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Design, synthesis, and evaluation of a novel 4-aminomethyl-4-fluoropiperidine as a T-type Ca2+ channel antagonist.
TLDR
Structural modification of the p Piperidine leads 1 and 2 afforded the fluorinated piperidine ( S)- 5, a potent and selective antagonist that displayed in vivo CNS efficacy without adverse cardiovascular effects.
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Pharmacological evaluation of novel Alzheimer's disease therapeutics: acetylcholinesterase inhibitors related to galanthamine.
TLDR
Because of its composite profile, including duration of action, oral therapeutic index and pharmacokinetics, P11149 is considered the better therapeutic candidate for the treatment of Alzheimer's disease.
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Comparison of the inhibitory potencies of N(G)-methyl-, N(G)-nitro- and N(G)-amino-L-arginine on EDRF function in the rat: evidence for continuous basal EDRF release.
TLDR
It is indicated that L-NNA is a potent antagonist of endothelium-derived relaxing factor formation in vitro and in vivo, and contractile and hypertensive effects of the argininolytic agents clearly demonstrates that a continuous basal release of endotHelium- derived relaxing factor/NO occurs in both isolated vascular rings and whole animals.
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Vascular alpha-1 adrenergic receptor subtypes in the regulation of arterial pressure.
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Vascular alpha 1D-adrenoceptors have a role in the pressor response to phenylephrine in the pithed rat.
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Development of 2-aminooxazoline 3-azaxanthenes as orally efficacious β-secretase inhibitors for the potential treatment of Alzheimer's disease.
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Physiological release of nitric oxide is dependent on the level of vascular tone.
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Discovery of 1,4-substituted piperidines as potent and selective inhibitors of T-type calcium channels.
TLDR
Compound 30 demonstrated a robust reduction in the number and duration of seizures at 33 nM plasma concentration, with no cardiovascular effects at up to 5.6 microM, and is a useful tool for probing the effects of T-type calcium channel inhibition.
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4-Fluorosulfonylpiperidines: selective 5-HT2A ligands for the treatment of insomnia.
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An Orally Available BACE1 Inhibitor That Affords Robust CNS Aβ Reduction without Cardiovascular Liabilities.
TLDR
Further optimization leading to the discovery of inhibitor 15 as an orally available and highly efficacious BACE1 inhibitor that robustly reduces CSF and brain Aβ levels in both rats and nonhuman primates is reported.
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