Zobrazeno 1 - 10
of 56
pro vyhledávání: '"Benzatropine"'
Publikováno v:
International Journal of Pharmaceutics. 357:55-60
Benztropine (BZ) is a potent muscarinic receptor antagonist that has been used for the treatment of Parkinson disease. However, the oral administration of BZ is often limited because of its many dose-related side effects. In this study, BZ was formul
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c56f7527a65ac4d23b5264c8d54af45b
https://doi.org/10.1016/j.ijpharm.2008.01.024
https://doi.org/10.1016/j.ijpharm.2008.01.024
Publikováno v:
Journal of Pharmaceutical Sciences. 97:1993-2007
A second generation of N-substituted 3alpha-[bis(4'-fluorophenyl)methoxy]-tropanes (GA 1-69, JHW 005 and JHW 013) binds with high affinity to the dopamine transporter (DAT) and are highly selective toward DAT compared to muscarinic receptor binding (
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::60a701b71c45f3e92e07aee6ebf4e25d
https://doi.org/10.1002/jps.21123
https://doi.org/10.1002/jps.21123
Publikováno v:
Biochemical Pharmacology. 75:2-16
The discovery and development of medications to treat addiction and notably, cocaine addiction, have been frustrated by both the complexity of the disorder and the lack of target validation in human subjects. The dopamine transporter has historically
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::79f60af901c03e75554ec280a07cdc6e
https://doi.org/10.1016/j.bcp.2007.08.007
https://doi.org/10.1016/j.bcp.2007.08.007
Autor:
Jianjing Cao, Jonathan L. Katz, Natalie D. Eddington, Sangeeta Raje, Jennifer Cornish, Amy Hauck Newman
Publikováno v:
Biopharmaceutics & Drug Disposition. 27:229-240
PURPOSE AHN 1-055, a benztropine (BZT) analog, binds with high affinity to the dopamine transporter (DAT), possesses behavioral, pharmacokinetic (PK) and brain microdialysate dopamine (DA) profiles distinct from cocaine. Accordingly, the objectives o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::09887be2c6687f6506ebe51febc30547
https://doi.org/10.1002/bdd.497
https://doi.org/10.1002/bdd.497
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:5419-5423
A series of N-8-substituted benztropinamines was synthesized and evaluated for binding at the dopamine (DAT), serotonin (SERT), norepinephrine (NET) transporters, and muscarinic M1 receptors. In general, the isosteric replacement of the C-3 benzhydro
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::42994db55dfc7363f9d5aa8a683f39a5
https://doi.org/10.1016/j.bmcl.2005.08.111
https://doi.org/10.1016/j.bmcl.2005.08.111
Publikováno v:
Annals of Emergency Medicine. 38:689-693
A 33-year-old man with a history of recreational benztropine abuse presented to the emergency department with confusion, abdominal pain, and distention. An abdominal radiograph revealed gross fecal loading. He was initially treated with intravenous f
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::167df7886749b134ad6e3d5ec2f72cb6
https://doi.org/10.1067/mem.2001.119458
https://doi.org/10.1067/mem.2001.119458
Publikováno v:
American Journal of Psychiatry. 158:918-925
Aberrant cholinergic inputs and synaptic neurotransmission in the prefrontal cortex induce cognitive impairment, which is a central feature of schizophrenia. Postsynaptic excitatory muscarinic cholinergic M(1) and M(4) receptors are the major cholino
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a87cc6a374b3d662458cb10273563c8f
https://doi.org/10.1176/appi.ajp.158.6.918
https://doi.org/10.1176/appi.ajp.158.6.918
Autor:
Michael J. Forster, Theresa A. Kopajtic, William L. Woolverton, Kenneth L. Alling, Gregory E. Agoston, Jonathan L. Katz, Richard H. Kline, Amy Hauck Newman
Publikováno v:
Psychopharmacology. 154:362-374
Rationale: Previous SAR studies demonstrated that small halogen substitutions on the diphenylether system of benztropine (BZT), such as a para-Cl group, retained high affinity at the cocaine binding site on the dopamine transporter. Despite this high
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::aa373569123e871c351cf293ca723be2
https://doi.org/10.1007/s002130000667
https://doi.org/10.1007/s002130000667
Autor:
Gerald S. Hecht, Gregory E. Agoston, William L. Woolverton, Jonathan L. Katz, Amy Hauck Newman
Publikováno v:
Psychopharmacology. 154:375-382
Rationale: Several halogenated analogs of benztropine (BZT) have previously been characterized as potent DA uptake inhibitors with behavioral profiles that indicate diminished psychomotor stimulant effects relative to cocaine. In a previous study usi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3e4a41308536dcbe0cac30475b00b644
https://doi.org/10.1007/s002130000616
https://doi.org/10.1007/s002130000616
Autor:
Daniele Simoni, Stefania Gessi, Riccardo Rondanin, Riccardo Baruchello, Pier Andrea Borea, Sabrina Cavallini, Marinella Roberti, Stefania Merighi, Silvia Marino, Francesco Paolo Invidiata, Clementina Bianchi, Anna Siniscalchi, Katia Varani, Marcello Rossi
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 11:823-827
6-Methoxylated and 8-oxygenated benztropines were prepared and evaluated for their DAT and SERT activity (binding and uptake inhibition). Methoxylation at the two-carbon bridge of benztropine produced a novel class of potent and selective DAT ligands
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::089f8947768377a82b54cac6d42f7822
https://doi.org/10.1016/s0960-894x(01)00068-3
https://doi.org/10.1016/s0960-894x(01)00068-3