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Page 1
From High-Throughput Screening to Target Validation: Benzo[d]isothiazoles as Potent and Selective Agonists of Human Transient Receptor Potential Cation Channel Subfamily M Member 5 Possessing In Vivo Gastrointestinal Prokinetic Activity in Rodents.
Barilli A, Aldegheri L, Bianchi F, Brault L, Brodbeck D, Castelletti L, Feriani A, Lingard I, Myers R, Nola S, Piccoli L, Pompilio D, Raveglia LF, Salvagno C, Tassini S, Virginio C, Sabat M. Barilli A, et al. Among authors: castelletti l. J Med Chem. 2021 May 13;64(9):5931-5955. doi: 10.1021/acs.jmedchem.1c00065. Epub 2021 Apr 23. J Med Chem. 2021. PMID: 33890770
1,2,4-Triazolyl octahydropyrrolo[2,3-b]pyrroles: A new series of potent and selective dopamine D3 receptor antagonists.
Micheli F, Bernardelli A, Bianchi F, Braggio S, Castelletti L, Cavallini P, Cavanni P, Cremonesi S, Dal Cin M, Feriani A, Oliosi B, Semeraro T, Tarsi L, Tomelleri S, Wong A, Visentini F, Zonzini L, Heidbreder C. Micheli F, et al. Among authors: castelletti l. Bioorg Med Chem. 2016 Apr 15;24(8):1619-36. doi: 10.1016/j.bmc.2016.02.031. Epub 2016 Feb 27. Bioorg Med Chem. 2016. PMID: 26951894
1,2,4-Triazolyl 5-Azaspiro[2.4]heptanes: Lead Identification and Early Lead Optimization of a New Series of Potent and Selective Dopamine D3 Receptor Antagonists.
Micheli F, Bacchi A, Braggio S, Castelletti L, Cavallini P, Cavanni P, Cremonesi S, Dal Cin M, Feriani A, Gehanne S, Kajbaf M, Marchió L, Nola S, Oliosi B, Pellacani A, Perdonà E, Sava A, Semeraro T, Tarsi L, Tomelleri S, Wong A, Visentini F, Zonzini L, Heidbreder C. Micheli F, et al. Among authors: castelletti l. J Med Chem. 2016 Sep 22;59(18):8549-76. doi: 10.1021/acs.jmedchem.6b00972. Epub 2016 Sep 9. J Med Chem. 2016. PMID: 27564135
Stable expression and functional characterization of a human nicotinic acetylcholine receptor with α6β2 properties: discovery of selective antagonists.
Capelli AM, Castelletti L, Chen YH, Van der Keyl H, Pucci L, Oliosi B, Salvagno C, Bertani B, Gotti C, Powell A, Mugnaini M. Capelli AM, et al. Among authors: castelletti l. Br J Pharmacol. 2011 May;163(2):313-29. doi: 10.1111/j.1476-5381.2011.01213.x. Br J Pharmacol. 2011. PMID: 21232042 Free PMC article.
Development of novel multipotent compounds modulating endocannabinoid and dopaminergic systems.
Grillo A, Chemi G, Brogi S, Brindisi M, Relitti N, Fezza F, Fazio D, Castelletti L, Perdona E, Wong A, Lamponi S, Pecorelli A, Benedusi M, Fantacci M, Valoti M, Valacchi G, Micheli F, Novellino E, Campiani G, Butini S, Maccarrone M, Gemma S. Grillo A, et al. Among authors: castelletti l. Eur J Med Chem. 2019 Dec 1;183:111674. doi: 10.1016/j.ejmech.2019.111674. Epub 2019 Sep 4. Eur J Med Chem. 2019. PMID: 31518969
Identification of a series of 1,3,4-oxadiazol-2-amines as potent alpha-7 agonists with efficacy in the novel object recognition model of cognition.
Skidmore J, Atcha Z, Boucherat E, Castelletti L, Chen DW, Coppo FT, Cutler L, Dunsdon RM, Heath BM, Hutchings R, Hurst DN, Javed S, Martin S, Maskell ES, Norton D, Pemberton DJ, Redshaw S, Rutter R, Sehmi SS, Scoccitti T, Temple HE, Theobald P, Ward RW, Wilson DM. Skidmore J, et al. Among authors: castelletti l. Bioorg Med Chem Lett. 2012 May 15;22(10):3560-3. doi: 10.1016/j.bmcl.2012.03.040. Epub 2012 Mar 16. Bioorg Med Chem Lett. 2012. PMID: 22503248
The discovery of 2-fluoro-N-(3-fluoro-4-(5-((4-morpholinobutyl)amino)-1,3,4-oxadiazol-2-yl)phenyl)benzamide, a full agonist of the alpha-7 nicotinic acetylcholine receptor showing efficacy in the novel object recognition model of cognition enhancement.
Skidmore J, Atcha Z, Boucherat E, Castelletti L, Chen DW, Coppo FT, Cutler L, Dunsdon RM, Heath BM, Hutchings R, Hurst DN, Javed S, Martin S, Maskell ES, Norton D, Pemberton DJ, Redshaw S, Rutter R, Sehmi SS, Scoccitti T, Temple HE, Theobald P, Ward RW, Wilson DM. Skidmore J, et al. Among authors: castelletti l. Bioorg Med Chem Lett. 2012 May 15;22(10):3531-4. doi: 10.1016/j.bmcl.2012.03.062. Epub 2012 Mar 21. Bioorg Med Chem Lett. 2012. PMID: 22503453
62 results