Search results for "Convulsants"
showing 10 items of 125 documents
Pharmacological heterogeneity of γ-aminobutyric acid receptors during development suggests distinct classes of rat cerebellar granule cells in situ
2001
The gamma-aminobutyric acid receptor (GABA(A)R) represents a ligand-gated Cl(-)-channel assembling as heteropentamere from 19 known subunits. Cerebellar granule cells contain a unique subset, namely the alpha1-, alpha6-, beta2-, gamma2- and delta-subunits. We studied their GABAergic pharmacology in situ using whole-cell patch-clamp recordings in brain slices and a modified Y-tube application system. The distribution of the EC50s for GABA in young (P8-P14) and medium aged animals (P15-P28) could be fitted with the sum of two Gaussian distributions with means of 60 and 185 microM and 27 and 214 microM, respectively. In older animals (P29-P48) the observed homogeneous range of sensitivities fi…
Evidences of cannabinoids-induced modulation of paroxysmal events in an experimental model of partial epilepsy in the rat.
2009
The anticonvulsant effect of cannabinoids (CB) has been shown to be mediated by the activation of the CB(1) receptor. This study evaluates the anticonvulsant activity of (R)-(+)-[2,3-dihydro-5-methyl-3-(4-morpholinylmethyl) pyrrolo[1,2,3-de]-1,4-benzoxazin-6-Yl]-1-naphthalenylmethanone (WIN55,212-2, CB agonist) alone or preceded by the administration of N-(piperidin-1-yl)-5-(4-iodophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (AM251, selective CB(1) antagonist) in an experimental in vivo model of complex partial seizures (maximal dentate gyrus activation - MDA) in the rat. WIN55,212-2 (21mgkg(-1)) exerted an anticonvulsant effect, significantly reduced by the pre-treatme…
Role of CB2 receptors and cGMP pathway on the cannabinoid-dependent antiepileptic effects in an in vivo model of partial epilepsy.
2014
This study aimed at providing an insight on the possible role of cannabi-noid (CB) type 2 receptors (CB2R) and cGMP pathway in the antiepileptic activity ofWIN 55,212-2, (R)-(+)-[2,3-dihydro-5-methyl-3-(4-morpholinylmethyl) pyrrolo[1,2,3-de]-1,4-benzoxazin-6-Yl]-1-naphthalenylmethanone, a non-selective CB agonist, in the maximal dentate activation (MDA) model of partial epilepsy in adult male rats. We evaluated the activity of a CB2 antagonist/inverse agonist AM630, [6-iodo-2-methyl-1-[2-(4-morpholinyl)ethyl]-1H-indol-3-yl](4-methoxyphenyl)methanone or 6-iodopravadoline, alone or in co-administration with WIN 55,212-2. Also, in the MDA model it was investigated the co-treatment of WIN55,212…
Actions of two GABAA receptor benzodiazepine-site ligands that are mediated via non-γ2-dependent modulation.
2011
The potent sedative-hypnotic zolpidem and the convulsant methyl-6,7-dimethoxy-4-ethyl-β-carboline-3-carboxylate (DMCM) act primarily by binding to the benzodiazepine site of the main inhibitory neurotransmitter receptor, the pentameric γ-aminobutyric acid type A receptor (GABA(A)). This binding depends critically on the wild-type F77 residue of the GABA(A) receptor γ2 subunit. Mice with γ2 subunit F77I point mutation (γ2I77 mouse line) lose the high-affinity nanomolar binding of these ligands as well as their most robust behavioral actions at low doses. Interestingly, the γ2I77 mice offer a tool to study the actions of these substances mediated via other possible binding sites of the GABA(A…
Altered atypical coupling of γ-aminobutyrate type A receptor agonist and convulsant binding sites in subunit-deficient mouse lines
2001
We searched for subunit correlations for GABA(A) receptor-associated atypically GABA-insensitive [35S]TBPS binding. The homomeric beta3 subunit receptors could be excluded, as GABA-insensitive [35S]TBPS binding was present in beta3-/- mice. Localization of GABA-insensitive [35S]TBPS binding correlated best with those of delta, alpha4 and alpha6 subunit mRNAs. The amounts of GABA-insensitive [35S]TBPS binding components were increased in delta-/- mice, but dramatically reduced in alpha6-/- mice, suggesting a role for alpha6 but excluding delta subunits.
Adjunctive Brivaracetam in Older Patients with Focal Seizures: Evidence from the BRIVAracetam add‑on First Italian netwoRk Study (BRIVAFIRST).
2022
BACKGROUND: The management of epilepsy in older adults has become part of daily practice because of an aging population. Older patients with epilepsy represent a distinct and more vulnerable clinical group as compared with younger patients, and they are generally under-represented in randomized placebo-controlled trials. Real-world studies can therefore be a useful complement to characterize the drug's profile. Brivaracetam is a rationally developed compound characterized by high-affinity binding to synaptic vesicle protein 2A and approved as adjunctive therapy for focal seizures in adults with epilepsy. OBJECTIVE: The aim of this study was to assess the 12-month effectiveness and tolerabil…
Determination of phenytoin in plasma by molecularly imprinted solid-phase extraction.
2001
Abstract A molecularly imprinted polymer (MIP) using phenytoin as template and methacrylamide as the functional monomer was prepared. The selectivity was measured by comparing capacity factors of phenytoin and other structurally related compounds. The polymer was evaluated as a selective sorbent in molecularly imprinted solid-phase extraction (MISPE). Several washing solvents were tested to study their ability to disrupt the non-specific interactions occurring between the sample and the polymer matrix and the role of water in the recognition process was also investigated. It was shown that the key step of successful sample extraction is the right choice of the washing solvent. Plasma sample…
Sexual Dysfunction and Mood Stabilizers in Long-Term Stable Patients With Bipolar Disorder.
2020
Abstract Background In addition to factors intrinsic to bipolar disorder (BD), sexual functioning (SF) can be affected by extrinsic causes, such as psychotropic drugs. However, the effect of mood stabilizers on SF and quality of life (QoL) is an underexplored research area. Aim To analyze SF in BD outpatients in euthymia for at least 6 months treated only with mood stabilizers and the association between SF and QoL. Methods A multicenter cross-sectional study was conducted in 114 BD outpatients treated with (i) lithium alone (L group); (ii) anticonvulsants alone (valproate or lamotrigine; A group); (iii) lithium plus anticonvulsants (L+A group); or (iv) lithium plus benzodiazepines (L+B gro…
Panniculitis due to potassium bromide.
1998
Potassium bromide again is well known to be surprisingly effective in patients with severe myoclonic epilepsy in infants (SME). Rare side effects on the skin reappeared, such as the febrile nodular panniculitis (Weber-Christian syndrome). In 1993 we described the first three cases of necrotizing panniculitis and introduced the term 'halogen panniculitis'. It is a systemic disease with crops of subcutaneous nodules, fever, elevated sedimentation rate, hepatosplenomegalia, and abdominal pain. Later severe necrosis of the skin and adipose tissue may happen with deep ulcerations. History and course of five cases, described in this paper, suggest either an allergy or toxic reason. Histologic pic…
Natural Course, Clinical Profile, and Treatment Strategies for Cerebral Cavernous Malformations
2022
A large body of evidence has suggested that the natural biology for symptomatic cerebral cavernous malformations (CCMs) is dynamic. These lesions exhibit a temporal clustering epiphenomenon and usually manifest with multispectral clinical patterns, the most relevant being hemorrhagic and seizurogenic events. Most patients with cerebral cavernous malformations are asymptomatic, and the lesions are detected as incidentalomas. However, association with the CCM3 gene, Zabramski type I and II lesions, and brainstem location have the propensity to increase the bleeding events. The rebleeding risk is 20%/year per lesion, which supports the need for surgical strategies for brainstem cavernous malfo…