Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: EC:3.1.1.8 (cholinesterase)
12,691 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Physostigmine, an acetyl cholinesterase inhibitor, and arecoline, a muscarinic agonist, have been shown to improve Alzheimer presenile dementia in some patients when administered parenterally. Both of these compounds are ineffective orally due to first-pass metabolism. The nasal route was examined as an alternative route of administration for both drugs. Nasal bioavailabilities and dispositions for both drugs were determined in rats. Physostigmine nasal bioavailability was 100% as compared with iv bioavailability, and that of arecoline was 85% when compared with bioavailability following im administration.
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PMID:Intranasal absorption of physostigmine and arecoline. 179 34

Acetylcholinesterase (AChE) in the cerebrospinal fluid (CSF) from patients with Alzheimer-type dementia and control subjects was analyzed by centrifugation on a sucrose density gradient, and by column chromatography on Sephadex G-200. The sedimentation coefficient and molecular weight of CSF AChE were calculated as 10S and 380,000, respectively, which corresponded to those of G4 isozyme in the brain. Other isozymes of AChE were not detected in the CSF of either patients with Alzheimer-type dementia or the controls. Sufficient activity of AChE was observed in the CSF of a patient with familial pseudocholinesterase deficiency, although the pseudocholinesterase activity was not found either in the serum or in the CSF. CSF AChE activity in control subjects increased with advancing age (P less than 0.02). AChE activity in the CSF was significantly lower in patients with presenile dementia (Alzheimer's disease), compared with age-matched control subjects (P less than 0.001). However, AChE activity in the CSF showed a wide variation among patients of Alzheimer-type dementia with a late onset (senile dementia).
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PMID:Acetylcholinesterase activity in cerebrospinal fluid of patients with Alzheimer's disease and senile dementia. 376 Sep 12

Eight patients affected by Alzheimer's Presenile Dementia (AD) received acute administration of physostigmine individual optimal dose per os (n = 4) or subcutaneously (n = 4). The individual physostigmine dose was assessed by means of serum cholinesterase activity monitoring. The possible beneficial effects after treatment were evaluated by using two memory tests: Reys' 15 words and Digit Span from Wechsler memory scale. Although a slight behavioral activation was noted in all patients after treatment, the comparison between mean scores obtained by AD patients in mnesic tests before and after the acute physostigmine administration, with either therapeutic modality, failed to reach the level of statistical significance. Some implications of these disappointing results are briefly discussed.
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PMID:Acute administration of individual optimal dose of physostigmine fails to improve mnesic performances in Alzheimers Presenile Dementia. 684 Sep 79