Synthesis of three alpha 7 agonists in labeled form

Autor: Rebecca Urbanek, J. Richard Heys, Peter N. Dorff, Timothy Blake, Scott W. Landvatter, James E. Hall, Charles S. Elmore, Mark E. Powell, Glen Ernst, John R. Harding, David A. Killick

Publikováno v: Journal of Labelled Compounds and Radiopharmaceuticals. 57:342-349

In support of a program to develop an alpha 7 agonist as a treatment for Alzheimer's disease, three drug candidates, 1, 2, and 3, were prepared in labeled forms. Compound 1 was prepared in C-14 labeled form by lithiation of [2,6-(14)C2]2-chloropyridi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::7178167c29bdf609d358c8677882b90a
https://doi.org/10.1002/jlcr.3186

Synthesis of a delta opioid agonist in [2H6], [2H4], [11C], and [14C] labeled forms

Autor: Cathy Dantzman, William E. Palmer, Peter N. Dorff, Charles S. Elmore, Christer Halldin, Valerie Hoesch, Kelly Brush, Magnus Schou, Thomas J. Hudzik, James E. Hall, Mark E. Powell

Publikováno v: Journal of Labelled Compounds and Radiopharmaceuticals. 54:847-854

In support of a program to develop a treatment for depression, four labeled forms of a delta opioid agonist were prepared. The [2H4] labeled form was prepared using a relatively straightforward conversion of [2H4]bromoethanol to [2H4]N-methyl-2-hydro

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::f4000e2278af836e8c0e84d179c0758d
https://doi.org/10.1002/jlcr.1939

Synthesis of the NK3 receptor antagonist AZD2624 in C-14-, H-3- and C-13-labeled forms

Autor: Thomas R. Simpson, Mark E. Powell, Peter N. Dorff, James E. Hall, Charles S. Elmore

Publikováno v: Journal of Labelled Compounds and Radiopharmaceuticals. 54:239-246

In support of a program to develop an antipsychotic treatment for schizophrenia, three labeled forms of the NK3 receptor antagonist AZD2624 have been prepared. [3H2]AZD2624 was synthesized by tritiodehalogenation for use in receptor occupancy and aut

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::5b1d3f8fe8dbeb88ee413ce2e1315970
https://doi.org/10.1002/jlcr.1858

In vitroassessment of metabolic drug–drug interaction potential of AZD2624, neurokinin-3 receptor antagonist, through cytochrome P450enzyme identification, inhibition, and induction studies

Autor: Yan Li, Stephen S. Ferguson, Diansong Zhou, Scott W. Grimm, Peter N. Dorff, Thomas R. Simpson

Publikováno v: Xenobiotica. 40:721-729

AZD2624 was pharmacologically characterized as a NK3 receptor antagonist intended for treatment of schizophrenia. The metabolic drug-drug interaction potential of AZD2624 was evaluated in in vitro studies. CYP3A4 and CYP3A5 appeared to be the primary

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f94c3b658572532b421de8d09dd0d4c8
https://doi.org/10.3109/00498254.2010.512670

Synthesis of 6-acrylamido-4-(2-[18F]fluoroanilino)quinazoline: a prospective irreversible EGFR binding probe

Autor: Leanne M. Reid, Neil Vasdev, Peter N. Dorff, James P. O'Neil, Henry F. VanBrocklin, Erathodiyil Nandanan, Andrew R. Gibbs

Publikováno v: Vasdev, Neil; Dorff, Peter N.; Gibbs, Andrew R.; Nandanan, Erathodiyil; Reid, Leanne M.; O'Neil, James P.; et al.(2004). Synthesis of 6-acrylamido-4-(2-[18F]fluoroanilino)quinazoline: A prospective irreversible EGFR binding probe. Lawrence Berkeley National Laboratory. Lawrence Berkeley National Laboratory: Lawrence Berkeley National Laboratory. Retrieved from: http://www.escholarship.org/uc/item/21z2c9sv

Acrylamido-quinazolines substituted at the 6-position bind irreversibly to the intracellular ATP binding domain of the epidermal growth factor receptor (EGFR). A general route was developed for preparing 6-substituted-4-anilinoquinazolines from [18F]

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f17c1a85d45cc943f6be4f1e2a910ea1
https://doi.org/10.1002/jlcr.903