Search results for "choline"

The influence of long-term dietary choline deficiency on choline metabolites in the rat brain

1996

Platelet membrane fluidity and platelet membrane lipid pattern in essential hypertension

1995

In a group of subjects with essential hypertension platelets were studied in resting conditions: platelet membrane fluidity was measured with the fluorescent probe 1.4-(trimethylamino)-phenyl-4-phenylhexatriene (TMA-DPH), platelet membrane cholesterol/phospholipid ratio was evaluated separating the membrane lipids with column chromatography, and platelet membrane individual phospholipids were determined using two-dimensional thin-layer chromatography. From the obtained results, it is evident that platelet membrane fluidity does not differentiate normals from hypertensives; platelet membrane cholesterol/phospholipid ratio is increased in hypertensives, while of the platelet membrane individu…

Chapter 23: Choline, a precursor of acetylcholine and phospholipids in the brain

1993

Publisher Summary The plasma level of free choline is remarkably constant at about 10 pM in animals and human. Ingestion of food, especially when rich in choline or lecithin, transiently elevates the plasma choline level up to 20 pM or more. In contrast, choline-deficient diet leads to a reduction of the plasma level by about 50%. Choline is considered an essential nutrient, which is predominantly supplied as phosphatidylcholine (lecithin). For a long time, neuroscientists have been intrigued by the fact that choline is a precursor for the biosynthesis of both acetylcholine (ACh) and phospholipids. For 50 years, lecithin has been marketed in Europe as a drug that was claimed to prevent exha…

1012 – Evaluation of a risk-scale for anticholinergic side-effects in elderly psychiatric inpatients

2013

Introduction Many commonly prescribed drugs have anticholinergic properties which can induce side-effects e.g. delirium, especially in an ageing brain with increased sensitivity. Risk-assessment before starting therapy may prevent such sideeffects. Objectives We rated anticholinergic pharmacological properties of prescribed medication and compared the theoretical risk with side-effects in clinical practice. Aims The scale should improve the safety of pharmacotherapy in gerontopsychiatry. Methods Based on five publications that considered anticholinergic properties of drugs, a risk-scale was established. Riskpoints for all drugs were summarized to a total score. Patients were selected from T…

Preclinical progress with CHF2819, a novel orally active acetylcholinesterase inhibitor

2002

(-)-(3aS,8aS,1S)-1,2,3,3a,8,8a-hexahydro-1,3a,8-trimethylpyrrolo[2,3-b]indol-5-ol-2′-ethylphenylcarbamate N-oxide hydrochloride (CHF2819) is a novel, orally active acetylcholinesterase inhibitor (AChEI) for Alzheimer's disease (AD). CHF2819 appears as a selective inhibitor of AChE, being 115 times more potent against this enzyme than butyrylcholinesterase (BuChE). Moreover, CHF2819 appears more selective for inhibiting central (brain) than peripheral (heart) AChE. In vivo studies show that CHF2819 significantly increases acetylcholine (ACh) levels in young adult rat hippocampus in a dose-dependent manner. Moreover, aged animals exhibit a marked increase in hippocampal concentrations of this…

Effects of indomethacin on muscarinic inhibition of endogenous noradrenaline release from rat isolated trachea

1993

The release of endogenous noradrenaline from rat isolated tracheae was evoked by electrical field stimulation (3 Hz, 540 pulses) in the presence of yohimbine, desipramine and tyrosine. The muscarine receptor agonist oxotremorine concentration-dependently inhibited the evoked release of noradrenaline by 95% at 1 μmol/l, EC50 values in two series of experiments 41 and 57 nmol/l, respectively. The effect of oxotremorine was antagonized by the non-selective muscarine receptor antagonist scopolamine (10–1000 nmol/l) in a manner suggesting a simple competitive interaction (slope of Schild plot −0.94; pA2 value 8.88). However, the M2 selective muscarine receptor antagonist methoctramine (0.1–10 μm…

CHF2819: Pharmacological profile of a novel acetylcholinesterase inhibitor

2002

CHF2819 is a novel orally active acetylcholinesterase inhibitor (AChEI) developed for the treatment of Alzheimer's disease (AD). CHF2819 is a selective inhibitor of AChE, it is 115 times more potent against this enzyme than against butyrylcholinesterase (BuChE). Moreover, CHF2819 is more selective for inhibition of central (brain) AChE than peripheral (heart) AChE. In vivo CHF2819, 0.5, 1.5, and 4.5 mg/kg p.o., significantly and in dose-dependent manner increased acetylcholine (ACh) levels in hippocampus of young adult rats. Moreover, aging animals, with lower basal ACh levels than young adult rats, also exhibit a marked increase in hippocampal levels of this neurotransmitter after administ…

<p>Future perspectives of anticholinergics for the treatment of asthma in adults and children</p>

2019

Despite major advances in therapeutic interventions and the availability of detailed treatment guidelines, a high proportion of patients with symptomatic asthma remain uncontrolled. Asthma management is largely guided by the Global Initiative for Asthma (GINA) strategy and is based on a backbone of inhaled corticosteroid (ICS) therapy with the use of additional therapies to achieve disease control. Inhaled long-acting bronchodilators alone and in combination are the preferred add-on treatment options. Although long-acting muscarinic antagonists (LAMAs) are a relatively recent addition to disease management recommendations for asthma, tiotropium has been extensively studied in a large clinic…

Psychotropic Effect of Combined Estrogen-Vit B6 Treatment in Endogenously Depressed Females

1985

Estrogens are among the most commonly prescribed substances in females. Also endogenous estrogen levels change dramatically throughout life and this biological variable has been associated with several psychological signs like premenstrual tension syndrome and depression in older age. Along with clinical practice there is increasing evidence from neuropharmacology suggesting a psychotropic action of estrogens (review: Holsboer, 1982). The most prominent findings are: 1. Reduction of monoamine-oxidase (MAO)-activity by estrogens (McEwen et al., 1978); 2. Competitive inhibition of catechol-o-methyltransferase by 2-hydroxyestrogens, which are major metabolites of estrogens in the CNS (Breuer e…

Gender-Specific Metabolomics Approach to Kidney Cancer

2021

Renal cell carcinoma (RCC) is the most common form of kidney malignancy. RCC is more common among men with a 2/1 male/female incidence ratio worldwide. Given the underlying epidemiological differences in the RCC incidence between males and females, we explored the gender specific 1H NMR serum metabolic profiles of RCC patients and their matched controls. A number of differential metabolites were shared by male and female RCC patients. These RCC specific changes included lower lactate, threonine, histidine, and choline levels together with increased levels of pyruvate, N-acetylated glycoproteins, beta-hydroxybutyrate, acetoacetate, and lysine. Additionally, serum lactate/pyruvate ratio was a…