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Azetidine and Piperidine Carbamates as Efficient, Covalent Inhibitors of Monoacylglycerol Lipase.
Butler CR, Beck EM, Harris A, Huang Z, McAllister LA, Am Ende CW, Fennell K, Foley TL, Fonseca K, Hawrylik SJ, Johnson DS, Knafels JD, Mente S, Noell GS, Pandit J, Phillips TB, Piro JR, Rogers BN, Samad TA, Wang J, Wan S, Brodney MA. Butler CR, et al. Among authors: samad ta. J Med Chem. 2017 Dec 14;60(23):9860-9873. doi: 10.1021/acs.jmedchem.7b01531. Epub 2017 Dec 5. J Med Chem. 2017. PMID: 29148769
Identification and Development of an Irreversible Monoacylglycerol Lipase (MAGL) Positron Emission Tomography (PET) Radioligand with High Specificity.
Zhang L, Butler CR, Maresca KP, Takano A, Nag S, Jia Z, Arakawa R, Piro JR, Samad T, Smith DL, Nason DM, O'Neil S, McAllister L, Schildknegt K, Trapa P, McCarthy TJ, Villalobos A, Halldin C. Zhang L, et al. J Med Chem. 2019 Sep 26;62(18):8532-8543. doi: 10.1021/acs.jmedchem.9b00847. Epub 2019 Sep 16. J Med Chem. 2019. PMID: 31483137
Discovery of Trifluoromethyl Glycol Carbamates as Potent and Selective Covalent Monoacylglycerol Lipase (MAGL) Inhibitors for Treatment of Neuroinflammation.
McAllister LA, Butler CR, Mente S, O'Neil SV, Fonseca KR, Piro JR, Cianfrogna JA, Foley TL, Gilbert AM, Harris AR, Helal CJ, Johnson DS, Montgomery JI, Nason DM, Noell S, Pandit J, Rogers BN, Samad TA, Shaffer CL, da Silva RG, Uccello DP, Webb D, Brodney MA. McAllister LA, et al. Among authors: samad ta. J Med Chem. 2018 Apr 12;61(7):3008-3026. doi: 10.1021/acs.jmedchem.8b00070. Epub 2018 Mar 15. J Med Chem. 2018. PMID: 29498843
Target occupancy study and whole-body dosimetry with a MAGL PET ligand [11C]PF-06809247 in non-human primates.
Arakawa R, Takano A, Nag S, Jia Z, Amini N, Maresca KP, Zhang L, Keliher EJ, Butler CR, Piro JR, Samad TA, Smith D, Nason D, O'Neil S, Trapa P, Fonseca KR, Litchfield J, McCarthy T, Carson RE, Halldin C. Arakawa R, et al. Among authors: samad ta. EJNMMI Res. 2022 Mar 4;12(1):13. doi: 10.1186/s13550-022-00882-2. EJNMMI Res. 2022. PMID: 35244788 Free PMC article.
Monoacylglycerol lipase activity is a critical modulator of the tone and integrity of the endocannabinoid system.
Chanda PK, Gao Y, Mark L, Btesh J, Strassle BW, Lu P, Piesla MJ, Zhang MY, Bingham B, Uveges A, Kowal D, Garbe D, Kouranova EV, Ring RH, Bates B, Pangalos MN, Kennedy JD, Whiteside GT, Samad TA. Chanda PK, et al. Among authors: samad ta. Mol Pharmacol. 2010 Dec;78(6):996-1003. doi: 10.1124/mol.110.068304. Epub 2010 Sep 20. Mol Pharmacol. 2010. PMID: 20855465
Loss of retrograde endocannabinoid signaling and reduced adult neurogenesis in diacylglycerol lipase knock-out mice.
Gao Y, Vasilyev DV, Goncalves MB, Howell FV, Hobbs C, Reisenberg M, Shen R, Zhang MY, Strassle BW, Lu P, Mark L, Piesla MJ, Deng K, Kouranova EV, Ring RH, Whiteside GT, Bates B, Walsh FS, Williams G, Pangalos MN, Samad TA, Doherty P. Gao Y, et al. Among authors: samad ta. J Neurosci. 2010 Feb 10;30(6):2017-24. doi: 10.1523/JNEUROSCI.5693-09.2010. J Neurosci. 2010. PMID: 20147530 Free PMC article.
51 results