Parkinsonʼs Disease Monotherapy With Controlled-Release MK-458 (PHNO)

Je, Ahlskog; Muenter,; Pa, Bailey; Pm, Miller

doi:10.1097/00002826-199106000-00004

Cited by 13 publications

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“…Examples of active pharmaceutical ingredients (API) which are currently marketed or under development and have an aminotetraline structural element with chiral substituents include the antidepressants sertraline 1 and (S)-8-OH-DPAT, 2 the anti-Parkinson agent Naxagolide, 3 and the antiplatelet agent Terutroban 4 (Fig. 1).…”

Section: Introductionmentioning

confidence: 99%

Synthesis and configuration determination of all enantiopure stereoisomers of the melatonin receptor ligand4-phenyl-2-propionamidotetralin using an expedient optical resolution of 4-phenyl-2-tetralone

et al. 2012

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An efficient and practical approach for the synthesis of all four stereoisomers of the MT(2) melatonin receptor ligand 4-phenyl-2-propionamidotetralin (4-P-PDOT), each in enantiomerically pure form (ee > 99.9%), was developed. The strategy involved an optical resolution procedure of the key precursor (±)-4-phenyl-2-tetralone with the unusual resolving agent (S)-mandelamide, through the formation of four dihydronaphtalene-spiro-oxazolidin-4-one diastereomers. Interestingly, NMR experimental observations in combination with geometric calculations, provided unambiguous configuration assignments of all stereocenters of the key spiro stereoisomers. Cleavage of each single spiro diastereomer under acidic conditions gave enantiopure (R)- or (S)-4-phenyl-2-tetralone, which were then converted to each 4-P-PDOT single enantiomer by using stereoselective reactions.

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Section: Introductionmentioning

confidence: 99%

Synthesis and configuration determination of all enantiopure stereoisomers of the melatonin receptor ligand4-phenyl-2-propionamidotetralin using an expedient optical resolution of 4-phenyl-2-tetralone

et al. 2012

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Transdermal dopaminergic D₂ receptor agonist therapy in Parkinson's disease with N‐0923 TDS: A double‐blind, placebo‐controlled study

et al. 2001

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N-0923 is a non-ergot, dopaminergic D(2) agonist designed to be transdermally available. It has anti-parkinsonian effects when infused intravenously. An adhesive matrix patch was developed to deliver N-0923 transdermally (N-0923 TDS). In this phase II trial, we evaluated the effectiveness of various doses of N-0923 TDS at replacing levodopa. Eighty-five Parkinson's disease (PD) patients were randomized to placebo or one of four doses of N-0923 TDS for 21 days. Change in daily levodopa dose was the primary efficacy measure. Significantly greater reductions in levodopa dose were achieved as compared to placebo for the two highest doses of N-0923 TDS. Patients treated with 33.5 mg and 67 mg N-0923 TDS decreased levodopa use by 26% and 28%, vs. 7% for placebo. N-0923 TDS was safe and well tolerated.

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Dopamine D1 and D2 receptor interactions in the MPTP-treated marmoset

Elliott

Walsh

1992

Neuroscience Letters

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Parkinsonʼs Disease Monotherapy With Controlled-Release MK-458 (PHNO)

Cited by 13 publications

References 0 publications

Synthesis and configuration determination of all enantiopure stereoisomers of the melatonin receptor ligand4-phenyl-2-propionamidotetralin using an expedient optical resolution of 4-phenyl-2-tetralone

Synthesis and configuration determination of all enantiopure stereoisomers of the melatonin receptor ligand4-phenyl-2-propionamidotetralin using an expedient optical resolution of 4-phenyl-2-tetralone

Transdermal dopaminergic D₂ receptor agonist therapy in Parkinson's disease with N‐0923 TDS: A double‐blind, placebo‐controlled study

Dopamine D1 and D2 receptor interactions in the MPTP-treated marmoset

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Parkinsonʼs Disease Monotherapy With Controlled-Release MK-458 (PHNO)

Cited by 13 publications

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Synthesis and configuration determination of all enantiopure stereoisomers of the melatonin receptor ligand4-phenyl-2-propionamidotetralin using an expedient optical resolution of 4-phenyl-2-tetralone

Synthesis and configuration determination of all enantiopure stereoisomers of the melatonin receptor ligand4-phenyl-2-propionamidotetralin using an expedient optical resolution of 4-phenyl-2-tetralone

Transdermal dopaminergic D2 receptor agonist therapy in Parkinson's disease with N‐0923 TDS: A double‐blind, placebo‐controlled study

Dopamine D1 and D2 receptor interactions in the MPTP-treated marmoset

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Transdermal dopaminergic D₂ receptor agonist therapy in Parkinson's disease with N‐0923 TDS: A double‐blind, placebo‐controlled study