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Calcitonin gene-related peptide (CGRP) receptor antagonists: pyridine as a replacement for a core amide group.
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In our continuing efforts to identify CGRP receptor antagonists that can be dosed orally for the treatment of migraine headache, we have investigated a pyridine bioisosteric replacement of a polar amide portion of a previous lead compound, BMS-694153. Pyridine derivatives were discovered and their
Olfactory sensitivity in medical laboratory workers occupationally exposed to organic solvent mixtures.
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BACKGROUND
Published epidemiological information relating the effects of occupational exposure to organic solvents (OS) to olfaction is limited.
OBJECTIVE
The objectives of this pilot study were to measure the chemosensory abilities of medical laboratory employees occupationally exposed to OS
Food effect on the oral bioavailability of Manidipine: single dose, randomized, crossover study in healthy male subjects.
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The effect of food on the oral bioavailability of a manidipine 20 mg tablet was studied after a single administration in 12 male healthy subjects. The clinical trial was conducted as an open, randomised, crossover study. In two different administration sessions, the subjects received a 20 mg
Results of a meta-analysis comparing the tolerability of lercanidipine and other dihydropyridine calcium channel blockers.
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BACKGROUND
Results from clinical studies suggest that the dihydropyridine calcium channel blocker (CCB) lercanidipine may be associated with a lower incidence of peripheral edema than are older dihydro-pyridine CCBs.
OBJECTIVE
The objective of the present study was to conduct a meta-analysis of
Oral absorption profile of nitrendipine in healthy subjects: a kinetic and dynamic study.
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1. In nine healthy male subjects the kinetics of nitrendipine were assessed after i.v. administration and its absorption profile was studied when given by a tablet formulation and by an osmotic pumping device (Osmet) with a zero-order in vitro release of 2.62 +/- 0.19 mg h-1 for 13 h. 2. Plasma
Characterization of the calcitonin gene-related peptide receptor antagonist telcagepant (MK-0974) in human isolated coronary arteries.
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The sensory neuropeptide calcitonin gene-related peptide (CGRP) plays a role in primary headaches, and CGRP receptor antagonists are effective in migraine treatment. CGRP is a potent vasodilator, raising the possibility that antagonism of its receptor could have cardiovascular effects. We therefore
Olfaction in migraineurs.
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Many investigators have described olfactory dysfunction among migraineurs. Olfactory stimuli can precipitate migraine, and olfactory hallucinations can occur as auras of migraines or as part of the symptom complex. Despite many reports linking olfactory phenomena and migraine, no evaluations of the
In vivo quantification of calcitonin gene-related peptide receptor occupancy by telcagepant in rhesus monkey and human brain using the positron emission tomography tracer [11C]MK-4232.
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Calcitonin gene-related peptide (CGRP) is a potent neuropeptide whose agonist interaction with the CGRP receptor (CGRP-R) in the periphery promotes vasodilation, neurogenic inflammation and trigeminovascular sensory activation. This process is implicated in the cause of migraine headaches, and
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