A novel anticholinesterase THB013: Biochemical and behavioural studies

A. Adem; A. H. Mohammed; B. Winblad; B. E. Henriksson

doi:10.1007/BF02250925

A novel anticholinesterase THB013: Biochemical and behavioural studies

A. Adem, A. H. Mohammed, B. Winblad, B. E. Henriksson

College of Medicine and Health Sciences

Huddinge Hospital

Research output: Contribution to journal › Article › peer-review

5 Scopus citations

Abstract

Clinical trials with tacrine (THA) have resulted in elevations of liver enzymes in Alzheimer patients that showed improvement. In an effort to minimize these side effects several THA analogues were synthesized. These analogues were compared to THA in biochemical as well as behavioural studies. In this study, the biochemical effects of THA and one of these analogs, THB 013, on plasma cholinesterase activity, cholinergic receptors as well as the effect of these drugs on spatial learning in adult rats were examined. THB 013 was, at lower concentration, more efficacious in inhibiting plasma cholinesterase as well as blocking the scopolamine induced disruption of spatial learning when administered 10 min before the scopolamine injection. It is possible that THB 013 with more potent cholinergic effects than THA might be useful in the treatment of Alzheimer's disease.

Original language	British English
Pages (from-to)	139-148
Number of pages	10
Journal	Journal of Neural Transmission - Parkinson's Disease and Dementia Section
Volume	8
Issue number	1-2
DOIs	https://doi.org/10.1007/BF02250925
State	Published - Feb 1994

Keywords

acetylcholine release
Alzheimer's disease
cholinergic
cholinesterases
muscarinic
spatial learning
tacrine
tacrine analogues
THB 013

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10.1007/BF02250925

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title = "A novel anticholinesterase THB013: Biochemical and behavioural studies",

abstract = "Clinical trials with tacrine (THA) have resulted in elevations of liver enzymes in Alzheimer patients that showed improvement. In an effort to minimize these side effects several THA analogues were synthesized. These analogues were compared to THA in biochemical as well as behavioural studies. In this study, the biochemical effects of THA and one of these analogs, THB 013, on plasma cholinesterase activity, cholinergic receptors as well as the effect of these drugs on spatial learning in adult rats were examined. THB 013 was, at lower concentration, more efficacious in inhibiting plasma cholinesterase as well as blocking the scopolamine induced disruption of spatial learning when administered 10 min before the scopolamine injection. It is possible that THB 013 with more potent cholinergic effects than THA might be useful in the treatment of Alzheimer's disease.",

keywords = "acetylcholine release, Alzheimer's disease, cholinergic, cholinesterases, muscarinic, spatial learning, tacrine, tacrine analogues, THB 013",

author = "A. Adem and Mohammed, {A. H.} and B. Winblad and Henriksson, {B. E.}",

year = "1994",

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T2 - Biochemical and behavioural studies

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AU - Mohammed, A. H.

AU - Winblad, B.

AU - Henriksson, B. E.

PY - 1994/2

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AB - Clinical trials with tacrine (THA) have resulted in elevations of liver enzymes in Alzheimer patients that showed improvement. In an effort to minimize these side effects several THA analogues were synthesized. These analogues were compared to THA in biochemical as well as behavioural studies. In this study, the biochemical effects of THA and one of these analogs, THB 013, on plasma cholinesterase activity, cholinergic receptors as well as the effect of these drugs on spatial learning in adult rats were examined. THB 013 was, at lower concentration, more efficacious in inhibiting plasma cholinesterase as well as blocking the scopolamine induced disruption of spatial learning when administered 10 min before the scopolamine injection. It is possible that THB 013 with more potent cholinergic effects than THA might be useful in the treatment of Alzheimer's disease.

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KW - cholinergic

KW - cholinesterases

KW - muscarinic

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KW - tacrine analogues

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A novel anticholinesterase THB013: Biochemical and behavioural studies

Abstract

Keywords

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