Search results for "Cholinergic"
showing 10 items of 251 documents
Behavioral deficits induced by lead exposure are accompanied by serotonergic and cholinergic alterations in the prefrontal cortex
2013
The effects of long-term lead (Pb) exposure producing a blood Pb concentration of lower than 20 μg/dL, i.e. below that associated with overt neurological deficits in occupationally exposed individuals, was studied in adult rats. In order to assess gender differences, we performed parallel behavioral experiments in male and female rats. Exposure to Pb acetate (50 ppm in drinking water) for 6 months induced motor and cognitive alterations, however these effects were gender- and task-dependent. Chronic lead exposure impaired spatial learning assessed in the Morris water maze test (MWM) in both genders, whereas it only induced hyperactivity in the open field and impaired motor coordination in t…
Adrenoceptor- and cholinoceptor-mediated mechanisms in the regulation of 5-hydroxytryptamine release from isolated tracheae of newborn rabbits
1996
Abstract 1. Isolated tracheae of newborn rabbits were incubated in vitro and the outflow of 5-hydroxytryptamine (5-HT) was determined by h.p.l.c. with electrochemical detection. Evidence has previously been provided that this 5-HT outflow derives from neuroendocrine epithelial (NEE) cells of the airway mucosa. 2. Phenylephrine (1, 10 and 30 microM) enhanced the outflow of 5-HT by 80, 290 and 205%, respectively. 5-HT outflow evoked by 10 microM phenylephrine was not affected by the presence of the neurotoxin tetrodotoxin (1 microM). 3. Rauwolscine, ARC 239 (an alpha(2B)-adrenoceptor preferring antagonist), yohimbine and prazosin antagonized the effect of 10 microM phenylephrine in a concentr…
Modulation of hippocampal theta oscillations and spatial memory by relaxin-3 neurons of the nucleus incertus.
2009
Hippocampal theta rhythm is thought to underlie learning and memory, and it is well established that “pacemaker” neurons in medial septum (MS) modulate theta activity. Recent studies in the rat demonstrated that brainstem-generated theta rhythm occurs through a multisynaptic pathway via the nucleus incertus (NI), which is the primary source of the neuropeptide relaxin-3 (RLN3). Therefore, this study examined the possible contribution of RLN3 to MS activity, and associated hippocampal theta activity and spatial memory. In anesthetized and conscious rats, we identified the ability of intraseptal RLN3 signaling to modulate neuronal activity in the MS and hippocampus and promote hippocampal the…
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…
Cellular expression of α4 subunit mRNA of the nicotinic acetylcholine receptor in the developing rat telencephalon
1995
By contrast to adult brain, little is known on the development of nicotinic acetylcholine receptor (nAChR) expression. Using a digoxigenin-labeled riboprobe for in situ hybridization, alpha 4 nAChR subunit mRNA expression was studied in embryonic and postnatal rat neocortex and hippocampus where it was transiently increased in neuronal subpopulations and preceded cholinergic fiber ingrowth. alpha 4 expression was increased in neocortical layer VIb between E20 and P2 and, about birth, in dentate gyrus granule cells subsequently decreasing to adult levels. nAChR mRNA expression is increased at the developing neuromuscular endplate preceding cholinergic innervation which triggers changes in no…
Regioisomeric 5(3)-aminomethyl-3(5)-phenylisoxazoles: synthesis, spectroscopic discrimination, and muscarinic activity.
1995
The regioselective synthesis of isomeric 5(3)-aminomethyl-3(5)-phenyl isoxazoles using different methods is described. Spectroscopic data, especially mass spectrometric fragmentation, were used to identify and characterize the regioisomers. The muscarinic activity of these isoxazoles was assayed on isolated guinea-pig ileum and atria as well as on isolated rabbit vas deferens. Regioisomere 5(3)-Aminomethyl-3(5)-phenyl-isoxazole: Synthese, spektroskopische Unterscheidung und muskarinische Aktivitat Es werden verschiedene Verfahren zur regioselektiven Darstellung von 5(3)-Aminomethyl-3(5)-phenyl-isoxazolen beschrieben, die anhand ihrer spektroskopischen Daten, insbesondere der massenspektrosk…
Lung function and long-term safety of tiotropium/olodaterol in East Asian patients with chronic obstructive pulmonary disease
2017
Background and purpose While the efficacy and safety of combined tiotropium and olodaterol in patients with COPD was established in a large clinical trial program, it is important to assess whether clinical data can be applied to geographic patient groups, particularly for East Asian patients who may have a different phenotypic profile to the global trial population. This study aimed to compare the lung function and safety profiles of tiotropium/olodaterol and monocomponents in East Asian and global populations from the TONADO® trials. Materials and methods In the replicate, double-blind, parallel-group, active-controlled, randomized, 52-week, Phase III TONADO studies, patients received tio…
Role of cholinergic neurons in the motor effects of glucagon-like peptide-2 in mouse colon
2010
Glucagon-like peptide-2 (GLP-2) reduces mouse gastric tone and small intestine transit, but its action on large intestine motility is still unknown. The purposes of the present study were 1) to examine the influence of GLP-2 on spontaneous mechanical activity and on neurally evoked responses, by recording intraluminal pressure from mouse isolated colonic segments; 2) to characterize GLP-2 mechanism of action; and 3) to determine the distribution of GLP-2 receptor (GLP-2R) in the mouse colonic muscle coat by immunohistochemistry. Exogenous GLP-2 (0.1–300 nM) induced a concentration-dependent reduction of the spontaneous mechanical activity, which was abolished by the desensitization of GLP-…
Evaluation of antidiuretic hormone before and after long-term treatment with desmopressin in a group of enuretic children
1998
Objective To determine the effect of long-term desmopressin therapy in enuretic patients on the levels of antidiuretic hormone (ADH) during and after the end of therapy. Patients and methods The study comprised 25 outpatients (18 boys and seven girls) aged 8–12 years at the start of therapy and 12–16 years at the end. The morning (08.00 hours) plasma ADH level was determined before treatment (T0) with desmopressin and 2 years after (T1) ending the therapy. Seven of the 25 patients evaluated had monosymptomatic (simple enuresis, SE) and 18 had other symptoms (complex enuresis, CE). Results In the patients with SE, the mean (SD) duration of therapy was 305 (183) days and they were re-evaluate…
Cholinergic and GABAergic regulation of nitric oxide synthesis in the guinea pig ileum.
1999
Nitric oxide (NO) synthesis was examined in intact longitudinal muscle-myenteric plexus preparations of the guinea pig ileum by determining the formation of [3H]citrulline during incubation with [3H]arginine. Spontaneous [3H]citrulline production after 30 min was 80–90 dpm/mg, which constituted ∼1% of the tissue radioactivity. Electrical stimulation (10 Hz) led to a threefold increase in [3H]citrulline formation. Removal of calcium from the medium or addition of N G-nitro-l-arginine strongly inhibited both spontaneous and electrically induced production of [3H]citrulline. TTX reduced the electrically induced but not spontaneous [3H]citrulline formation. The electrically induced formation o…