Search results for "galant"

Controlled Iontophoretic Delivery in Vitro and in Vivo of ARN14140—A Multitarget Compound for Alzheimer’s Disease

2019

ARN14140 is a galantamine-memantine conjugate that acts upon both cholinergic and glutamatergic pathways for better management of Alzheimer's disease. Poor oral bioavailability and pharmacokinetics meant that earlier preclinical in vivo studies employed intracerebroventricular injection to administer ARN14140 directly to the brain. The aim of the present study was to evaluate the feasibility of using constant current transdermal iontophoresis for the noninvasive systemic delivery of ARN14140 and to quantify the amounts present in the blood and the brain. Preliminary experiments in vitro were performed using porcine skin and validated with human skin. Cumulative ARN14140 permeation across th…

Glycoprotein and ganglioside changes in human trophoblasts after exposure to pulsed doppler ultrasound

1995

Changes in glycoprotein and ganglioside composition in human trophoblasts (eighth week of gestation) after in vitro exposure to pulsed Doppler ultrasound (pulse duration 1.22 microseconds; repetition frequency 11.1 kHz; center frequency 4 MHz; ISPPA = 175.5 W/cm2; ISPTA = 0.59 W/cm2) were investigated. Evacuated trophoblasts were divided in two halves and insonated for 10 min on top of a 6-cm layer of 5% gelatin in 50-mL tubes (Falcon) at 37 degrees C. One half of each trophoblast was sham insonated and served as an internal control. After insonation trophoblasts were maintained at 37 degrees C for 24 h. Glycoproteins were detected using alpha-D-mannose specific lectins from Galanthus nival…

Histoire de Madame de Mucie : une épouse de parlementaire dijonnais héroïne de roman galant

2017

International audience

Evaluation of Galantamine transbuccal absorption by reconstituted human oral epithelium and porcine tissue as buccal mucosa models: Part I

2008

Over the last decade, interest in delivering drugs through buccal mucosa has increased. As a major limitation in buccal drug delivery could be the low permeability of the epithelium, the aim of this study was to evaluate the aptitude of galantamine, useful in Alzheimer's disease, to penetrate the buccal mucosa. The evaluation of the ability of galantamine to permeate through the buccal epithelium was investigated using two permeation models. Firstly, in vitro permeation experiments were carried out using reconstituted human oral non-keratinised epithelium and Transwell diffusion cells system. Results were validated by ex vivo experiments using porcine buccal mucosa as membrane and Franz typ…

Galantamine delivery on buccal mucosa: permeation enhancement and design of matrix tablets

2009

The most important feature in transbuccal drug delivery is the low drug passage through the buccal mucosa. In our previous work we demonstrated the aptitude of Galantamine to penetrate the buccal tissue. The collected data suggested that Galantamine passively crosses the membrane, but the calculated Js and Kp values showed that the drug amount that crosses the membrane wasn’t sufficient to assure blood therapeutic level. So, in this study, ex vivo permeation tests, using porcine buccal mucosa, were performed in presence of physical or chemical enhancers. No significant differences in penetration rate were observed using chemical enhancers as sodium dehydrocholate, EDTA disodium salt and tri…

Genetic diversity in five populations of Galanthus from Sicily using isozymes

2009

Le “plaisir sucré” de la duchesse : un point sur la production du « galant de Madame » à la fin du Moyen Âge. https://preo.u-bourgogne.fr/crescentis/…

2021

Among the range of products elaborated in the Dukes of Burgundy vineyards at the end of the Middle Ages, the galant is first quoted in 1383. This paper strives to shed new light upon the sources in which the galant appears, i.e. the accountability documentation of the Dukes’ vineyards. Our research focuses on two demesnes located near Dijon: Talant and Chenôve.The study of this rare product (2-4% of total production), which was certainly flavored with gentian, shows that the notion of fortified wine should be reconsidered for the 14th and 15th centuries. The galant was obtained only by heating white grape must in a cauldron, searching to reach a diminution of one- or two-thirds of the basic…

Allosteric modulation of nicotinic receptors as a treatment strategy for Alzheimer's disease.

2000

Impairment of the central cholinergic system has a pivotal role in the cognitive decline observed in patients with Alzheimer’s disease (AD). One of the most prominent cholinergic deficits is the reduced number of nicotinic acetylcholine receptors (nAChR) in the brain. Since these receptors are important for memory and learning, enhancing nicotinic neurotransmission is a promising treatment strategy for AD. The two most common approaches to correcting these cholinergic deficits are to increase the synaptic availability of acetylcholine (ACh) by inhibiting acetylcholinesterase (AChE), or to mimic the effects of ACh (nicotinic agonists) by acting directly on nicotinic receptors. Clinical studi…

Unconventional ligands and modulators of nicotinic receptors

2002

Evidence gathered from epidemiologic and behavioral studies have indicated that neuronal nicotinic receptors (nAChRs) are intimately involved in the pathogenesis of a number of neurologic disorders, including Alzheimer's disease, Parkinson's disease, and schizophrenia. In the mammalian brain, neuronal nAChRs, in addition to mediating fast synaptic transmission, modulate fast synaptic transmission mediated by the major excitatory and inhibitory neurotransmitters glutamate and GABA, respectively. Of major interest, however, is the fact that the activity of the different subtypes of neuronal nAChR is also subject to modulation by substances of endogenous origin such as choline, the tryptophan …

Galantamine is an allosterically potentiating ligand of neuronal nicotinic but not of muscarinic acetylcholine receptors.

2003

Galantamine (Reminyl), an approved treatment for Alzheimer's disease (AD), is a potent allosteric potentiating ligand (APL) of human alpha 3 beta 4, alpha 4 beta 2, and alpha 6 beta 4 nicotinic receptors (nAChRs), and of the chicken/mouse chimeric alpha 7/5-hydroxytryptamine3 receptor, as was shown by whole-cell patch-clamp studies of human embryonic kidney-293 cells stably expressing a single nAChR subtype. Galantamine potentiates agonist responses of the four nAChR subtypes studied in the same window of concentrations (i.e., 0.1-1 microM), which correlates with the cerebrospinal fluid concentration of the drug at the recommended daily dosage of 16 to 24 mg. At concentrations10 microM, gal…