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关键词:'P9159'
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J H Steinbach et al.
The Journal of physiology, 537(Pt 3), 715-733 (2001-12-18)
1. We have studied the kinetic properties of channel gating of recombinant alpha 1 beta 2 gamma 2L GABA(A) receptors transiently expressed in human embryonic kidney 293 cells, using the cell-attached, single-channel patch-clamp technique. The receptors were activated by GABA
D R Curtis et al.
Experimental brain research, 64(1), 105-113 (1986-01-01)
When administered microelectrophoretically GABA and piperidine-4-sulphonic acid depolarized the central terminations of muscle group Ia and Ib afferent fibres in the lumbar intermediate nucleus and Clarke's column of cats anaesthetised with pentobarbitone sodium. Both this depolarization, and primary afferent depolarization
J W Miller et al.
Neuropharmacology, 29(7), 649-655 (1990-07-01)
This study characterized the role of GABA in the central medial intralaminar nucleus on seizures induced by pentylenetetrazol given systemically. Injections of the direct selective GABAA agonist, piperidine-4-sulfonic acid or the indirect GABAA agonists, flurazepam and pentobarbital, in this region
J W Miller et al.
Neuroscience, 43(1), 41-49 (1991-01-01)
This study determined the effects of discrete microinjections of GABA agonists in the cholinergic nuclei of the pontomesencephalic tegmentum on spontaneous behavior and seizures induced by intravenous pentylenetetrazol, bicuculline or strychnine, in the rat. Injections of both the GABAA agonist
G Akk et al.
The Journal of physiology, 532(Pt 3), 673-684 (2001-04-21)
Neurosteroids are produced in the brain, and can have rapid actions on membrane channels of neurons. Pregnenolone sulfate (PS) is a sulfated neurosteroid which reduces the responses of the [gamma]-aminobutyric acid A (GABA(A)) receptor. We analysed the actions of PS
B Ebert et al.
Molecular pharmacology, 46(5), 957-963 (1994-11-01)
Using systematic combination of alpha 1, alpha 3, and alpha 5 with beta 1, beta 2, and beta 3, together with gamma 1, gamma 2, and gamma 3, we have investigated the contributions of the various alpha, beta, and gamma
Daniel J Shin et al.
Molecular pharmacology, 95(1), 70-81 (2018-10-20)
Under both physiologic and clinical conditions GABAA receptors are exposed to multiple agonists, including the transmitter GABA, endogenous or exogenous neuroactive steroids, and various GABAergic anesthetic and sedative drugs. The functional output of the receptor reflects the interplay among all
Kate K O'Toole et al.
Molecular pharmacology, 81(2), 189-197 (2011-11-02)
The GABA type A receptor (GABA(A)R) is expressed ubiquitously throughout the brain and is a target for many therapeutic agents, including general anesthetics and benzodiazepines, which enhance receptor function by increasing the open probability (P(o)) of the ion channel. It
Alison L Althaus et al.
Neuropharmacology, 181, 108333-108333 (2020-09-26)
Zuranolone (SAGE-217) is a novel, synthetic, clinical stage neuroactive steroid GABAA receptor positive allosteric modulator designed with the pharmacokinetic properties to support oral daily dosing. In vitro, zuranolone enhanced GABAA receptor current at nine unique human recombinant receptor subtypes, including
Lorenzo Ricci et al.
Biochemical pharmacology, 71(10), 1510-1519 (2006-03-17)
The use of the antiepileptic drug, 4-aminobutyrate transaminase (GABA-T) inhibitor vigabatrin (VIGA), has been recently cautioned because it is associated to irreversible field defects from damage of the retina. Since novel GABA-T inhibitors might prove useful in epilepsy or other
G Maksay et al.
European journal of pharmacology, 411(1-2), 55-60 (2001-01-04)
In order to study the correlation of the thermodynamic driving forces of binding with the efficacies of displacing ligands, the specific binding of [3H]SR 95531 [2-(3-carboxypropyl)3-amino-6-p-methoxyphenylpyridazinium bromide], a GABA(A) receptor antagonist, was studied in cell lines stably expressing human alpha(1)beta(3)gamma(2)
Gustav Akk et al.
Molecular pharmacology, 74(3), 614-627 (2008-06-12)
Neuroactive steroids are among the most efficacious modulators of the mammalian GABA-A receptor. Previous work has proposed that receptor potentiation is mediated by steroid interactions with a site defined by the residues alpha1Asn407/Tyr410 in the M4 transmembrane domain and residue
E H Wong et al.
Journal of neurochemistry, 44(4), 1162-1167 (1985-04-01)
GABAA receptor agonists modulate [3H]diazepam binding in rat cortical membranes with different efficacies. At 23 degrees C, the relative potencies for enhancement of [3H]diazepam binding by agonists parallel their potencies in inhibiting [3H]gamma-aminobutyric acid [( 3H]GABA) binding. The agonist concentrations
D R Curtis et al.
Brain research, 422(1), 192-195 (1987-09-29)
Divalent metal cations, including zinc, cadmium, cobalt, nickel, strontium, manganese, magnesium and calcium, reduced the depolarization by microelectrophoretic gamma-aminobutyric acid (GABA) and piperidine-4-sulphonic acid of the central terminations of muscle group Ia primary afferent fibres in the cat spinal cord
F W Foong et al.
Pain, 27(3), 361-371 (1986-12-01)
In barbiturate anaesthetized cats, tonic inhibition of the excitation of lumbar dorsal horn neurones by impulses in unmyelinated primary afferents was measured by reversibly cooling the spinal cord at the thoraco-lumbar junction. Tonic inhibition was reduced by microinjection of the
Norbert Topf et al.
Anesthesiology, 98(2), 306-311 (2003-01-29)
Volatile anesthetics prolong inhibitory postsynaptic potentials in central neurons an allosteric action on the gamma-aminobutyric acid type A (GABA(A)) receptor, an effect that may underlie the hypnotic actions of these agents. Inhaled anesthetics such as isoflurane act to enhance responses
B D Gynther et al.
Experimental brain research, 74(2), 365-374 (1989-01-01)
In the spinal cord of pentobarbitone anaesthetised cats, increases in the electrical threshold of the terminations of extensor muscle group Ia afferent fibres, produced by tetanic stimulation of either the appropriate peripheral nerve or the central termination, were associated with
J W Miller et al.
Epilepsia, 34(6), 973-978 (1993-11-01)
The cerebellum is electrically and metabolically active during seizures. Numerous studies have also shown that cerebellar electrical stimulation and lesions of the cerebellar cortex or nuclei influence seizure threshold, but there are significant contradictions, with different effects observed even in
S M O'Shea et al.
Brain research, 852(2), 344-348 (2000-03-11)
Using the whole-cell patch-clamp technique, we have determined that propofol, but not midazolam, increases the efficacy of piperidine-4-sulphonic acid (P4S), a partial agonist at alpha1beta1gamma2s, GABA(A) receptors expressed in HEK 293 cells. These findings are consistent with the idea that
M S Jensen et al.
Neuropharmacology, 23(12A), 1441-1450 (1984-12-01)
Electrophysiological recordings from mouse neurones in tissue culture have been used to investigate how agents which interact with the benzodiazepine receptor modulate neuronal responses to gamma-aminobutyric acid (GABA) and its mimetics, 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol (THIP) and piperidine-4-sulphonic acid (P4S). Experiments were performed
B Ebert et al.
Molecular pharmacology, 52(6), 1150-1156 (1997-12-16)
Using human gamma-aminobutyric acid type A (GABAA) receptor subunit combinations, expressed in cell lines and Xenopus laevis oocytes, the pharmacology of a number of ligands interacting directly with the GABA recognition site has been studied in [3H]muscimol binding and electrophysiologically.
E Falch et al.
Journal of neurochemistry, 44(1), 68-75 (1985-01-01)
The relationship between structure, in vivo activity, and in vitro activity of some analogues of the gamma-aminobutyric acid (GABA) agonist piperidine-4-sulphonic acid (P4S) was studied. The syntheses of 1,2,3,6-tetrahydropyridine-4-sulphonic acid (DH-P4S) and (RS)-pyrrolidin-3-yl-methanesulphonamide (PMSA-amide) are described. Like P4S, its unsaturated
Angelo Keramidas et al.
The Journal of physiology, 575(Pt 1), 11-22 (2006-06-10)
The binding of the neurotransmitter GABA induces conformational changes in the GABAA receptor (GABAAR), leading to the opening of a gate that controls ion permeation through an integral transmembrane pore. A number of structural elements within each subunit, located near
D R Curtis et al.
Experimental brain research, 64(1), 114-118 (1986-01-01)
When administered microelectrophoretically, GABA and the GABA-mimetic piperidine-4-sulphonic acid (P4S) appear to have no direct hyperpolarizing or depolarizing effect on the terminations of motor axon collaterals excited electrically in the ventral horn of the lumbar spinal cord of the cat.
Ko Ko et al.
Journal of medical virology (2020-06-25)
This study aimed to investigate the prevalence trend of hepatitis B virus (HBV) and hepatitis C virus (HCV) infections and their genotype distribution among hemodialysis patients, determining their long-term prognosis and the risk factors to the mortality. This cohort study
Piperidine-4-sulphonic acid, a new specific GABA agonist.
P Krogsgaard-Larsen et al.
Journal of neurochemistry, 34(3), 756-759 (1980-03-01)
Marc C Gielen et al.
The Journal of neuroscience : the official journal of the Society for Neuroscience, 32(17), 5707-5715 (2012-04-28)
GABA(A) receptors (GABA(A)Rs) composed of αβγ subunits are allosterically modulated by the benzodiazepines (BDZs). Agonists at the BDZ binding site potentiate submaximal GABA responses by increasing the apparent affinity of GABA(A)Rs for GABA. Although BDZs were initially thought to affect
E Galvez-Ruano et al.
Journal of neuroscience research, 42(5), 666-673 (1995-12-01)
Based on our molecular modeling investigations of the glycinergic receptor, we expanded our studies to similarly investigate the GABAergic receptor. New data suggest there may exist a slightly different agonistic mechanism for the molecules described herein as compared to glycine.
S L Hansen et al.
British journal of pharmacology, 133(4), 539-549 (2001-06-16)
Based on an unexpected high maximum response to piperidine-4-sulphonic acid (P4S) at human alpha1alpha6beta2gamma2 GABA(A) receptors expressed in Xenopus oocytes attempts to correlate this finding with the pharmacological profile of P4S and other GABA(A) receptor ligands in neuronal cultures from
P Helén et al.
The Journal of neuroscience : the official journal of the Society for Neuroscience, 4(6), 1405-1413 (1984-06-01)
The 2-deoxy-D[1-14C]glucose method of Sokoloff was used to measure local cerebral glucose utilization (LCGU) in rats after injections of the GABA receptor agonist, muscimol (1.6 mg/kg and 4.0 mg/kg, i.v.); the muscarinic receptor antagonist, scopolamine (0.4 mg/kg and 2.0 mg/kg
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