.

Quadri M, Garai S, Thakur GA, Stokes C, Gulsevin A, Horenstein NA, Papke RL.

Mol Pharmacol. 2019 Jan;95(1):43-61. doi: 10.1124/mol.118.113340. Epub 2018 Oct 22.

PMID:
30348894
4.

The novel peripherally active cannabinoid type 1 and serotonin type 3 receptor agonist AM9405 inhibits gastrointestinal motility and reduces abdominal pain in mouse models mimicking irritable bowel syndrome.

Salaga M, Binienda A, Tichkule RB, Thakur GA, Makriyannis A, Storr M, Fichna J.

Eur J Pharmacol. 2018 Oct 5;836:34-43. doi: 10.1016/j.ejphar.2018.08.016. Epub 2018 Aug 17.

PMID:
30121173
5.

PSD95 and nNOS interaction as a novel molecular target to modulate conditioned fear: relevance to PTSD.

Li LP, Dustrude ET, Haulcomb MM, Abreu AR, Fitz SD, Johnson PL, Thakur GA, Molosh AI, Lai Y, Shekhar A.

Transl Psychiatry. 2018 Aug 14;8(1):155. doi: 10.1038/s41398-018-0208-5.

6.

Hydrogen sulfide inhibits Kir2 and Kir3 channels by decreasing sensitivity to the phospholipid phosphatidylinositol 4,5-bisphosphate (PIP2).

Ha J, Xu Y, Kawano T, Hendon T, Baki L, Garai S, Papapetropoulos A, Thakur GA, Plant LD, Logothetis DE.

J Biol Chem. 2018 Mar 9;293(10):3546-3561. doi: 10.1074/jbc.RA117.001679. Epub 2018 Jan 9.

PMID:
29317494
7.

Cannabinoid Receptor 1 Positive Allosteric Modulators for Posttraumatic Stress Disorder.

Shekhar A, Thakur GA.

Neuropsychopharmacology. 2018 Jan;43(1):226-227. doi: 10.1038/npp.2017.230. No abstract available.

8.

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.

PMID:
29158048
9.

Positive Allosteric Modulation of Cannabinoid Receptor Type 1 Suppresses Pathological Pain Without Producing Tolerance or Dependence.

Slivicki RA, Xu Z, Kulkarni PM, Pertwee RG, Mackie K, Thakur GA, Hohmann AG.

Biol Psychiatry. 2018 Nov 15;84(10):722-733. doi: 10.1016/j.biopsych.2017.06.032. Epub 2017 Jul 8.

10.

Design and Synthesis of Cannabinoid 1 Receptor (CB1R) Allosteric Modulators: Drug Discovery Applications.

Kulkarni AR, Garai S, Janero DR, Thakur GA.

Methods Enzymol. 2017;593:281-315. doi: 10.1016/bs.mie.2017.06.018. Epub 2017 Jul 14.

PMID:
28750808
11.

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.

12.

The interaction between alpha 7 nicotinic acetylcholine receptor and nuclear peroxisome proliferator-activated receptor-α represents a new antinociceptive signaling pathway in mice.

Donvito G, Bagdas D, Toma W, Rahimpour E, Jackson A, Meade JA, AlSharari S, Kulkarni AR, Ivy Carroll F, Lichtman AH, Papke RL, Thakur GA, Imad Damaj M.

Exp Neurol. 2017 Sep;295:194-201. doi: 10.1016/j.expneurol.2017.06.014. Epub 2017 Jun 9.

13.

Persistent activation of α7 nicotinic ACh receptors associated with stable induction of different desensitized states.

Papke RL, Stokes C, Damaj MI, Thakur GA, Manther K, Treinin M, Bagdas D, Kulkarni AR, Horenstein NA.

Br J Pharmacol. 2018 Jun;175(11):1838-1854. doi: 10.1111/bph.13851. Epub 2017 Jun 8.

PMID:
28477386
14.

Small molecule inhibitors of PSD95-nNOS protein-protein interactions suppress formalin-evoked Fos protein expression and nociceptive behavior in rats.

Carey LM, Lee WH, Gutierrez T, Kulkarni PM, Thakur GA, Lai YY, Hohmann AG.

Neuroscience. 2017 May 4;349:303-317. doi: 10.1016/j.neuroscience.2017.02.055. Epub 2017 Mar 8.

15.

Human Cannabinoid Receptor 2 Ligand-Interaction Motif: Transmembrane Helix 2 Cysteine, C2.59(89), as Determinant of Classical Cannabinoid Agonist Activity and Binding Pose.

Zhou H, Peng Y, Halikhedkar A, Fan P, Janero DR, Thakur GA, Mercier RW, Sun X, Ma X, Makriyannis A.

ACS Chem Neurosci. 2017 Jun 21;8(6):1338-1347. doi: 10.1021/acschemneuro.7b00003. Epub 2017 Mar 1.

PMID:
28220706
16.

Enantiospecific Allosteric Modulation of Cannabinoid 1 Receptor.

Laprairie RB, Kulkarni PM, Deschamps JR, Kelly MEM, Janero DR, Cascio MG, Stevenson LA, Pertwee RG, Kenakin TP, Denovan-Wright EM, Thakur GA.

ACS Chem Neurosci. 2017 Jun 21;8(6):1188-1203. doi: 10.1021/acschemneuro.6b00310. Epub 2017 Feb 7.

PMID:
28103441
17.

Scalable, One-Pot, Microwave-Accelerated Tandem Synthesis of Unsymmetrical Urea Derivatives.

Kulkarni AR, Garai S, Thakur GA.

J Org Chem. 2017 Jan 20;82(2):992-999. doi: 10.1021/acs.joc.6b02521. Epub 2016 Dec 30.

PMID:
27966953
18.

Leveraging allostery to improve G protein-coupled receptor (GPCR)-directed therapeutics: cannabinoid receptor 1 as discovery target.

Janero DR, Thakur GA.

Expert Opin Drug Discov. 2016 Dec;11(12):1223-1237. Epub 2016 Oct 21. Review.

19.

A high efficacy cannabinergic ligand (AM4054) used as a discriminative stimulus: Generalization to other adamantyl analogs and Δ(9)-THC in rats.

Järbe TU, LeMay BJ, Thakur GA, Makriyannis A.

Pharmacol Biochem Behav. 2016 Sep;148:46-52. doi: 10.1016/j.pbb.2016.06.001. Epub 2016 Jun 2.

20.

The α7 nicotinic receptor dual allosteric agonist and positive allosteric modulator GAT107 reverses nociception in mouse models of inflammatory and neuropathic pain.

Bagdas D, Wilkerson JL, Kulkarni A, Toma W, AlSharari S, Gul Z, Lichtman AH, Papke RL, Thakur GA, Damaj MI.

Br J Pharmacol. 2016 Aug;173(16):2506-20. doi: 10.1111/bph.13528. Epub 2016 Jul 18.

21.

Tolerance to the Diuretic Effects of Cannabinoids and Cross-Tolerance to a κ-Opioid Agonist in THC-Treated Mice.

Chopda GR, Parge V, Thakur GA, Gatley SJ, Makriyannis A, Paronis CA.

J Pharmacol Exp Ther. 2016 Aug;358(2):334-41. doi: 10.1124/jpet.116.232132. Epub 2016 May 26.

22.

Mapping Cannabinoid 1 Receptor Allosteric Site(s): Critical Molecular Determinant and Signaling Profile of GAT100, a Novel, Potent, and Irreversibly Binding Probe.

Laprairie RB, Kulkarni AR, Kulkarni PM, Hurst DP, Lynch D, Reggio PH, Janero DR, Pertwee RG, Stevenson LA, Kelly ME, Denovan-Wright EM, Thakur GA.

ACS Chem Neurosci. 2016 Jun 15;7(6):776-98. doi: 10.1021/acschemneuro.6b00041. Epub 2016 Apr 25.

23.

Source memory in rats is impaired by an NMDA receptor antagonist but not by PSD95-nNOS protein-protein interaction inhibitors.

Smith AE, Xu Z, Lai YY, Kulkarni PM, Thakur GA, Hohmann AG, Crystal JD.

Behav Brain Res. 2016 May 15;305:23-9. doi: 10.1016/j.bbr.2016.02.021. Epub 2016 Feb 22.

24.

Critical Molecular Determinants of α7 Nicotinic Acetylcholine Receptor Allosteric Activation: SEPARATION OF DIRECT ALLOSTERIC ACTIVATION AND POSITIVE ALLOSTERIC MODULATION.

Horenstein NA, Papke RL, Kulkarni AR, Chaturbhuj GU, Stokes C, Manther K, Thakur GA.

J Biol Chem. 2016 Mar 4;291(10):5049-67. doi: 10.1074/jbc.M115.692392. Epub 2016 Jan 7.

25.

Novel Electrophilic and Photoaffinity Covalent Probes for Mapping the Cannabinoid 1 Receptor Allosteric Site(s).

Kulkarni PM, Kulkarni AR, Korde A, Tichkule RB, Laprairie RB, Denovan-Wright EM, Zhou H, Janero DR, Zvonok N, Makriyannis A, Cascio MG, Pertwee RG, Thakur GA.

J Med Chem. 2016 Jan 14;59(1):44-60. doi: 10.1021/acs.jmedchem.5b01303. Epub 2015 Nov 28.

26.

In vitro and non-invasive in vivo effects of the cannabinoid-1 receptor agonist AM841 on gastrointestinal motor function in the rat.

Abalo R, Chen C, Vera G, Fichna J, Thakur GA, López-Pérez AE, Makriyannis A, Martín-Fontelles MI, Storr M.

Neurogastroenterol Motil. 2015 Dec;27(12):1721-35. doi: 10.1111/nmo.12668. Epub 2015 Sep 20.

27.

Small molecule inhibitors of PSD95-nNOS protein-protein interactions as novel analgesics.

Lee WH, Xu Z, Ashpole NM, Hudmon A, Kulkarni PM, Thakur GA, Lai YY, Hohmann AG.

Neuropharmacology. 2015 Oct;97:464-75. doi: 10.1016/j.neuropharm.2015.05.038. Epub 2015 Jun 10.

28.

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.

29.

The analgesic-like properties of the alpha7 nAChR silent agonist NS6740 is associated with non-conducting conformations of the receptor.

Papke RL, Bagdas D, Kulkarni AR, Gould T, AlSharari SD, Thakur GA, Damaj MI.

Neuropharmacology. 2015 Apr;91:34-42. doi: 10.1016/j.neuropharm.2014.12.002. Epub 2014 Dec 11.

30.

Probing the carboxyester side chain in controlled deactivation (-)-δ(8)-tetrahydrocannabinols.

Nikas SP, Sharma R, Paronis CA, Kulkarni S, Thakur GA, Hurst D, Wood JT, Gifford RS, Rajarshi G, Liu Y, Raghav JG, Guo JJ, Järbe TU, Reggio PH, Bergman J, Makriyannis A.

J Med Chem. 2015 Jan 22;58(2):665-81. doi: 10.1021/jm501165d. Epub 2014 Dec 16.

31.

Cannabinoids alleviate experimentally induced intestinal inflammation by acting at central and peripheral receptors.

Fichna J, Bawa M, Thakur GA, Tichkule R, Makriyannis A, McCafferty DM, Sharkey KA, Storr M.

PLoS One. 2014 Oct 2;9(10):e109115. doi: 10.1371/journal.pone.0109115. eCollection 2014.

32.

Parental psychopathology in families of children with attention-deficit/hyperactivity disorder and exposed to maternal smoking during pregnancy.

Sengupta SM, Fortier MÈ, Thakur GA, Bhat V, Grizenko N, Joober R.

J Child Psychol Psychiatry. 2015 Feb;56(2):122-9. doi: 10.1111/jcpp.12286. Epub 2014 Jun 24.

PMID:
24961295
33.

Prophylactic cannabinoid administration blocks the development of paclitaxel-induced neuropathic nociception during analgesic treatment and following cessation of drug delivery.

Rahn EJ, Deng L, Thakur GA, Vemuri K, Zvonok AM, Lai YY, Makriyannis A, Hohmann AG.

Mol Pain. 2014 Apr 18;10:27. doi: 10.1186/1744-8069-10-27.

34.

In-vivo pharmacological evaluation of the CB1-receptor allosteric modulator Org-27569.

Gamage TF, Ignatowska-Jankowska BM, Wiley JL, Abdelrahman M, Trembleau L, Greig IR, Thakur GA, Tichkule R, Poklis J, Ross RA, Pertwee RG, Lichtman AH.

Behav Pharmacol. 2014 Apr;25(2):182-5. doi: 10.1097/FBP.0000000000000027.

35.
36.

The activity of GAT107, an allosteric activator and positive modulator of α7 nicotinic acetylcholine receptors (nAChR), is regulated by aromatic amino acids that span the subunit interface.

Papke RL, Horenstein NA, Kulkarni AR, Stokes C, Corrie LW, Maeng CY, Thakur GA.

J Biol Chem. 2014 Feb 14;289(7):4515-31. doi: 10.1074/jbc.M113.524603. Epub 2013 Dec 20.

37.

Controlled-deactivation cannabinergic ligands.

Sharma R, Nikas SP, Paronis CA, Wood JT, Halikhedkar A, Guo JJ, Thakur GA, Kulkarni S, Benchama O, Raghav JG, Gifford RS, Järbe TU, Bergman J, Makriyannis A.

J Med Chem. 2013 Dec 27;56(24):10142-57. doi: 10.1021/jm4016075. Epub 2013 Dec 10.

38.

Diuretic effects of cannabinoid agonists in mice.

Chopda GR, Vemuri VK, Sharma R, Thakur GA, Makriyannis A, Paronis CA.

Eur J Pharmacol. 2013 Dec 5;721(1-3):64-9. doi: 10.1016/j.ejphar.2013.09.053. Epub 2013 Oct 5.

39.

Effects of a novel CB1 agonist on visual attention in male rats: role of strategy and expectancy in task accuracy.

Miller RL, Thakur GA, Stewart WN, Bow JP, Bajaj S, Makriyannis A, McLaughlin PJ.

Exp Clin Psychopharmacol. 2013 Oct;21(5):416-25. doi: 10.1037/a0033668.

41.

Novel adamantyl cannabinoids as CB1 receptor probes.

Thakur GA, Bajaj S, Paronis C, Peng Y, Bowman AL, Barak LS, Caron MG, Parrish D, Deschamps JR, Makriyannis A.

J Med Chem. 2013 May 23;56(10):3904-21. doi: 10.1021/jm4000775. Epub 2013 May 14.

42.

Behavioral effects of the novel potent cannabinoid CB1 agonist AM 4054.

McLaughlin PJ, Thakur GA, Vemuri VK, McClure ED, Brown CM, Winston KM, Wood JT, Makriyannis A, Salamone JD.

Pharmacol Biochem Behav. 2013 Aug;109:16-22. doi: 10.1016/j.pbb.2013.04.011. Epub 2013 Apr 19.

43.

Association between obesity-related gene FTO and ADHD.

Choudhry Z, Sengupta SM, Grizenko N, Thakur GA, Fortier ME, Schmitz N, Joober R.

Obesity (Silver Spring). 2013 Dec;21(12):E738-44. doi: 10.1002/oby.20444. Epub 2013 Jun 13.

44.

Selected rapporteur summaries from the XX World Congress of Psychiatric Genetics, Hamburg, Germany, October 14-18, 2012.

Anderson-Schmidt H, Beltcheva O, Brandon MD, Byrne EM, Diehl EJ, Duncan L, Gonzalez SD, Hannon E, Kantojärvi K, Karagiannidis I, Kos MZ, Kotyuk E, Laufer BI, Mantha K, McGregor NW, Meier S, Nieratschker V, Spiers H, Squassina A, Thakur GA, Tiwari Y, Viswanath B, Way MJ, Wong CC, O'Shea A, DeLisi LE.

Am J Med Genet B Neuropsychiatr Genet. 2013 Mar;162B(2):96-121. doi: 10.1002/ajmg.b.32132. Epub 2013 Jan 22.

45.

Cannabinoid discrimination and antagonism by CB(1) neutral and inverse agonist antagonists.

Kangas BD, Delatte MS, Vemuri VK, Thakur GA, Nikas SP, Subramanian KV, Shukla VG, Makriyannis A, Bergman J.

J Pharmacol Exp Ther. 2013 Mar;344(3):561-7. doi: 10.1124/jpet.112.201962. Epub 2013 Jan 3.

47.

Analysis of tolerance and behavioral/physical dependence during chronic CB1 agonist treatment: effects of CB1 agonists, antagonists, and noncannabinoid drugs.

Desai RI, Thakur GA, Vemuri VK, Bajaj S, Makriyannis A, Bergman J.

J Pharmacol Exp Ther. 2013 Feb;344(2):319-28. doi: 10.1124/jpet.112.198374. Epub 2012 Nov 29.

48.

Comprehensive phenotype/genotype analyses of the norepinephrine transporter gene (SLC6A2) in ADHD: relation to maternal smoking during pregnancy.

Thakur GA, Sengupta SM, Grizenko N, Choudhry Z, Joober R.

PLoS One. 2012;7(11):e49616. doi: 10.1371/journal.pone.0049616. Epub 2012 Nov 20.

49.

Family-based association study of ADHD and genes increasing the risk for smoking behaviours.

Thakur GA, Sengupta SM, Grizenko N, Choudhry Z, Joober R.

Arch Dis Child. 2012 Dec;97(12):1027-33. doi: 10.1136/archdischild-2012-301882. Epub 2012 Oct 29.

PMID:
23109089
50.

Diuretic effects of cannabinoids.

Paronis CA, Thakur GA, Bajaj S, Nikas SP, Vemuri VK, Makriyannis A, Bergman J.

J Pharmacol Exp Ther. 2013 Jan;344(1):8-14. doi: 10.1124/jpet.112.199331. Epub 2012 Sep 27.

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