Chloride channels and their modulation by neurotransmitters and drugs

  • 384 Pages
  • 3.12 MB
  • English

Raven Press , New York
GABA -- Receptors -- Congresses., Benzodiazepines -- Receptors -- Congresses., Chloride channels -- Congresses., Chlorides -- metabolism -- congresses., GABA -- physiology -- congresses., Ion Channels -- metabolism -- congresses., Neural Transmission -- congresses., Receptors, GABA-Benzodiazepine -- physiology -- congre
Statementvolume editors, Giovanni Biggio, E. Costa.
SeriesAdvances in biochemical psychopharmacology ;, v. 45
ContributionsBiggio, Giovanni., Costa, Erminio., Capo Boi Conference on Neuroscience (5th : 1987 : Villasimius, Italy)
LC ClassificationsRM315 .A4 vol. 45, QP364.7 .A4 vol. 45
The Physical Object
Paginationxv, 384 p. :
ID Numbers
Open LibraryOL2061301M
ISBN 100881674494
LC Control Number88042745

Adv Biochem Psychopharmacol. ; Chloride channels and their modulation by neurotransmitters and drugs.

Description Chloride channels and their modulation by neurotransmitters and drugs FB2

[No authors listed] PMID. Author(s): Biggio,Giovanni; Costa,Erminio; Capo Boi Conference on Neuroscience,(5th: Villasimius, Italy) Title(s): Chloride channels and their modulation. In this study, we elucidate the validity of a modified glutamate‐gated chloride channel (GluCl cryst) as a structurally accessible model for GABA A receptors.

In contrast to native‐like controls, GluCl cryst exhibits classical activation by its neurotransmitter ligand L‐glutamate.

The modified channel is also sensitive to allosteric modulators associated with human GABA A receptors, and Cited by: 3. Different mechanisms of action have been proposed to explain the effects of antiepileptic drugs (AEDs) including modulation of voltage‐dependent sodium calcium and potassium channels, enhancement of γ‐aminobutyric acid (GABA)‐mediated neuronal inhibition, and reduction in glutamate‐mediated excitatory transmission.

Recent advances in understanding the physiology of ion channels and Author: Ben A. Chindo, Bulus Adzu, Karniyus S. Gamaniel.

Details Chloride channels and their modulation by neurotransmitters and drugs FB2

GABA/benzodiazepine coupling was evaluated in 8 regions of rat brain by the ability of GABA to stimulate nM [3H]flunitrazepam binding.

Rats were t Cited by: The book follows the major milestones of brain development, from formation of the neural tube, through neurogenesis, neuronal migration, and the organization of brain wiring.

Ligand-gated. These channels are also known as the ionotropic receptors and get opened in response to specific ligand molecules binding to the extracellular domain of the receptor proteins [28, 29, 30].Binding of the ligand causes a conformational change in the channel protein that ultimately leads to the opening of the channel gate and subsequent ion flux across the plasma.

The effect of propofol, a novel short acting anaesthetic, on the function of the GABA A /ionophore receptor complex was studied in vitro in cortical membrane preparations from rat cerebral cortex and was compared with the action of pentobarbital and alphaxalone, two general anaesthetics known to enhance GABAergic transmission.

Propofol, mimicking the action of pentobarbital and. G. Biggio, E. Costa (Eds.), Chloride Channels and Their Modulation by Neurotransmitters and Drugs, Raven Press, New York (), p. Google Scholar Sher et al., GABA receptors are classified as GABA-A (activating chloride channels) and GABA-B (potentiating cAMP formation).

GABA-A receptors are the site of action for several neuroactive drugs, including benzodiazepines, barbiturates, picrotoxin, and muscimol. Alcohol also binds to GABA-A receptors. In G. Biggio and E. Costa (Eds.), Chloride Channels and their Modulation by Neurotransmitters and Drugs, Advances in Biochemical Psychopharmacology, Vol.

45, Raven, New York,pp. 18 Weiss, D.S., Barnes, Jr., E.M. and Hablitz, J.J., Whole- cell and single-channel recordings of GABA-gated currents in cultured chick cerebral neurons. New information has also been obtained on the modulation of calcium channel gating by neurotransmitters and drugs.

(J Am Coll CardioI;) Newer Techniques to Study Calcium Currents During the last two decades, calcium currents were stud­ied (l,2) in multicellular preparations from SA node, A V node, Purkinje fibers and ventricular.

Reuter H. Calcium channel modulation by neurotransmitters, enzymes and drugs. Nature. Feb 17; ()– Reuter H, Kokubun S, Prod'hom B. Properties and modulation of cardiac calcium channels.

J Exp Biol. Sep; – Tsien RW, Bean BP, Hess P. It is possible, therefore, that endogenous 5HT modulates the activity of the bumetanide-sensitive (inward) chloride cotransporter.

Modulation of this cotransporter by neurotransmitters such as GABA (Sun and Murali, ; Schomberg et al., ) and glutamate (Sun and Murali, ; Sun and Murali, ; Schomberg et al., ) was demonstrated. All of these drugs modulate GABA-receptor regulated chloride channels at the cellular level assayed by electrophysiological or radioactive ion tracer techniques.

Specific receptor sites for GABA, benzodiazepines, picrotoxin/convulsants, and barbiturates can be assayed in. Allosteric Site – secondary site at which drugs bind to modulate the binding of the agonist to the receptor primary binding site to either enhance (positive allosterism) or reduce (negative allosterism) its effects.

Channel-blocking Site – site at which drugs bind to block the movement of Na + and CA 2+ ions into the cell; NMDA Antagonists –. Sodium, calcium (Ca 2+), K +, and chloride (Cl –) ions move into and out of neurons through ion always move passively down electrochemical gradients through ion channels, which are long polypeptides comprising several subunits that span the plasma membrane several times.

channels selective for Cl ions, with some permeability for bicarbonate anions (49). Exceptionally, in s, a cation-selectiveGABA-gatedchannelhasbeendiscovered(50).Excit-atory neurotransmitters increase the cation conductance to depolarize the membrane, whereas inhibitory neurotransmit.

In biology, cell signaling (cell signalling in British English) or cell-cell communication, governs the basic activities of cells and coordinates multiple-cell actions. A signal is an entity that codes or conveys ical processes are complex molecular interactions that involve a lot of signals.

The ability of cells to perceive and correctly respond to their microenvironment is. Calcium (Ca 2+)-activated chloride (Cl −) channels (CaCCs) play a role in the modulation of action potentials and synaptic responses in the somatodendritic regions of central the vertebrate retina, large Ca 2+-activated Cl − currents (I Cl(Ca)) regulate synaptic transmission at photoreceptor terminals; however, the molecular identity of CaCCs that mediate I Cl(Ca) remains unclear.

Animation 2. Neurotransmitters bind to receptors like a lock and key. Specific transmitters bind and open specific receptors. Ligand and Receptor by Casey Henley is licensed under a Creative Commons Attribution Non-Commercial Share-Alike (CC BY-NC-SA) International License.

The voltage-gated channels involved in the action potential are specific to one ion, whereas excitatory ionotropic. The NLRP3 inflammasome regulates production of the pro-inflammatory cytokines interleukin-1β (IL-1β) and IL, and contributes to inflammation exacerbating disease.

Fenamate non-steroidal anti-inflammatory drugs (NSAIDs) were recently described as NLRP3 inflammasome inhibitors via chloride channel inhibitio Chemical Science HOT Article Collection.

Voltage-sensitive K-currents in sympathetic neurons and their modulation by neurotransmitters. Brown DA, Adams PR, Constanti A. A description is given of methods for voltage clamping and for studies of the several varieties of K-currents occurring in sympathetic neurons.

Figure 2. Structure of the GABA A receptor-chloride channel complex and location of binding sites for different CNS-active drugs. GABA A receptors are formed by different membrane-spanning subunits arranged in different pentameric combinations.

GABA binds to two sites located between α and β subunits, triggering the opening of the chloride channel, which produces. In contrast to excitatory neurotransmitters, inhibitory neurotransmitters prevent a neuron from firing an action potential.

There are three types of GABA receptors, A, B and C. GABA type A (GABA A) and GABA type C (GABA C) receptors are ligand-gated chloride ion (Cl-) channels.

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Receptors Presynaptic NMDA receptors and spike timing-dependent long-term depression at cortical synapses. The immediate effects of activating a channel can be described as: Excitation: Increasing the voltage of the cell and potentially leading to ate is the chief excitatory neurotransmitter; Inhibition: Decreasing the voltage of the cell and potentially reducing firing.

neurotransmitters are separated into 2 categories based off of their size 1. neuropeptides are relatively large transmitter molecules composed of amino acids 2. small-molecule neurotransmitters are comprised of molecules such as glutamate and GABA (individual amino acids) and transmitters acetylcholine, serotonin, and histamine.

MONNA is a TMEM16A (ANO1) calcium-activated chloride channel blocker. MONNA blocks rhTMEM16A (ANO1) channel currents in HEK cells with and IC 50 of μM. The compound MONNA does not affect related human or mouse chloride channels bestrophin-1, CLC2 and CFTR at concentrations up to 10 μM.

Neurons that produce GABA as their output are called GABAergic neurons, and have chiefly inhibitory action at receptors in the adult spiny cells are a typical example of inhibitory central nervous system GABAergic cells.

In contrast, GABA exhibits both excitatory and inhibitory actions in insects, mediating muscle activation at synapses between nerves and muscle cells, and. Z Antagonist effect: Drug binds to the receptor but does not activate a biological response X Another site for drug actions is ion channels, which exist for many ions such as sodium, potassium, chloride, and calcium and can be open at some times and closed at other times.

Neurotransmitters or drugs may be excitatory or inhibitory depending. The open chloride channels allow negatively charged chlorine into the cell, which inhibits the cell from firing.

Chloride ions (Cl-) have a negative charge and also have a higher concentration outside the neurons in the extracellular space. When t.Title: Modulation of Midbrain Dopamine Neurotransmission by Serotonin, a Versatile Interaction Between Neurotransmitters and Significance for Antipsychotic Drug Action VOLUME: 4 ISSUE: 1 Author(s):J.

E. Olijslagers, T. R. Werkman, A. C. McCreary, C. G. Kruse and W. J. Wadman Affiliation:Center for NeuroScience-Swammerdam Institute for Life Sciences, University of Amsterdam,KruislaanAll psychiatric drugs act by affecting neurotransmitters.

Understanding their mechanism of action and adverse effects is key to developing new drugs. Moreover, one half of all medicines prescribed today have something in common: at the molecular level, they act on the same type of target.