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Pharmacologic characterization of JNJ-42226314, [1-(4-fluorophenyl)indol-5-yl]-[3-[4-(thiazole-2-carbonyl)piperazin-1-yl]azetidin-1-yl]methanone, a reversible, selective and potent monoacylglycerol lipase inhibitor.

Wyatt RM, Fraser I, Welty N, Lord B, Wennerholm M, Sutton SW, Ameriks MK, Dugovic C, Yun S, White A, Nguyen L, Koudriakova T, Tian G, Suarez J, Szewczuk L, Bonnette W, Ahn K, Ghosh B, Flores CM, Connolly PJ, Zhu B, Macielag MJ, Brandt MR, Chevalier K, Zhang SP, Lovenberg TW, Bonaventure P.

J Pharmacol Exp Ther. 2019 Dec 9. pii: jpet.119.262139. doi: 10.1124/jpet.119.262139. [Epub ahead of print]


Low-value clinical practices in injury care: A scoping review and expert consultation survey.

Moore L, Lauzier F, Tardif PA, Boukar KM, Farhat I, Archambault P, Mercier É, Lamontagne F, Chassé M, Stelfox HT, Berthelot S, Gabbe B, Lecky F, Yanchar N, Champion H, Kortbeek J, Cameron P, Bonaventure PL, Paquet J, Truchon C, Turgeon AF; Canadian Traumatic brain injury Research Consortium.

J Trauma Acute Care Surg. 2019 Jun;86(6):983-993. doi: 10.1097/TA.0000000000002246.


GPR139 and Dopamine D2 Receptor Co-express in the Same Cells of the Brain and May Functionally Interact.

Wang L, Lee G, Kuei C, Yao X, Harrington A, Bonaventure P, Lovenberg TW, Liu C.

Front Neurosci. 2019 Mar 26;13:281. doi: 10.3389/fnins.2019.00281. eCollection 2019.


In vivo Characterization of a Selective, Orally Available, and Brain Penetrant Small Molecule GPR139 Agonist.

Shoblock JR, Welty N, Fraser I, Wyatt R, Lord B, Lovenberg T, Liu C, Bonaventure P.

Front Pharmacol. 2019 Mar 21;10:273. doi: 10.3389/fphar.2019.00273. eCollection 2019.


In vivo Calcium Imaging Reveals That Cortisol Treatment Reduces the Number of Place Cells in Thy1-GCaMP6f Transgenic Mice.

Indersmitten T, Schachter MJ, Young S, Welty N, Otte S, Nassi JJ, Lovenberg T, Bonaventure P, Wyatt RM.

Front Neurosci. 2019 Mar 1;13:176. doi: 10.3389/fnins.2019.00176. eCollection 2019.


Mutagenesis of GPR139 reveals ways to create gain or loss of function receptors.

Wang L, Lee G, Shih A, Kuei C, Nepomuceno D, Wennerholm M, Fan F, Wu J, Bonaventure P, Lovenberg TW, Liu C.

Pharmacol Res Perspect. 2019 Feb 7;7(1):e00466. doi: 10.1002/prp2.466. eCollection 2019 Feb.


Orexin Depolarizes Central Amygdala Neurons via Orexin Receptor 1, Phospholipase C and Sodium-Calcium Exchanger and Modulates Conditioned Fear.

Dustrude ET, Caliman IF, Bernabe CS, Fitz SD, Grafe LA, Bhatnagar S, Bonaventure P, Johnson PL, Molosh AI, Shekhar A.

Front Neurosci. 2018 Dec 18;12:934. doi: 10.3389/fnins.2018.00934. eCollection 2018.


Utilizing Miniature Fluorescence Microscopy to Image Hippocampal Place Cell Ensemble Function in Thy1.GCaMP6f Transgenic Mice.

Indersmitten T, Berdyyeva T, Aluisio L, Lovenberg T, Bonaventure P, Wyatt RM.

Curr Protoc Pharmacol. 2018 Sep;82(1):e42. doi: 10.1002/cpph.42. Epub 2018 Aug 20.


The Zinc Transporter SLC39A7 (ZIP7) Is Essential for Regulation of Cytosolic Zinc Levels.

Woodruff G, Bouwkamp CG, de Vrij FM, Lovenberg T, Bonaventure P, Kushner SA, Harrington AW.

Mol Pharmacol. 2018 Sep;94(3):1092-1100. doi: 10.1124/mol.118.112557. Epub 2018 Jul 6.


Re-evaluation of Adrenocorticotropic Hormone and Melanocyte Stimulating Hormone Activation of GPR139 in Vitro.

Nepomuceno D, Kuei C, Dvorak C, Lovenberg T, Liu C, Bonaventure P.

Front Pharmacol. 2018 Mar 2;9:157. doi: 10.3389/fphar.2018.00157. eCollection 2018.


Evaluation of JNJ-54717793 a Novel Brain Penetrant Selective Orexin 1 Receptor Antagonist in Two Rat Models of Panic Attack Provocation.

Bonaventure P, Dugovic C, Shireman B, Preville C, Yun S, Lord B, Nepomuceno D, Wennerholm M, Lovenberg T, Carruthers N, Fitz SD, Shekhar A, Johnson PL.

Front Pharmacol. 2017 Jun 9;8:357. doi: 10.3389/fphar.2017.00357. eCollection 2017.


Selective Inhibition of Orexin-2 Receptors Prevents Stress-Induced ACTH Release in Mice.

Yun S, Wennerholm M, Shelton JE, Bonaventure P, Letavic MA, Shireman BT, Lovenberg TW, Dugovic C.

Front Behav Neurosci. 2017 May 8;11:83. doi: 10.3389/fnbeh.2017.00083. eCollection 2017.


4-Methyl-6,7-dihydro-4H-triazolo[4,5-c]pyridine-Based P2X7 Receptor Antagonists: Optimization of Pharmacokinetic Properties Leading to the Identification of a Clinical Candidate.

Letavic MA, Savall BM, Allison BD, Aluisio L, Andres JI, De Angelis M, Ao H, Beauchamp DA, Bonaventure P, Bryant S, Carruthers NI, Ceusters M, Coe KJ, Dvorak CA, Fraser IC, Gelin CF, Koudriakova T, Liang J, Lord B, Lovenberg TW, Otieno MA, Schoetens F, Swanson DM, Wang Q, Wickenden AD, Bhattacharya A.

J Med Chem. 2017 Jun 8;60(11):4559-4572. doi: 10.1021/acs.jmedchem.7b00408. Epub 2017 May 25.


Hospital length of stay following admission for traumatic brain injury in a Canadian integrated trauma system: A retrospective multicenter cohort study.

Tardif PA, Moore L, Boutin A, Dufresne P, Omar M, Bourgeois G, Bonaventure PL, Kuimi BL, Turgeon AF.

Injury. 2017 Jan;48(1):94-100. doi: 10.1016/j.injury.2016.10.042. Epub 2016 Nov 6.


An institutional study of time delays for symptomatic carotid endarterectomy.

Charbonneau P, Bonaventure PL, Drudi LM, Beaudoin N, Blair JF, Elkouri S.

J Vasc Surg. 2016 Dec;64(6):1726-1733. doi: 10.1016/j.jvs.2016.06.100. Epub 2016 Sep 20.


Corrigendum to "Hypothalamic orexin's role in exacerbated cutaneous vasodilation responses to an anxiogenic stimulus in a surgical menopause model" [Psychoneuroendocrinology 65 (2016) 127-137].

Federici LM, Caliman IF, Molosh AI, Fitz SD, Truitt WA, Bonaventure P, Carpenter JS, Shekhar A, Johnson PL.

Psychoneuroendocrinology. 2016 Nov;73:275. doi: 10.1016/j.psyneuen.2016.08.001. Epub 2016 Sep 3. No abstract available.


Managing critically ill patients with severe traumatic brain injury: How should we season the recipe?

Bonaventure PL, Lauzier F, Turgeon AF.

Can J Anaesth. 2016 Jun;63(6):647-51. doi: 10.1007/s12630-016-0635-9. Epub 2016 Apr 4. No abstract available.


Direct Imaging of Hippocampal Epileptiform Calcium Motifs Following Kainic Acid Administration in Freely Behaving Mice.

Berdyyeva TK, Frady EP, Nassi JJ, Aluisio L, Cherkas Y, Otte S, Wyatt RM, Dugovic C, Ghosh KK, Schnitzer MJ, Lovenberg T, Bonaventure P.

Front Neurosci. 2016 Feb 29;10:53. doi: 10.3389/fnins.2016.00053. eCollection 2016.


Hypothalamic orexin's role in exacerbated cutaneous vasodilation responses to an anxiogenic stimulus in a surgical menopause model.

Federici LM, Caliman IF, Molosh AI, Fitz SD, Truitt WA, Bonaventure P, Carpenter JS, Shekhar A, Johnson PL.

Psychoneuroendocrinology. 2016 Mar;65:127-37. doi: 10.1016/j.psyneuen.2015.12.011. Epub 2015 Dec 18.


Substituted 5,6-(Dihydropyrido[3,4-d]pyrimidin-7(8H)-yl)-methanones as P2X7 Antagonists.

Ziff J, Rudolph DA, Stenne B, Koudriakova T, Lord B, Bonaventure P, Lovenberg TW, Carruthers NI, Bhattacharya A, Letavic MA, Shireman BT.

ACS Chem Neurosci. 2016 Apr 20;7(4):498-504. doi: 10.1021/acschemneuro.5b00304. Epub 2016 Jan 19.


Identification and SAR of Glycine Benzamides as Potent Agonists for the GPR139 Receptor.

Dvorak CA, Coate H, Nepomuceno D, Wennerholm M, Kuei C, Lord B, Woody D, Bonaventure P, Liu C, Lovenberg T, Carruthers NI.

ACS Med Chem Lett. 2015 Jul 20;6(9):1015-8. doi: 10.1021/acsmedchemlett.5b00247. eCollection 2015 Sep 10.


A novel radioligand for the ATP-gated ion channel P2X7: [3H] JNJ-54232334.

Lord B, Ameriks MK, Wang Q, Fourgeaud L, Vliegen M, Verluyten W, Haspeslagh P, Carruthers NI, Lovenberg TW, Bonaventure P, Letavic MA, Bhattacharya A.

Eur J Pharmacol. 2015 Oct 15;765:551-9. doi: 10.1016/j.ejphar.2015.09.026. Epub 2015 Sep 18.


Structure and function of the amygdaloid NPY system: NPY Y2 receptors regulate excitatory and inhibitory synaptic transmission in the centromedial amygdala.

Wood J, Verma D, Lach G, Bonaventure P, Herzog H, Sperk G, Tasan RO.

Brain Struct Funct. 2016 Sep;221(7):3373-91. doi: 10.1007/s00429-015-1107-7. Epub 2015 Sep 13.


GPR139, an Orphan Receptor Highly Enriched in the Habenula and Septum, Is Activated by the Essential Amino Acids L-Tryptophan and L-Phenylalanine.

Liu C, Bonaventure P, Lee G, Nepomuceno D, Kuei C, Wu J, Li Q, Joseph V, Sutton SW, Eckert W, Yao X, Yieh L, Dvorak C, Carruthers N, Coate H, Yun S, Dugovic C, Harrington A, Lovenberg TW.

Mol Pharmacol. 2015 Nov;88(5):911-25. doi: 10.1124/mol.115.100412. Epub 2015 Sep 8.



Johnson PL, Federici LM, Fitz SD, Renger JJ, Shireman B, Winrow CJ, Bonaventure P, Shekhar A.

Depress Anxiety. 2015 Sep;32(9):671-83. doi: 10.1002/da.22403. Epub 2015 Aug 19.


NPY Y2 receptors in the central amygdala reduce cued but not contextual fear.

Verma D, Wood J, Lach G, Mietzsch M, Weger S, Heilbronn R, Herzog H, Bonaventure P, Sperk G, Tasan RO.

Neuropharmacology. 2015 Dec;99:665-74. doi: 10.1016/j.neuropharm.2015.08.038. Epub 2015 Aug 24.


Characterization of JNJ-42847922, a Selective Orexin-2 Receptor Antagonist, as a Clinical Candidate for the Treatment of Insomnia.

Bonaventure P, Shelton J, Yun S, Nepomuceno D, Sutton S, Aluisio L, Fraser I, Lord B, Shoblock J, Welty N, Chaplan SR, Aguilar Z, Halter R, Ndifor A, Koudriakova T, Rizzolio M, Letavic M, Carruthers NI, Lovenberg T, Dugovic C.

J Pharmacol Exp Ther. 2015 Sep;354(3):471-82. doi: 10.1124/jpet.115.225466. Epub 2015 Jul 15.


Novel methyl substituted 1-(5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanones are P2X7 antagonists.

Rudolph DA, Alcazar J, Ameriks MK, Anton AB, Ao H, Bonaventure P, Carruthers NI, Chrovian CC, De Angelis M, Lord B, Rech JC, Wang Q, Bhattacharya A, Andres JI, Letavic MA.

Bioorg Med Chem Lett. 2015 Aug 15;25(16):3157-63. doi: 10.1016/j.bmcl.2015.06.004. Epub 2015 Jun 9.


Novel Octahydropyrrolo[3,4-c]pyrroles Are Selective Orexin-2 Antagonists: SAR Leading to a Clinical Candidate.

Letavic MA, Bonaventure P, Carruthers NI, Dugovic C, Koudriakova T, Lord B, Lovenberg TW, Ly KS, Mani NS, Nepomuceno D, Pippel DJ, Rizzolio M, Shelton JE, Shah CR, Shireman BT, Young LK, Yun S.

J Med Chem. 2015 Jul 23;58(14):5620-36. doi: 10.1021/acs.jmedchem.5b00742. Epub 2015 Jul 8.


Novel benzamide-based histamine h3 receptor antagonists: the identification of two candidates for clinical development.

Letavic MA, Aluisio L, Apodaca R, Bajpai M, Barbier AJ, Bonneville A, Bonaventure P, Carruthers NI, Dugovic C, Fraser IC, Kramer ML, Lord B, Lovenberg TW, Li LY, Ly KS, Mcallister H, Mani NS, Morton KL, Ndifor A, Nepomuceno SD, Pandit CR, Sands SB, Shah CR, Shelton JE, Snook SS, Swanson DM, Xiao W.

ACS Med Chem Lett. 2015 Mar 13;6(4):450-4. doi: 10.1021/ml5005156. eCollection 2015 Apr 9.


Selective pharmacological blockade of the 5-HT7 receptor attenuates light and 8-OH-DPAT induced phase shifts of mouse circadian wheel running activity.

Shelton J, Yun S, Losee Olson S, Turek F, Bonaventure P, Dvorak C, Lovenberg T, Dugovic C.

Front Behav Neurosci. 2015 Jan 15;8:453. doi: 10.3389/fnbeh.2014.00453. eCollection 2014.


A selective orexin-1 receptor antagonist attenuates stress-induced hyperarousal without hypnotic effects.

Bonaventure P, Yun S, Johnson PL, Shekhar A, Fitz SD, Shireman BT, Lebold TP, Nepomuceno D, Lord B, Wennerholm M, Shelton J, Carruthers N, Lovenberg T, Dugovic C.

J Pharmacol Exp Ther. 2015 Mar;352(3):590-601. doi: 10.1124/jpet.114.220392. Epub 2015 Jan 12.


Zolpidem reduces hippocampal neuronal activity in freely behaving mice: a large scale calcium imaging study with miniaturized fluorescence microscope.

Berdyyeva T, Otte S, Aluisio L, Ziv Y, Burns LD, Dugovic C, Yun S, Ghosh KK, Schnitzer MJ, Lovenberg T, Bonaventure P.

PLoS One. 2014 Nov 5;9(11):e112068. doi: 10.1371/journal.pone.0112068. eCollection 2014.


Pharmacology of a novel central nervous system-penetrant P2X7 antagonist JNJ-42253432.

Lord B, Aluisio L, Shoblock JR, Neff RA, Varlinskaya EI, Ceusters M, Lovenberg TW, Carruthers N, Bonaventure P, Letavic MA, Deak T, Drinkenburg W, Bhattacharya A.

J Pharmacol Exp Ther. 2014 Dec;351(3):628-41. doi: 10.1124/jpet.114.218487. Epub 2014 Sep 30.


Pharmacological or genetic orexin1 receptor inhibition attenuates MK-801 induced glutamate release in mouse cortex.

Aluisio L, Fraser I, Berdyyeva T, Tryputsen V, Shireman BT, Shoblock J, Lovenberg T, Dugovic C, Bonaventure P.

Front Neurosci. 2014 May 20;8:107. doi: 10.3389/fnins.2014.00107. eCollection 2014.


PET brain imaging of neuropeptide Y2 receptors using N-11C-methyl-JNJ-31020028 in pigs.

Winterdahl M, Audrain H, Landau AM, Smith DF, Bonaventure P, Shoblock JR, Carruthers N, Swanson D, Bender D.

J Nucl Med. 2014 Apr;55(4):635-9. doi: 10.2967/jnumed.113.125351. Epub 2014 Mar 10.


Orexin-1 receptor blockade dysregulates REM sleep in the presence of orexin-2 receptor antagonism.

Dugovic C, Shelton JE, Yun S, Bonaventure P, Shireman BT, Lovenberg TW.

Front Neurosci. 2014 Feb 14;8:28. doi: 10.3389/fnins.2014.00028. eCollection 2014.


Selective orexin receptor antagonists.

Lebold TP, Bonaventure P, Shireman BT.

Bioorg Med Chem Lett. 2013 Sep 1;23(17):4761-9. doi: 10.1016/j.bmcl.2013.06.057. Epub 2013 Jul 4. Review.


Pharmacological characterization of a novel centrally permeable P2X7 receptor antagonist: JNJ-47965567.

Bhattacharya A, Wang Q, Ao H, Shoblock JR, Lord B, Aluisio L, Fraser I, Nepomuceno D, Neff RA, Welty N, Lovenberg TW, Bonaventure P, Wickenden AD, Letavic MA.

Br J Pharmacol. 2013 Oct;170(3):624-40. doi: 10.1111/bph.12314.


Comparison of the ex vivo receptor occupancy profile of ketamine to several NMDA receptor antagonists in mouse hippocampus.

Lord B, Wintmolders C, Langlois X, Nguyen L, Lovenberg T, Bonaventure P.

Eur J Pharmacol. 2013 Sep 5;715(1-3):21-5. doi: 10.1016/j.ejphar.2013.06.028. Epub 2013 Jul 16.


The discovery of potent selective NPY Y(2) antagonists.

Chai W, Wong VD, Nepomuceno D, Bonaventure P, Lovenberg TW, Carruthers NI.

Bioorg Med Chem Lett. 2013 Jul 15;23(14):4141-4. doi: 10.1016/j.bmcl.2013.05.038. Epub 2013 May 22.


Synthesis and Pharmacological Characterization of Two Novel, Brain Penetrating P2X7 Antagonists.

Letavic MA, Lord B, Bischoff F, Hawryluk NA, Pieters S, Rech JC, Sales Z, Velter AI, Ao H, Bonaventure P, Contreras V, Jiang X, Morton KL, Scott B, Wang Q, Wickenden AD, Carruthers NI, Bhattacharya A.

ACS Med Chem Lett. 2013 Mar 12;4(4):419-22. doi: 10.1021/ml400040v. eCollection 2013 Apr 11.


Chronic administration of the Y2 receptor antagonist, JNJ-31020028, induced anti-depressant like-behaviors in olfactory bulbectomized rat.

Morales-Medina JC, Dumont Y, Bonaventure P, Quirion R.

Neuropeptides. 2012 Dec;46(6):329-34. doi: 10.1016/j.npep.2012.09.009. Epub 2012 Oct 25.


Translational evaluation of JNJ-18038683, a 5-hydroxytryptamine type 7 receptor antagonist, on rapid eye movement sleep and in major depressive disorder.

Bonaventure P, Dugovic C, Kramer M, De Boer P, Singh J, Wilson S, Bertelsen K, Di J, Shelton J, Aluisio L, Dvorak L, Fraser I, Lord B, Nepomuceno D, Ahnaou A, Drinkenburg W, Chai W, Dvorak C, Sands S, Carruthers N, Lovenberg TW.

J Pharmacol Exp Ther. 2012 Aug;342(2):429-40. doi: 10.1124/jpet.112.193995. Epub 2012 May 8.


In vitro pharmacological characterization of RXFP3 allosterism: an example of probe dependency.

Alvarez-Jaimes L, Sutton SW, Nepomuceno D, Motley ST, Cik M, Stocking E, Shoblock J, Bonaventure P.

PLoS One. 2012;7(2):e30792. doi: 10.1371/journal.pone.0030792. Epub 2012 Feb 7.


The discovery and synthesis of JNJ 31020028, a small molecule antagonist of the Neuropeptide Y Y₂ receptor.

Swanson DM, Wong VD, Jablonowski JA, Shah C, Rudolph DA, Dvorak CA, Seierstad M, Dvorak LK, Morton K, Nepomuceno D, Atack JR, Bonaventure P, Lovenberg TW, Carruthers NI.

Bioorg Med Chem Lett. 2011 Sep 15;21(18):5552-6. doi: 10.1016/j.bmcl.2011.06.136. Epub 2011 Jul 18.


Pharmacological blockade of serotonin 5-HT₇ receptor reverses working memory deficits in rats by normalizing cortical glutamate neurotransmission.

Bonaventure P, Aluisio L, Shoblock J, Boggs JD, Fraser IC, Lord B, Lovenberg TW, Galici R.

PLoS One. 2011;6(6):e20210. doi: 10.1371/journal.pone.0020210. Epub 2011 Jun 20.


Chimeric, mutant orexin receptors show key interactions between orexin receptors, peptides and antagonists.

Tran DT, Bonaventure P, Hack M, Mirzadegan T, Dvorak C, Letavic M, Carruthers N, Lovenberg T, Sutton SW.

Eur J Pharmacol. 2011 Sep 30;667(1-3):120-8. doi: 10.1016/j.ejphar.2011.05.074. Epub 2011 Jun 12.


Selective blockade of the orexin-2 receptor attenuates ethanol self-administration, place preference, and reinstatement.

Shoblock JR, Welty N, Aluisio L, Fraser I, Motley ST, Morton K, Palmer J, Bonaventure P, Carruthers NI, Lovenberg TW, Boggs J, Galici R.

Psychopharmacology (Berl). 2011 May;215(1):191-203. doi: 10.1007/s00213-010-2127-x. Epub 2010 Dec 22.


Novel tetrahydropyrido[3,2-c]pyrroles as 5-HT(7) antagonists.

Rudolph DA, Dvorak CA, Dvorak L, Nepomuceno D, Bonaventure P, Lovenberg TW, Carruthers NI.

Bioorg Med Chem Lett. 2011 Jan 1;21(1):42-4. doi: 10.1016/j.bmcl.2010.11.078. Epub 2010 Nov 24.


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