415704-24-4Relevant academic research and scientific papers
BIOMARKERS RELATED TO PARKINSON'S DISEASE AND METHODS OF USING THE SAME
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Paragraph 0265; 0293, (2021/10/15)
The present disclosure relates to the treatment of Parkinson's disease. The present disclosure provides, in some embodiments, methods of treating Parkinson's disease in a patient in need thereof. In some embodiments, the methods disclosed herein comprise
(S)-ALPHA-FLUOROMETHYLTYROSINE AS DECARBOXYLASE INHIBITORS FOR USE IN THE TREATMENT OF HYPOTENSION
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Paragraph 0159; 0187, (2021/12/31)
Provided are methods of using and drug delivery systems comprising inhibitors of pathogenic, bacterial metabolite production and conjugates of the inhibitors.
DECARBOXYLASE INHIBITORS FOR TREATING PARKINSON'S DISEASE
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Paragraph 0168, (2020/07/04)
Provided are inhibitors of pathogenic, bacterial metabolite production and conjugates of the inhibitors. Also provided are pharmaceutical compositions containing the inhibitors or conjugates and methods of using the same.
INDOLE AHR INHIBITORS AND USES THEREOF
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Paragraph 00683-00684, (2018/11/22)
The present invention provides compounds useful as inhibitors of AHR, compositions thereof, and methods of using the same.
Trace amine-associated receptor agonists: Synthesis and evaluation of thyronamines and related analogues
Hart, Matthew E.,Suchland, Katherine L.,Miyakawa, Motonori,Bunzow, James R.,Grandy, David K.,Scanlan, Thomas S.
, p. 1101 - 1112 (2007/10/03)
We have previously shown that several thyronamines, decarboxylated and deiodinated metabolites of the thyroid hormone, potently activate an orphan G protein-coupled receptor in vitro (TAAR1) and induced hypothermia in vivo on a rapid time scale [Scanlan, T. S.; Suchland, K. L.; Hart, M. E.; Chiellini, G.; Huang, Y.; Kruzich, P. J.; Frascarelli, S.; Crossley, D. A.; Bunzow, J. R.; Ronca-Testoni, S.; Lin, E. T.; Hatton, D.; Zucchi, R.; Grandy, D. K. 3-Iodothyronamine is an endogenous and rapid-acting derivative of thyroid hormone. Nat. Med. 2004, 10 (6), 638-642]. Herein, we report the synthesis of these thyronamines. Additionally, a large number of thyroamine derivatives were synthesized in an effort to understand the molecular basis of TAAR1 activation and hypothermia induction. Several derivatives were found to potently activate both rTAAR1 and mTAAR1 in vitro (compounds 77, 85, 91, and 92). When administered to mice at a 50 mg/kg dose, these derivatives all induced significant hypothermia within 60 min and exhibited a hypothermic induction profile analogous to 3-iodothyronamine (1, T1AM) except 91, which proved to be more efficacious. On the basis of this result, a dose-dependent profile for 91 was generated and an ED50 of 30 μmol/kg was calculated. Compound 91 proved to be more potent than T1AM for TAAR1 activation and exhibits increased potency and efficacy for hypothermia induction. These data further strengthen the pharmacological correlation linking TAAR1 activation by thyronamines and hypothermia induction in mice.
