Approved and marketed drugs are frequently studied in nonclinical models to evaluate the
potential application to additional disease indications or to gain insight about molecular …

Cholinesterase inhibitors vary in their selectivity for acetylcholinesterase versus
butyrylcholinesterase. We examined several cholinesterase inhibitors and assessed the relative role …

Clozapine was studied in functional assays at human muscarinic M 1 −M 5 receptors
expressed in Chinese hamster ovary cells. Clozapine was a full agonist at the muscarinic M 4 …

A series of iV-benzylpiperidine benzisoxazoles has been developed as potent and selective
inhibitors of the enzyme acetylcholinesterase (AChE). The benzisoxazole heterocycle was …

PF-3084014 [(S)-2-((S)-5,7-difluoro-1,2,3,4-tetrahydronaphthalen-3-ylamino)-N-(1-(2-methyl-1-(neopentylamino)propan-2-yl)-1H-imidazol-4-yl)pentanamide]
is a novel γ-secretase …

9-Amino-1,2,3,4-tetrahydroacridine (THA) has been reported to cause improvement in patients
with senile dementia of the Alzheimer's type. We have examined some effects of THA in …

0.33±0.09 nM. Derivatives 2a-d and 10 displayed weak in vitroinhibition of butyryl-cholinesterase
(BuChE) with IC50S= 600-23 000 nM. The most selective compound was 2a with a …

Herein is described the synthesis and structure-activity relationship of a novel series of
aromatic and heteroaromatic 3-(l-benzyl-4-piperidinyl) propan-l-one derivatives that display …

A novel series of tetralin containing amino imidazoles, derived from modification of the
corresponding phenyl acetic acid derivatives is described. Replacement of the amide led to …

The primary sequence of adrenal proenkephalin has recently been reported by three
groups 1–3 who have isolated and sequenced the cDNA for this prohormone. Several …