Influence of tacrine on dopamine-induced reactions of the gastric
smooth muscle of rats

Turijski, V.; Krustev, A.; Getova-Spassova, D.; Spassov, V.

doi:10.1358/mf.2004.26.2.800062

Cited by 2 publications

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“…Tacrine is a more potent inhibitor of BChE than AChE [37]. In addition to the acetylcholine concentration, tacrine increases the extraneuronal concentration of noradrenaline and dopamine [38]. In addition, tacrine affects the glutamate-induced excitotoxicity, causes the induction of a neuroprotective AChE isoform and a reduction in oxidative stress-induced effects [39].…”

Section: Anticholinesterase Drugsmentioning

confidence: 99%

Electrochemical Acetylcholinesterase Sensors for Anti-Alzheimer’s Disease Drug Determination

Ivanov,

Shamagsumova,

Larina

et al. 2024

Biosensors

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Neurodegenerative diseases and Alzheimer’s disease (AD), as one of the most common causes of dementia, result in progressive losses of cholinergic neurons and a reduction in the presynaptic markers of the cholinergic system. These consequences can be compensated by the inhibition of acetylcholinesterase (AChE) followed by a decrease in the rate of acetylcholine hydrolysis. For this reason, anticholinesterase drugs with reversible inhibition effects are applied for the administration of neurodegenerative diseases. Their overdosage, variation in efficiency and recommendation of an individual daily dose require simple and reliable measurement devices capable of the assessment of the drug concentration in biological fluids and medications. In this review, the performance of electrochemical biosensors utilizing immobilized cholinesterases is considered to show their advantages and drawbacks in the determination of anticholinesterase drugs. In addition, common drugs applied in treating neurodegenerative diseases are briefly characterized. The immobilization of enzymes, nature of the signal recorded and its dependence on the transducer modification are considered and the analytical characteristics of appropriate biosensors are summarized for donepezil, huperzine A, rivastigmine, eserine and galantamine as common anti-dementia drugs. Finally, the prospects for the application of AChE-based biosensors in clinical practice are discussed.

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Section: Anticholinesterase Drugsmentioning

confidence: 99%

Electrochemical Acetylcholinesterase Sensors for Anti-Alzheimer’s Disease Drug Determination

Ivanov,

Shamagsumova,

Larina

et al. 2024

Biosensors

View full text Add to dashboard Cite

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Calcium-independent tacrine-induced relaxation of rat gastric corpus smooth muscles

Krustev

Argirova

Getova

et al. 2006

Can. J. Physiol. Pharmacol.

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Tacrine, a non-competitive reversible acetylcholinesterase and butyrylcholineserase inhibitor, caused a concentration-dependent tonic contraction of gastric smooth muscle preparations in the concentration range 1 x 10(-7) mol/L - 1 x 10(-5) mol/L, whereas concentrations higher than 2 x 10(-5) mol/L induced a biphasic effect; a short-time contraction was followed by a prolonged relaxation. To shed some light on the mechanism underlying this untypical relaxation, the amplitude of mechanical reactions caused by tacrine were compared with those of tacrine in the presence of atropine, ipratropium, metrifonate, TTX, nifedipine, D-600, caffeine, apamin, and charybdotoxin. The results obtained revealed that the relaxation was neither cholinergic in nature, nor mediated by the influence of the drug on intramural neuronal structures. It was not influenced by processes inducing changes in cytosolic Ca2+ levels. This assumption was confirmed by experiments with permeabilized muscle preparations that were pre-contracted in a solution with pCa 5.5. Tacrine relaxed the smooth muscles in spite of the constant intracellular Ca2+ concentration resulting from the permeabilization. These findings argue that tacrine at concentrations higher than 2 x 10(-5) mol/L has a desensitizing effect on the contractile apparatus of gastric corpus smooth muscle preparations towards Ca2+.

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Influence of tacrine on dopamine-induced reactions of the gastric smooth muscle of rats

Cited by 2 publications

References 0 publications

Electrochemical Acetylcholinesterase Sensors for Anti-Alzheimer’s Disease Drug Determination

Electrochemical Acetylcholinesterase Sensors for Anti-Alzheimer’s Disease Drug Determination

Calcium-independent tacrine-induced relaxation of rat gastric corpus smooth muscles

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