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The Discovery of a Novel Phosphodiesterase (PDE) 4B-Preferring Radioligand for Positron Emission Tomography (PET) Imaging.
Zhang L, Chen L, Beck EM, Chappie TA, Coelho RV, Doran SD, Fan KH, Helal CJ, Humphrey JM, Hughes Z, Kuszpit K, Lachapelle EA, Lazzaro JT, Lee C, Mather RJ, Patel NC, Skaddan MB, Sciabola S, Verhoest PR, Young JM, Zasadny K, Villalobos A. Zhang L, et al. J Med Chem. 2017 Oct 26;60(20):8538-8551. doi: 10.1021/acs.jmedchem.7b01050. Epub 2017 Oct 9. J Med Chem. 2017. PMID: 28957634
First-in-Human Evaluation of 18F-PF-06445974, a PET Radioligand That Preferentially Labels Phosphodiesterase-4B.
Wakabayashi Y, Stenkrona P, Arakawa R, Yan X, Van Buskirk MG, Jenkins MD, Santamaria JAM, Maresca KP, Takano A, Liow JS, Chappie TA, Varrone A, Nag S, Zhang L, Hughes ZA, Schmidt CJ, Doran SD, Mannes A, Zanotti-Fregonara P, Ooms M, Morse CL, Zoghbi SS, Halldin C, Pike VW, Innis RB. Wakabayashi Y, et al. Among authors: hughes za. J Nucl Med. 2022 Dec;63(12):1919-1924. doi: 10.2967/jnumed.122.263838. Epub 2022 Jun 30. J Nucl Med. 2022. PMID: 35772961 Free PMC article.
The synthesis and biological evaluation of quinolyl-piperazinyl piperidines as potent serotonin 5-HT1A antagonists.
Childers WE Jr, Havran LM, Asselin M, Bicksler JJ, Chong DC, Grosu GT, Shen Z, Abou-Gharbia MA, Bach AC 3rd, Harrison BL, Kagan N, Kleintop T, Magolda R, Marathias V, Robichaud AJ, Sabb AL, Zhang MY, Andree TH, Aschmies SH, Beyer C, Comery TA, Day M, Grauer SM, Hughes ZA, Rosenzweig-Lipson S, Platt B, Pulicicchio C, Smith DE, Sukoff-Rizzo SJ, Sullivan KM, Adedoyin A, Huselton C, Hirst WD. Childers WE Jr, et al. Among authors: hughes za. J Med Chem. 2010 May 27;53(10):4066-84. doi: 10.1021/jm1000908. J Med Chem. 2010. PMID: 20443629
Correlating efficacy in rodent cognition models with in vivo 5-hydroxytryptamine1a receptor occupancy by a novel antagonist, (R)-N-(2-methyl-(4-indolyl-1-piperazinyl)ethyl)-N-(2-pyridinyl)-cyclohexane carboxamide (WAY-101405).
Hirst WD, Andree TH, Aschmies S, Childers WE, Comery TA, Dawson LA, Day M, Feingold IB, Grauer SM, Harrison BL, Hughes ZA, Kao J, Kelly MG, van der Lee H, Rosenzweig-Lipson S, Saab AL, Smith DL, Sullivan K, Rizzo SJ, Tio C, Zhang MY, Schechter LE. Hirst WD, et al. Among authors: hughes za. J Pharmacol Exp Ther. 2008 Apr;325(1):134-45. doi: 10.1124/jpet.107.133082. Epub 2008 Jan 8. J Pharmacol Exp Ther. 2008. PMID: 18182558
60 results