An isoquinoline alkaloid obtained from Dicentra cucullaria and other plants. It is a competitive antagonist for GABA-A receptors.
Drugs that bind to but do not activate GABA RECEPTORS, thereby blocking the actions of endogenous GAMMA-AMINOBUTYRIC ACID and GABA RECEPTOR AGONISTS.
Drugs that bind to but do not activate GABA-A RECEPTORS thereby blocking the actions of endogenous or exogenous GABA-A RECEPTOR AGONISTS.
The most common inhibitory neurotransmitter in the central nervous system.
A neurotoxic isoxazole isolated from species of AMANITA. It is obtained by decarboxylation of IBOTENIC ACID. Muscimol is a potent agonist of GABA-A RECEPTORS and is used mainly as an experimental tool in animal and tissue studies.
Cell surface proteins which bind GAMMA-AMINOBUTYRIC ACID and contain an integral membrane chloride channel. Each receptor is assembled as a pentamer from a pool of at least 19 different possible subunits. The receptors belong to a superfamily that share a common CYSTEINE loop.
An alkaloid found in the seeds of STRYCHNOS NUX-VOMICA. It is a competitive antagonist at glycine receptors and thus a convulsant. It has been used as an analeptic, in the treatment of nonketotic hyperglycinemia and sleep apnea, and as a rat poison.
A noncompetitive antagonist at GABA-A receptors and thus a convulsant. Picrotoxin blocks the GAMMA-AMINOBUTYRIC ACID-activated chloride ionophore. Although it is most often used as a research tool, it has been used as a CNS stimulant and an antidote in poisoning by CNS depressants, especially the barbiturates.
Cell-surface proteins that bind GAMMA-AMINOBUTYRIC ACID with high affinity and trigger changes that influence the behavior of cells. GABA-A receptors control chloride channels formed by the receptor complex itself. They are blocked by bicuculline and usually have modulatory sites sensitive to benzodiazepines and barbiturates. GABA-B receptors act through G-proteins on several effector systems, are insensitive to bicuculline, and have a high affinity for L-baclofen.
Endogenous compounds and drugs that bind to and activate GAMMA-AMINOBUTYRIC ACID receptors (RECEPTORS, GABA).
A GAMMA-AMINOBUTYRIC ACID derivative that is a specific agonist of GABA-B RECEPTORS. It is used in the treatment of MUSCLE SPASTICITY, especially that due to SPINAL CORD INJURIES. Its therapeutic effects result from actions at spinal and supraspinal sites, generally the reduction of excitatory transmission.
Substances that act in the brain stem or spinal cord to produce tonic or clonic convulsions, often by removing normal inhibitory tone. They were formerly used to stimulate respiration or as antidotes to barbiturate overdose. They are now most commonly used as experimental tools.
Substances used for their pharmacological actions on glycinergic systems. Glycinergic agents include agonists, antagonists, degradation or uptake inhibitors, depleters, precursors, and modulators of receptor function.
The function of opposing or restraining the excitation of neurons or their target excitable cells.
Heterocyclic acids that are derivatives of 4-pyridinecarboxylic acid (isonicotinic acid).
Endogenous compounds and drugs that bind to and activate GABA-A RECEPTORS.
The basic cellular units of nervous tissue. Each neuron consists of a body, an axon, and dendrites. Their purpose is to receive, conduct, and transmit impulses in the NERVOUS SYSTEM.
Therapeutic introduction of ions of soluble salts into tissues by means of electric current. In medical literature it is commonly used to indicate the process of increasing the penetration of drugs into surface tissues by the application of electric current. It has nothing to do with ION EXCHANGE; AIR IONIZATION nor PHONOPHORESIS, none of which requires current.
A short-acting barbiturate that is effective as a sedative and hypnotic (but not as an anti-anxiety) agent and is usually given orally. It is prescribed more frequently for sleep induction than for sedation but, like similar agents, may lose its effectiveness by the second week of continued administration. (From AMA Drug Evaluations Annual, 1994, p236)
Substances used for their pharmacological actions on GABAergic systems. GABAergic agents include agonists, antagonists, degradation or uptake inhibitors, depleters, precursors, and modulators of receptor function.
A non-essential amino acid. It is found primarily in gelatin and silk fibroin and used therapeutically as a nutrient. It is also a fast inhibitory neurotransmitter.
A potent excitatory amino acid antagonist with a preference for non-NMDA iontropic receptors. It is used primarily as a research tool.
The D-enantiomer is a potent and specific antagonist of NMDA glutamate receptors (RECEPTORS, N-METHYL-D-ASPARTATE). The L form is inactive at NMDA receptors but may affect the AP4 (2-amino-4-phosphonobutyrate; APB) excitatory amino acid receptors.
The injection of very small amounts of fluid, often with the aid of a microscope and microsyringes.
Derivatives of BUTYRIC ACID that contain one or more amino groups attached to the aliphatic structure. Included under this heading are a broad variety of acid forms, salts, esters, and amides that include the aminobutryrate structure.
Drugs that bind to but do not activate GABA-B RECEPTORS thereby blocking the actions of endogenous or exogenous GABA-B RECEPTOR AGONISTS.
Use of electric potential or currents to elicit biological responses.
A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company.
Electrical responses recorded from nerve, muscle, SENSORY RECEPTOR, or area of the CENTRAL NERVOUS SYSTEM following stimulation. They range from less than a microvolt to several microvolts. The evoked potential can be auditory (EVOKED POTENTIALS, AUDITORY), somatosensory (EVOKED POTENTIALS, SOMATOSENSORY), visual (EVOKED POTENTIALS, VISUAL), or motor (EVOKED POTENTIALS, MOTOR), or other modalities that have been reported.
Drugs that bind to but do not activate excitatory amino acid receptors, thereby blocking the actions of agonists.
A subset of GABA RECEPTORS that signal through their interaction with HETEROTRIMERIC G-PROTEINS.
Abrupt changes in the membrane potential that sweep along the CELL MEMBRANE of excitable cells in response to excitation stimuli.
The communication from a NEURON to a target (neuron, muscle, or secretory cell) across a SYNAPSE. In chemical synaptic transmission, the presynaptic neuron releases a NEUROTRANSMITTER that diffuses across the synaptic cleft and binds to specific synaptic receptors, activating them. The activated receptors modulate specific ion channels and/or second-messenger systems in the postsynaptic cell. In electrical synaptic transmission, electrical signals are communicated as an ionic current flow across ELECTRICAL SYNAPSES.
The study of the generation and behavior of electrical charges in living organisms particularly the nervous system and the effects of electricity on living organisms.
Pregnane derivatives in which two side-chain methyl groups or two methylene groups in the ring skeleton (or a combination thereof) have been oxidized to keto groups.
A benzodiazepine with anticonvulsant, anxiolytic, sedative, muscle relaxant, and amnesic properties and a long duration of action. Its actions are mediated by enhancement of GAMMA-AMINOBUTYRIC ACID activity.
Clinical or subclinical disturbances of cortical function due to a sudden, abnormal, excessive, and disorganized discharge of brain cells. Clinical manifestations include abnormal motor, sensory and psychic phenomena. Recurrent seizures are usually referred to as EPILEPSY or "seizure disorder."
Derivatives of BUTYRIC ACID that include a double bond between carbon 2 and 3 of the aliphatic structure. Included under this heading are a broad variety of acid forms, salts, esters, and amides that include the aminobutryrate structure.
Substances that do not act as agonists or antagonists but do affect the GAMMA-AMINOBUTYRIC ACID receptor-ionophore complex. GABA-A receptors (RECEPTORS, GABA-A) appear to have at least three allosteric sites at which modulators act: a site at which BENZODIAZEPINES act by increasing the opening frequency of GAMMA-AMINOBUTYRIC ACID-activated chloride channels; a site at which BARBITURATES act to prolong the duration of channel opening; and a site at which some steroids may act. GENERAL ANESTHETICS probably act at least partly by potentiating GABAergic responses, but they are not included here.
Specialized junctions at which a neuron communicates with a target cell. At classical synapses, a neuron's presynaptic terminal releases a chemical transmitter stored in synaptic vesicles which diffuses across a narrow synaptic cleft and activates receptors on the postsynaptic membrane of the target cell. The target may be a dendrite, cell body, or axon of another neuron, or a specialized region of a muscle or secretory cell. Neurons may also communicate via direct electrical coupling with ELECTRICAL SYNAPSES. Several other non-synaptic chemical or electric signal transmitting processes occur via extracellular mediated interactions.
Cell surface receptors that bind GLYCINE with high affinity and trigger intracellular changes which influence the behavior of cells. Glycine receptors in the CENTRAL NERVOUS SYSTEM have an intrinsic chloride channel and are usually inhibitory.
An electrophysiologic technique for studying cells, cell membranes, and occasionally isolated organelles. All patch-clamp methods rely on a very high-resistance seal between a micropipette and a membrane; the seal is usually attained by gentle suction. The four most common variants include on-cell patch, inside-out patch, outside-out patch, and whole-cell clamp. Patch-clamp methods are commonly used to voltage clamp, that is control the voltage across the membrane and measure current flow, but current-clamp methods, in which the current is controlled and the voltage is measured, are also used.
Inorganic or organic derivatives of phosphinic acid, H2PO(OH). They include phosphinates and phosphinic acid esters.
A curved elevation of GRAY MATTER extending the entire length of the floor of the TEMPORAL HORN of the LATERAL VENTRICLE (see also TEMPORAL LOBE). The hippocampus proper, subiculum, and DENTATE GYRUS constitute the hippocampal formation. Sometimes authors include the ENTORHINAL CORTEX in the hippocampal formation.
A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.
A cylindrical column of tissue that lies within the vertebral canal. It is composed of WHITE MATTER and GRAY MATTER.
A broad-spectrum excitatory amino acid antagonist used as a research tool.
The voltage differences across a membrane. For cellular membranes they are computed by subtracting the voltage measured outside the membrane from the voltage measured inside the membrane. They result from differences of inside versus outside concentration of potassium, sodium, chloride, and other ions across cells' or ORGANELLES membranes. For excitable cells, the resting membrane potentials range between -30 and -100 millivolts. Physical, chemical, or electrical stimuli can make a membrane potential more negative (hyperpolarization), or less negative (depolarization).
Depolarization of membrane potentials at the SYNAPTIC MEMBRANES of target neurons during neurotransmission. Excitatory postsynaptic potentials can singly or in summation reach the trigger threshold for ACTION POTENTIALS.
A pharmaceutical agent that displays activity as a central nervous system and respiratory stimulant. It is considered a non-competitive GAMMA-AMINOBUTYRIC ACID antagonist. Pentylenetetrazole has been used experimentally to study seizure phenomenon and to identify pharmaceuticals that may control seizure susceptibility.
The posterior pair of the quadrigeminal bodies which contain centers for auditory function.
An aminoperhydroquinazoline poison found mainly in the liver and ovaries of fishes in the order TETRAODONTIFORMES, which are eaten. The toxin causes paresthesia and paralysis through interference with neuromuscular conduction.
An amino acid that, as the D-isomer, is the defining agonist for the NMDA receptor subtype of glutamate receptors (RECEPTORS, NMDA).
A benzodiazepine derivative used mainly as a hypnotic.
The domestic cat, Felis catus, of the carnivore family FELIDAE, comprising over 30 different breeds. The domestic cat is descended primarily from the wild cat of Africa and extreme southwestern Asia. Though probably present in towns in Palestine as long ago as 7000 years, actual domestication occurred in Egypt about 4000 years ago. (From Walker's Mammals of the World, 6th ed, p801)
An anxiolytic benzodiazepine derivative with anticonvulsant, sedative, and amnesic properties. It has also been used in the symptomatic treatment of alcohol withdrawal.
A non-essential amino acid naturally occurring in the L-form. Glutamic acid is the most common excitatory neurotransmitter in the CENTRAL NERVOUS SYSTEM.
A class of chemicals derived from barbituric acid or thiobarbituric acid. Many of these are GABA MODULATORS used as HYPNOTICS AND SEDATIVES, as ANESTHETICS, or as ANTICONVULSANTS.
Nucleus in the anterior part of the HYPOTHALAMUS.
A pregnane found in the urine of pregnant women and sows. It has anesthetic, hypnotic, and sedative properties.
Most generally any NEURONS which are not motor or sensory. Interneurons may also refer to neurons whose AXONS remain within a particular brain region in contrast to projection neurons, which have axons projecting to other brain regions.
Endogenous compounds and drugs that bind to and activate GABA-B RECEPTORS.
Drugs that bind to and activate excitatory amino acid receptors.
Inorganic compounds derived from hydrochloric acid that contain the Cl- ion.
A class of ionotropic glutamate receptors characterized by affinity for N-methyl-D-aspartate. NMDA receptors have an allosteric binding site for glycine which must be occupied for the channel to open efficiently and a site within the channel itself to which magnesium ions bind in a voltage-dependent manner. The positive voltage dependence of channel conductance and the high permeability of the conducting channel to calcium ions (as well as to monovalent cations) are important in excitotoxicity and neuronal plasticity.
Cell-surface proteins that bind glutamate and trigger changes which influence the behavior of cells. Glutamate receptors include ionotropic receptors (AMPA, kainate, and N-methyl-D-aspartate receptors), which directly control ion channels, and metabotropic receptors which act through second messenger systems. Glutamate receptors are the most common mediators of fast excitatory synaptic transmission in the central nervous system. They have also been implicated in the mechanisms of memory and of many diseases.
(2S-(2 alpha,3 beta,4 beta))-2-Carboxy-4-(1-methylethenyl)-3-pyrrolidineacetic acid. Ascaricide obtained from the red alga Digenea simplex. It is a potent excitatory amino acid agonist at some types of excitatory amino acid receptors and has been used to discriminate among receptor types. Like many excitatory amino acid agonists it can cause neurotoxicity and has been used experimentally for that purpose.
Refers to animals in the period of time just after birth.
Central gray matter surrounding the CEREBRAL AQUEDUCT in the MESENCEPHALON. Physiologically it is probably involved in RAGE reactions, the LORDOSIS REFLEX; FEEDING responses, bladder tonus, and pain.
Neural tracts connecting one part of the nervous system with another.
The relationship between the dose of an administered drug and the response of the organism to the drug.
Several groups of nuclei in the thalamus that serve as the major relay centers for sensory impulses in the brain.
The part of the brain that connects the CEREBRAL HEMISPHERES with the SPINAL CORD. It consists of the MESENCEPHALON; PONS; and MEDULLA OBLONGATA.
An inhibitor of glutamate decarboxylase. It decreases the GAMMA-AMINOBUTYRIC ACID concentration in the brain, thereby causing convulsions.
A benzodiazepine with pharmacologic actions similar to those of DIAZEPAM that can cause ANTEROGRADE AMNESIA. Some reports indicate that it is used as a date rape drug and suggest that it may precipitate violent behavior. The United States Government has banned the importation of this drug.
GRAY MATTER located in the dorsomedial part of the MEDULLA OBLONGATA associated with the solitary tract. The solitary nucleus receives inputs from most organ systems including the terminations of the facial, glossopharyngeal, and vagus nerves. It is a major coordinator of AUTONOMIC NERVOUS SYSTEM regulation of cardiovascular, respiratory, gustatory, gastrointestinal, and chemoreceptive aspects of HOMEOSTASIS. The solitary nucleus is also notable for the large number of NEUROTRANSMITTERS which are found therein.
A conditionally essential nutrient, important during mammalian development. It is present in milk but is isolated mostly from ox bile and strongly conjugates bile acids.
A transition zone in the anterior part of the diencephalon interposed between the thalamus, hypothalamus, and tegmentum of the mesencephalon. Components of the subthalamus include the SUBTHALAMIC NUCLEUS, zona incerta, nucleus of field H, and the nucleus of ansa lenticularis. The latter contains the ENTOPEDUNCULAR NUCLEUS.
Paired bundles of NERVE FIBERS entering and leaving the SPINAL CORD at each segment. The dorsal and ventral nerve roots join to form the mixed segmental spinal nerves. The dorsal roots are generally afferent, formed by the central projections of the spinal (dorsal root) ganglia sensory cells, and the ventral roots are efferent, comprising the axons of spinal motor and PREGANGLIONIC AUTONOMIC FIBERS.
The action of a drug that may affect the activity, metabolism, or toxicity of another drug.
Projection neurons in the CEREBRAL CORTEX and the HIPPOCAMPUS. Pyramidal cells have a pyramid-shaped soma with the apex and an apical dendrite pointed toward the pial surface and other dendrites and an axon emerging from the base. The axons may have local collaterals but also project outside their cortical region.
Drugs used to prevent SEIZURES or reduce their severity.
A common name for fish of the family Percidae, belonging to the suborder Percoidei, order PERCIFORMES.
A disorder characterized by recurrent episodes of paroxysmal brain dysfunction due to a sudden, disorderly, and excessive neuronal discharge. Epilepsy classification systems are generally based upon: (1) clinical features of the seizure episodes (e.g., motor seizure), (2) etiology (e.g., post-traumatic), (3) anatomic site of seizure origin (e.g., frontal lobe seizure), (4) tendency to spread to other structures in the brain, and (5) temporal patterns (e.g., nocturnal epilepsy). (From Adams et al., Principles of Neurology, 6th ed, p313)
Order of mammals whose members are adapted for flight. It includes bats, flying foxes, and fruit bats.
A condition characterized by abnormal posturing of the limbs that is associated with injury to the brainstem. This may occur as a clinical manifestation or induced experimentally in animals. The extensor reflexes are exaggerated leading to rigid extension of the limbs accompanied by hyperreflexia and opisthotonus. This condition is usually caused by lesions which occur in the region of the brainstem that lies between the red nuclei and the vestibular nuclei. In contrast, decorticate rigidity is characterized by flexion of the elbows and wrists with extension of the legs and feet. The causative lesion for this condition is located above the red nuclei and usually consists of diffuse cerebral damage. (From Adams et al., Principles of Neurology, 6th ed, p358)
Derivatives of GLUTAMIC ACID. Included under this heading are a broad variety of acid forms, salts, esters, and amides that contain the 2-aminopentanedioic acid structure.
Nerve structures through which impulses are conducted from a peripheral part toward a nerve center.
The 12th cranial nerve. The hypoglossal nerve originates in the hypoglossal nucleus of the medulla and supplies motor innervation to all of the muscles of the tongue except the palatoglossus (which is supplied by the vagus). This nerve also contains proprioceptive afferents from the tongue muscles.
Genetically identical individuals developed from brother and sister matings which have been carried out for twenty or more generations or by parent x offspring matings carried out with certain restrictions. This also includes animals with a long history of closed colony breeding.
Substances used for their pharmacological actions on any aspect of neurotransmitter systems. Neurotransmitter agents include agonists, antagonists, degradation inhibitors, uptake inhibitors, depleters, precursors, and modulators of receptor function.
Neurons which activate MUSCLE CELLS.
Ventral part of the DIENCEPHALON extending from the region of the OPTIC CHIASM to the caudal border of the MAMMILLARY BODIES and forming the inferior and lateral walls of the THIRD VENTRICLE.
An aggregation of cells in the middle hypothalamus dorsal to the ventromedial nucleus and bordering the THIRD VENTRICLE.
Expulsion of milk from the mammary alveolar lumen, which is surrounded by a layer of milk-secreting EPITHELIAL CELLS and a network of myoepithelial cells. Contraction of the myoepithelial cells is regulated by neuroendocrine signals.
Paired bodies containing mostly GRAY MATTER and forming part of the lateral wall of the THIRD VENTRICLE of the brain.
Organic compounds that contain phosphorus as an integral part of the molecule. Included under this heading is broad array of synthetic compounds that are used as PESTICIDES and DRUGS.
A genus in the family Blattidae containing several species, the most common being P. americana, the American cockroach.
Collections of small neurons centrally scattered among many fibers from the level of the TROCHLEAR NUCLEUS in the midbrain to the hypoglossal area in the MEDULLA OBLONGATA.
Region of hypothalamus between the ANTERIOR COMMISSURE and OPTIC CHIASM.
A barbiturate that is used as a sedative. Secobarbital is reported to have no anti-anxiety activity.
A class of saturated compounds consisting of two rings only, having two or more atoms in common, containing at least one hetero atom, and that take the name of an open chain hydrocarbon containing the same total number of atoms. (From Riguady et al., Nomenclature of Organic Chemistry, 1979, p31)
Cell surface receptors that bind signalling molecules released by neurons and convert these signals into intracellular changes influencing the behavior of cells. Neurotransmitter is used here in its most general sense, including not only messengers that act to regulate ion channels, but also those which act on second messenger systems and those which may act at a distance from their release sites. Included are receptors for neuromodulators, neuroregulators, neuromediators, and neurohumors, whether or not located at synapses.
The thin layer of GRAY MATTER on the surface of the CEREBRAL HEMISPHERES that develops from the TELENCEPHALON and folds into gyri and sulchi. It reaches its highest development in humans and is responsible for intellectual faculties and higher mental functions.
Cell membrane glycoproteins that form channels to selectively pass chloride ions. Nonselective blockers include FENAMATES; ETHACRYNIC ACID; and TAMOXIFEN.
Injections into the cerebral ventricles.
A nicotinic antagonist used primarily as a ganglionic blocker in animal research. It has been used as an antihypertensive agent but has been supplanted by more specific drugs in most clinical applications.
Neurotransmitter receptors located on or near presynaptic terminals or varicosities. Presynaptic receptors which bind transmitter molecules released by the terminal itself are termed AUTORECEPTORS.
The front part of the hindbrain (RHOMBENCEPHALON) that lies between the MEDULLA and the midbrain (MESENCEPHALON) ventral to the cerebellum. It is composed of two parts, the dorsal and the ventral. The pons serves as a relay station for neural pathways between the CEREBELLUM to the CEREBRUM.
A group of two-ring heterocyclic compounds consisting of a benzene ring fused to a diazepine ring.
The tendency of a phenomenon to recur at regular intervals; in biological systems, the recurrence of certain activities (including hormonal, cellular, neural) may be annual, seasonal, monthly, daily, or more frequently (ultradian).
A group of compounds with the heterocyclic ring structure of benzo(c)pyridine. The ring structure is characteristic of the group of opium alkaloids such as papaverine. (From Stedman, 25th ed)
A region extending from the PONS & MEDULLA OBLONGATA through the MESENCEPHALON, characterized by a diversity of neurons of various sizes and shapes, arranged in different aggregations and enmeshed in a complicated fiber network.
Techniques used mostly during brain surgery which use a system of three-dimensional coordinates to locate the site to be operated on.
An enzyme that converts brain gamma-aminobutyric acid (GAMMA-AMINOBUTYRIC ACID) into succinate semialdehyde, which can be converted to succinic acid and enter the citric acid cycle. It also acts on beta-alanine. EC 2.6.1.19.
A potent benzodiazepine receptor antagonist. Since it reverses the sedative and other actions of benzodiazepines, it has been suggested as an antidote to benzodiazepine overdoses.

Somatic recording of GABAergic autoreceptor current in cerebellar stellate and basket cells. (1/1439)

Patch-clamp recordings were performed from stellate and basket cells in rat cerebellar slices. Under somatic voltage clamp, short depolarizing pulses were applied to elicit action potentials in the axon. After the action potential, a bicuculline- and Cd2+-sensitive current transient was observed. A similar response was obtained when eliciting axonal firing by extracellular stimulation. With an isotonic internal Cl- solution, the peak amplitude of this current varied linearly with the holding potential, yielding an extrapolated reversal potential of -20 to 0 mV. Unlike synaptic or autaptic GABAergic currents obtained in the same preparation, the current transient had a slow rise-time and a low variability between trials. This current was blocked when 10 mM BAPTA was included in the recording solution. In some experiments, the current transient elicited axonal action potentials. The current transient was reliably observed in animals aged 12-15 d, with a mean amplitude of 82 pA at -70 mV, but was small and rare in the age group 29-49 d. Numerical simulations could account for all properties of the current transient by assuming that an action potential activates a distributed GABAergic conductance in the axon. The actual conductance is probably restricted to release sites, with an estimated mean presynaptic current response of 10 pA per site (-70 mV, age 12-15 d). We conclude that in developing rats, stellate and basket cell axons have a high density of GABAergic autoreceptors and that a sizable fraction of the corresponding current can be measured from the soma.  (+info)

Retinal input induces three firing patterns in neurons of the superficial superior colliculus of neonatal rats. (2/1439)

By using an in vitro isolated brain stem preparation, we recorded extracellular responses to electrical stimulation of the optic tract (OT) from 71 neurons in the superficial superior colliculus (SC) of neonatal rats (P1-13). At postnatal day 1 (P1), all tested neurons (n = 10) already received excitatory input from the retina. Sixty-nine (97%) superficial SC neurons of neonatal rats showed three response patterns to OT stimulation, which depended on stimulus intensity. A weak stimulus evoked only one spike that was caused by activation of non-N-methyl-D-aspartate (NMDA) glutamate receptors. A moderate stimulus elicited a short train (<250 ms) of spikes, which was induced by activation of both NMDA and non-NMDA receptors. A strong stimulus gave rise to a long train (>300 ms) of spikes, which was associated with additional activation of L-type high-threshold calcium channels. The long train firing pattern could also be induced either by temporal summation of retinal inputs or by blocking gamma-aminobutyric acid-A receptors. Because retinal ganglion cells show synchronous bursting activity before eye opening at P14, the retinotectal inputs appear to be sufficient to activate L-type calcium channels in the absence of pattern vision. Therefore activation of L-type calcium channels is likely to be an important source for calcium influx into SC neurons in neonatal rats.  (+info)

The superior olivary nucleus and its influence on nucleus laminaris: a source of inhibitory feedback for coincidence detection in the avian auditory brainstem. (3/1439)

Located in the ventrolateral region of the avian brainstem, the superior olivary nucleus (SON) receives inputs from nucleus angularis (NA) and nucleus laminaris (NL) and projects back to NA, NL, and nucleus magnocellularis (NM). The reciprocal connections between the SON and NL are of particular interest because they constitute a feedback circuit for coincidence detection. In the present study, the chick SON was investigated. In vivo tracing studies show that the SON projects predominantly to the ipsilateral NM, NL, and NA. In vitro whole-cell recording reveals single-cell morphology, firing properties, and postsynaptic responses. SON neurons are morphologically and physiologically suited for temporal integration; their firing patterns do not reflect the temporal structure of their excitatory inputs. Of most interest, direct stimulation of the SON evokes long-lasting inhibition in NL neurons. The inhibition blocks both intrinsic spike generation and orthodromically evoked activity in NL neurons and can be eliminated by bicuculline methiodide, a potent antagonist for GABAA receptor-mediated neurotransmission. These results strongly suggest that the SON provides GABAergic inhibitory feedback to laminaris neurons. We discuss a mechanism whereby SON-evoked GABAergic inhibition can influence the coding of interaural time differences for sound localization in the avian auditory brainstem.  (+info)

Concurrent inhibition and excitation of phrenic motoneurons during inspiration: phase-specific control of excitability. (4/1439)

The movements that define behavior are controlled by motoneuron output, which depends on the excitability of motoneurons and the synaptic inputs they receive. Modulation of motoneuron excitability takes place over many time scales. To determine whether motoneuron excitability is specifically modulated during the active versus the quiescent phase of rhythmic behavior, we compared the input-output properties of phrenic motoneurons (PMNs) during inspiratory and expiratory phases of respiration. In neonatal rat brainstem-spinal cord preparations that generate rhythmic respiratory motor outflow, we blocked excitatory inspiratory synaptic drive to PMNs and then examined their phase-dependent responses to superthreshold current pulses. Pulses during inspiration elicited fewer action potentials compared with identical pulses during expiration. This reduced excitability arose from an inspiratory-phase inhibitory input that hyperpolarized PMNs in the absence of excitatory inspiratory inputs. Local application of bicuculline blocked this inhibition as well as the difference between inspiratory and expiratory firing. Correspondingly, bicuculline locally applied to the midcervical spinal cord enhanced fourth cervical nerve (C4) inspiratory burst amplitude. Strychnine had no effect on C4 output. Nicotinic receptor antagonists neither potentiated C4 output nor blocked its potentiation by bicuculline, further indicating that the inhibition is not from recurrent inhibitory pathways. We conclude that it is bulbospinal in origin. These data demonstrate that rapid changes in motoneuron excitability occur during behavior and suggest that integration of overlapping, opposing synaptic inputs to motoneurons is important in controlling motor outflow. Modulation of phasic inhibition may represent a means for regulating the transfer function of PMNs to suit behavioral demands.  (+info)

Long-term suppression of synaptic transmission by tetanization of a single pyramidal cell in the mouse hippocampus in vitro. (5/1439)

1. The consequences of stimulating a single pyramidal cell in the CA1 area of the hippocampus for synaptic transmission in the stratum radiatum were investigated. 2. Tetanic activation of single pyramids caused by depolarizing current injection, but not an equal number of distributed action potentials, reduced excitatory transmission by 20 %, with a delayed onset, for more than 1 h. 3. EPSPs in the tetanized pyramidal cells were increased for equally long periods but this was not the cause of the field EPSP reduction. Spontaneous somatic IPSPs were not affected; evoked IPSPs were decreased in the tetanized cell. 4. Paired pulse facilitation of the field EPSPs was unchanged. 5. The field EPSP reduction was markedly diminished by a knife cut along the base of pyramidal cells in CA1. 6. The addition of antagonists of GABA, NMDA and metabotropic glutamate receptors blocked or diminished the field EPSP slope reduction evoked by intracellular stimulation. 7. Simultaneous recordings revealed long-lasting excitations of interneurons located in the outer oriens layer as a result of single pyramid tetanization. 8. Intense firing of small numbers of pyramidal cells can thus persistently inhibit mass transmission through the hippocampus. This effect involves activation of interneurons by glutamate receptors.  (+info)

Inhibitory contributions to spatiotemporal receptive-field structure and direction selectivity in simple cells of cat area 17. (6/1439)

Intracortical inhibition contributes to direction selectivity in primary visual cortex, but how it acts has been unclear. We investigated this problem in simple cells of cat area 17 by taking advantage of the link between spatiotemporal (S-T) receptive-field structure and direction selectivity. Most cells in layer 4 have S-T-oriented receptive fields in which gradients of response timing across the field confer a preferred direction of motion. Linear summation of responses across the receptive field, followed by a static nonlinear amplification, has been shown previously to account for directional tuning in layer 4. We tested the hypotheses that inhibition acts by altering S-T structure or the static nonlinearity or both. Drifting and counterphasing sine wave gratings were used to measure direction selectivity and S-T structure, respectively, in 17 layer 4 simple cells before and during iontophoresis of bicuculline methiodide (BMI), a GABAA antagonist. S-T orientation was quantified from fits to response temporal phase versus stimulus spatial phase data. Bicuculline reduced direction selectivity and S-T orientation in nearly all cells, and reductions in the two measures were well correlated (r = 0.81) and reversible. Using conventional linear predictions based on response phase and amplitude, we found that BMI-induced changes in S-T structure also accounted well for absolute changes in the amplitude and phase of responses to gratings drifting in the preferred and nonpreferred direction. For each cell we also calculated an exponent used to estimate the static nonlinearity. Bicuculline reduced the exponent in most cells, but the changes were not correlated with reductions in direction selectivity. We conclude that GABAA-mediated inhibition influences directional tuning in layer 4 primarily by sculpting S-T receptive-field structure. The source of the inhibition is likely to be other simple cells with certain spatiotemporal relationships to their target. Despite reductions in the two measures, most receptive fields maintained some directional tuning and S-T orientation during BMI. This suggests that their excitatory inputs, arising from the lateral geniculate nucleus and within area 17, are sufficient to create some S-T orientation and that inhibition accentuates it. Finally, BMI also reduced direction selectivity in 8 of 10 simple cells tested in layer 6, but the reductions were not accompanied by systematic changes in S-T structure. This reflects the fact that S-T orientation, as revealed by our first-order measures of the receptive field, is weak there normally. Inhibition likely affects layer 6 cells via more complex, nonlinear interactions.  (+info)

Choline and selective antagonists identify two subtypes of nicotinic acetylcholine receptors that modulate GABA release from CA1 interneurons in rat hippocampal slices. (7/1439)

Neuronal nicotinic receptors (nAChR) are known to control transmitter release in the CNS. Thus, this study was aimed at exploring the diversity and localization of nAChRs present in CA1 interneurons in rat hippocampal slices. The use of a U-tube as the agonist delivery system was critical for the reliable detection of nicotinic responses induced by brief exposure of the neurons to ACh or to the alpha7 nAChR-selective agonist choline. The present study demonstrated that CA1 interneurons, in addition to expressing functional alpha7 nAChRs, also express functional alpha4beta2-like nAChRs and that activation of both receptors facilitates an action potential-dependent release of GABA. Depending on the experimental condition, one of the following nicotinic responses was recorded from the interneurons by means of the patch-clamp technique: a nicotinic whole-cell current, depolarization accompanied by action potentials, or GABA-mediated postsynaptic currents (PSCs). Responses mediated by alpha7 nAChRs were short-lasting, whereas those mediated by alpha4beta2 nAChRs were long-lasting. Thus, phasic or tonic inhibition of CA1 interneurons may be achieved by selective activation of alpha7 or alpha4beta2 nAChRs, respectively. It can also be suggested that synaptic levels of choline generated by hydrolysis of ACh in vivo may be sufficient to control the activity of the alpha7 nAChRs. The finding that methyllycaconitine and dihydro-beta-erythroidine (antagonists of alpha7 and alpha4beta2 nAChRs, respectively) increased the frequency and amplitude of GABAergic PSCs suggests that there is an intrinsic cholinergic activity that sustains a basal level of nAChR activity in these interneurons.  (+info)

Synchronized paroxysmal activity in the developing thalamocortical network mediated by corticothalamic projections and "silent" synapses. (8/1439)

In mouse thalamocortical slices in vitro, the potassium channel blocker 4-AP and GABAA receptor antagonist bicuculline together induced spontaneous prolonged depolarizations in layer VI neurons from postnatal day 2 (P2), in ventroposterior nucleus neurons (VP) from P7, and in reticular nucleus neurons (RTN) from P8. Dual whole-cell recordings revealed that prolonged bursts were synchronized in layer VI, VP, and RTN. Bursts were present in cortex isolated from thalamus, but not in thalamus isolated from cortex, indicating that bursts originated in cortex and propagated to thalamus. Prolonged bursts were synchronized in layer VI when vertical cuts extended from pia mater through layers IV or V, but were no longer synchronized when cuts extended through layer VI and white matter. In voltage-clamp recordings before P10, burst conductance of all three neuronal populations was dominated by the NMDA receptor-mediated conductance, and therefore synapses were "silent". In cortex and RTN, after P10, bursts were associated with strong AMPA/kainate receptor-mediated conductances, and synapses had become "functional"; silent synapses persisted in a large proportion of VP cells after P10. Before P9, the NMDA receptor antagonist APV or the non-NMDA receptor antagonist CNQX blocked the prolonged bursts. After P9, CNQX continued to block the prolonged bursts, but APV merely shortened their duration. Thus, NMDA receptor-based silent synapses are essential for paroxysmal corticothalamic activity during early postnatal development, and connections between layer VI neurons are sufficient for horizontal cortical synchronization.  (+info)

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This could also be associated to differences in the genetic background of the CB1 knockout mice used and/or completely different experimental circumstances. Collectively, a majority of evidence helps a job for CB1 receptors in the control of emotional behavior and suggests the existence of an anxiolytic endocannabinoid tone. The protective impact of cannabinoids in traumatic brain injury was first indicated in studies with the nonpsychotropic cannabinoid dexanabinol (HU-211) (Fig. 1b). These research have demonstrated lowered brain injury and improved motor and cognitive perform in HU-211-treated animals in a rat mannequin of TBI.. A related mechanism has been postulated for cannabinoids by Cheer et al. , who reported that local application of the cannabinoid agonist HU-210 to mind slices containing the VTA increased dopaminergic neuronal activity, which might be blocked by the GABAA antagonist bicuculline. There is evidence for added sites of motion, such as CB1 receptors on the terminals of ...
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TY - JOUR. T1 - Bicuculline and strychnine suppress the mesencephalic locomotor region-induced inhibition of group III muscle afferent input to the dorsal horn. AU - Degtyarenko, A. M.. AU - Kaufman, Marc P. PY - 2003/5/25. Y1 - 2003/5/25. N2 - We examined the effect of iontophoretic application of bicuculline methiodide and strychnine hydrochloride on the mesencephalic locomotor region (MLR)-induced inhibition of dorsal horn cells in paralyzed cats. The activity of 60 dorsal horn cells was recorded extracellularly in laminae I, II, V-VII of spinal segments L7-S1. Each of the cells was shown to receive group III muscle afferent input as demonstrated by their responses to electrical stimulation of the tibial nerve (mean latency and threshold of activation: 20.1±6.4 ms and 15.2±1.4 times motor threshold, respectively). Electrical stimulation of the MLR suppressed transmission in group III muscle afferent pathways to dorsal horn cells. Specifically the average number of impulses generated by the ...
Spontaneously opening, chloride-selective channels that showed outward rectification were recorded in ripped-off patches from rat cultured hippocampal neurons and in cell-attached patches from rat hippocampal CA1 pyramidal neurons in slices. In both preparations, channels had multiple conductance states and the most common single-channel conductance varied. In the outside-out patches it ranged from 12 to 70 pS (Vp=40 mV) whereas in the cell-attached patches it ranged from 56 to 85 pS (-Vp=80 mV). Application of GABA to a patch showing spontaneous channel activity evoked a rapid, synchronous activation of channels. During prolonged exposure to either 5 or 100 microM GABA, the open probability of channels decreased. Application of GABA appeared to have no immediate effect on single-channel conductance. Exposure of the patches to 100 microM bicuculline caused a gradual decrease on the single-channel conductance of the spontaneous channels. The time for complete inhibition to take place was slower ...
Hello all,. Ive recently ran into trouble recording mIPSCs in a synaptically active in vitro neuron population. In all cases, Ive been using whole-cell configuration and performing -70 VC recordings. For mEPSCs (in the presence of TTX and bicuculline), I use a 140 mM K-Gluconate based buffer and get beautiful recordings with mEPSC rates around 6-10 Hz. However, when recording mIPSCs (in the presence of TTX, CNQX, AP5) using either a 140 mM Cs-Cl based buffer or 140 mM KCl based buffer, Ive recently started running into issues. Immediately after break-in, my holding current drops precipitously to around -500 pA. This leads to a horribly messy recording in which I cant even pick out events amongst the noise. Previously (as of a few weeks ago), I was reliably able to record mIPSCs with a frequency of around 1-3 Hz. Now, even if I am able to occasionally get a somewhat stable seal, the noise is terrible. Ive tried making up new intracellular and extracellular buffers 3 times now. Sterile ...
GABA binding and bicuculline in spinal cord and cortical membranes from adult rat and from mouse neurons in cell culture. Brain Res. 1982 Jul 22; 244(1):145-53 ...
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This work examined the electrophysiological correlates of chorea induced by bicuculline microinjection into the GPe. The behavioral effects in the present study are in line with those described earlier (Grabli et al. 2004), showing a direct relationship between the location of injections in the GPe and the induced abnormal hyperbehavioral symptoms. Bicuculline caused a marked increase in the firing rate of GPe neurons, which was associated with drastic changes in firing pattern. In some bicuculline-affected GPe neurons, pauses became more pronounced (BHF), whereas in others they were almost completely abolished (CHF). These abnormal activity patterns were associated with a reduction in the information capacity of neurons. Bicuculline also induced regularity in both the spiking and bursting activity in the GPe. However, there was very little correlated activity in the GPe either in the temporal or in the spectral domains. There were no gross changes in the activity of GPi neurons after GPe ...
JNeurosci Print ISSN: 0270-6474 Online ISSN: 1529-2401. The ideas and opinions expressed in JNeurosci do not necessarily reflect those of SfN or the JNeurosci Editorial Board. Publication of an advertisement or other product mention in JNeurosci should not be construed as an endorsement of the manufacturers claims. SfN does not assume any responsibility for any injury and/or damage to persons or property arising from or related to any use of any material contained in JNeurosci.. ...
We recorded from pairs of cultured, synaptically connected thalamic neurons. Evoked excitatory postsynaptic currents (EPSCs) reversed at +17 mV and were blocked reversibly by 1 mM kynurenic acid, a glutamate receptor antagonist. NMDA and non-NMDA receptors mediated excitatory post-synaptic responses, as shown by selective block of EPSC components with 50 microM (+/-)-2-amino-5-phosphonopentanoic acid and 10 microM 6,7-dinitroquinoxaline-2,3-dione, respectively. Inhibitory postsynaptic responses were evoked less frequently and were blocked by the GABAA receptor antagonist (-)-bicuculline methochloride. The pharmacological profiles of whole-cell calcium currents and evoked EPSCs were compared. With 50 microM cadmium chloride (Cd), whole-cell low voltage-activated (LVA) calcium currents were reduced in amplitude and high voltage- activated (HVA) calcium currents and excitatory synaptic transmission were completely blocked. This suggests that the residual calcium influx through LVA channels into the ...
Inhibition in the neostriatum was investigated in rat in vitro slice preparation using intracellular recording and labeling technique. The initial response recorded following local stimulation is a monosynaptically activated EPSP. In 17% of the neurons tested, IPSPs were observed following EPSPs evoked by local stimulation. In paired shock experiments reduction of test EPSP amplitude or action potentials occurred over interstimulus intervals (ISIs) of 3-38 msec. In some neurons, a pulse injection of depolarizing current was used to trigger an action potential which was in a paired shock, used to condition a test monosynaptically induced EPSP. Test EPSPs were shunted over ISIs less than 45 msec. Paired shock performed on the slices perfused with the medium containing GABA antagonists (e.g., bicuculline methiodide, picrotoxin, or penicillin-G) resulted invariably in potentiation of test EPSPs. Inhibition in the neostriatum in vitro is demonstrated as reduction in test amplitude in paired shock tests, by
Lendormin is used to treat, control and prevent insomnia and other conditions. It contains Brotizolam as an active ingredient. Lendormin works by increasing the inhibitory effect of gamma-aminobutyric acid on the central nervous system. ...
Bicuculline, Carbachol, Cholinergic Agonist, Gaba, Hippocampal Formation, Hippocampus, Neuron, Neurons, Population, Rats, Separated, Urethane
몬혐 1엔섙늏 죿찪관련, 돆롟·볹돆관련, 쓫렇긷, 홝겾 붊편신곟왃 죿거홝겾많졯돆읙 엵관섯읃 삵펷볹앚닧. 몬혐 2엔섙늏 읺런핞 붊편신곟 믺웓드읃 섺뵿홒핓엪 뵿섙핓였닧. 핓즼많 앚설 몬혐드윸 햊젖돜 수죿읙 찪읺릀 곟련핞 수 엉늏 핞겾젋읃 각즼곟 자윸믂롟 읺릀 곟련핓엪 몬혐 3엔섙늏 햊젖돜 단윀 수죿읙 닧수죿 숣섙혐 롟즼슞티 몬혐윸롟 뵿섙핓였닧. ,푞 3,읙 AIC왃 BIC읙 갗읃 븼굎핞 겨관 숣섙혐 롟즼슞티 몬혐볹닧 몬혐3읙 닧수죿 숣섙혐 롟즼슞티 몬혐엔섙 설몀련읺 햫샀핓늏 겆윸롟 낐탄낦닧.. 몬혐 1엔섙 샡홝붊편 믺웓 줕 죿찪관련 붊편신곟, 돆롟·볹돆관련 붊편신곟, 쓫렇긷 붊편신곟, 홝겾 붊편신곟각 죿거홝겾많졯돆릀 아홒신킣늏 욑읺윸롟 낐탄낦닧. 귵릭곟 햊젖돜 수죿읙 찪읺릀 곟련핞 몬혐 3엔섙늏 붊법죿젖찪, 죿찪굯엪윀받, 볹돆 붊편, ...
The principal finding in this study is that orexin modulates the activity of RVLM adrenal sympathetic premotor neurons, resulting in excitation of adrenal chromaffin cells. We showed that local glucoprivation or disinhibition of PeH neurons increased ASNA, whereas inhibition of PeH neurons abolished the ASNA response after systemic glucoprivation. Conversely, glucoprivation of perifornical neurons subsequent to activation by the GABAA antagonist bicuculline reduced the adrenal sympathoexcitatory response. In addition, local neuroglucoprivation in the RVLM failed to activate premotor neurons in vivo or in vitro, suggesting that RVLM neurons are not intrinsically glucose-sensitive. Finally, ASNA was directly correlated with plasma metanephrine levels but not normetanephrine levels, confirming that adrenal sympathoexcitation coincides with adrenaline release into the circulation. The ASNA, noradrenaline, and adrenaline responses to glucoprivation noted in our study were consistent with previous ...
Direct-write printing of stem cells within biomaterials presents an opportunity to engineer tissue for in vitro modeling and regenerative medicine. Here, a first example of constructing neural tissue by printing human neural stem cells that are differentiated in situ to functional neurons and supporting neuroglia is reported. The supporting biomaterial incorporates a novel clinically relevant polysaccharide-based bioink comprising alginate, carboxymethyl-chitosan, and agarose. The printed bioink rapidly gels by stable cross-linking to form a porous 3D scaffold encapsulating stem cells for in situ expansion and differentiation. Differentiated neurons form synaptic contacts, establish networks, are spontaneously active, show a bicuculline-induced increased calcium…. ...
We have shown that the inhibitory phosphorylation of the WNK/SPAK-regulated Thr906/Thr1007 motif in KCC2 is substantially reduced during the course of CNS development. Second, regulated KCC2 Thr906/Thr1007 phosphorylation is essential for mouse survival; antagonizing the normal developmental down-regulation of KCC2 Thr906/Thr1007 via homozygous phospho-mimetic mutagenesis of these sites causes respiratory arrest and early postnatal death. Third, corroborating and extending previous in vitro findings (24, 26), phospho-mimetic mutation of Thr906/Thr1007 in vivo prevents KCC2 from dynamically increasing its Cl− extrusion capacity (such as in response to a Cl− load). This results in an imbalance of neuronal excitation and inhibition that leads to impaired rhythmogenesis in respiratory and locomotor networks accompanied by profound neuronal hyperexcitability manifesting as touch-evoked generalized seizures. Fourth, Kcc2E/E mice exhibit anomalous neuronal distribution with normal dendritic spine ...
Tytuł projektu: Udostępnianie cyfrowe zasobów polskich czasopism z nauk przyrodniczych i rolniczych w bazie AGRO. Nr umowy: POPC.02.03.01-00-0038/18-00 (okres realizacji 2018-2021). Kwota dofinansowania: 7 442 980,00 z. W ramach Programu Operacyjnego Polska Cyfrowa na lata 2014-2020, Oś Priorytetowa nr 2 E-administracja i otwarty rząd Działanie nr 2.3 Cyfrowa dostępność i użyteczność informacji sektora publicznego Poddziałanie nr 2.3.1 Cyfrowe udostępnienie informacji sektora publicznego ze źródeł administracyjnych i zasobów nauki (typ projektu: cyfrowe udostępnienie zasobów nauki) Instytucja Finansująca: Centrum Projektów Polska Cyfrowa ...
Neuronal injury due to seizures may result from a mismatch of energy demand and adenosine triphosphate (ATP) synthesis. However, ATP demand and oxygen consumption rates have not been accurately determined, yet, for different patterns of epileptic activity, such as interictal and ictal events. We studied interictal-like and seizure-like epileptiform activity induced by the GABAA antagonist bicuculline alone, and with co-application of the M-current blocker XE-991, in rat hippocampal slices. Metabolic changes were investigated based on recording partial oxygen pressure, extracellular potassium concentration, and intracellular flavine adenine dinucleotide (FAD) redox potential. Recorded data were used to calculate oxygen consumption and relative ATP consumption rates, cellular ATP depletion, and changes in FAD/FADH2 ratio by applying a reactive-diffusion and a two compartment metabolic model. Oxygen-consumption rates were ca. five times higher during seizure activity than interictal activity. Additionally,
Slices of human cortical tissue from epilepsy surgery were investigated with intracellular recordings to elucidate the mechanisms contributing to augmented synaptic excitation and to repetitive activity. The analysis of single synaptic potentials revealed, amongst other differences to rodent cortex, a disturbance of GABAA inhibition, namely depolarizing responses. A tentative ionic mechanism, impaired KCl outward-transport (KCC2), was evaluated in a rat model (0-Mg hyperexcitability). The observed down-regulation of KCC2 mRNA after 0-Mg-ACSF exposure of slices may contribute to the depolarizations by GABA. The factors enabling repetitive activity were addressed with a paired-pulse paradigm. In slices from epilepsy surgery, synaptic responses were virtually constant with interstimulus intervals between 100 and 1000 ms. Tiagabine markedly prolonged the effects of released GABA at GABAA receptors, but paired-pulse behaviour was only slightly affected. We demonstrate that bicuculline-induced ...
Centrally released oxytocin (OXT) has anxiolytic and anti-stress effects. Delayed gastric emptying (GE) induced by acute restraint stress (ARS) for 90 min is completely restored following 5 consecutive days of chronic homotypic restraint stress (CHS), via up-regulating hypothalamic OXT expression in rats. However, the mechanism behind the restoration of delayed GE following CHS remains unclear. Gamma-aminobutyric acid (GABA)-projecting neurons in the paraventricular nucleus (PVN) have been shown to inhibit corticotropin releasing factor (CRF) synthesis via GABA(A) receptors. We hypothesized that GABA(A) receptors are involved in mediating the inhibitory effect of OXT on CRF expression in the PVN, which in turn restores delayed GE following CHS. OXT (0.5 μg) and selective GABA(A) receptor antagonist, bicuculline methiodide (BMI) (100 ng), were administered intracerebroventricularly (icv). Solid GE was measured under non-stressed (NS), ARS and CHS conditions. Expression of CRF mRNA in the PVN was ...
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We employed dual probe microdialysis in the nucleus accumbens and ipsilateral ventral pallidum of the halothane anaesthetized rat to investigate the effect of intra-accumbens perfusion with the sulphated octapeptide cholecystokinin (CCK-8S, 10-1000 nM, 60 min) alone and in the presence of the selective CCK1 and CCK2 receptor antagonists L-364,718 (10 and 100 nM) and PD134308 (10 nM), tetrodotoxin (TTX, 1000 nM) and the GABA(A) receptor antagonist bicuculline (1000 nM), on dialysate GABA levels in the ventral pallidum ...
Bicuculline methiodide (BIC-Mel) (10-100 microM) altered the kinetics of N-methyl-D-aspartate (NMDA) responses in single-channel and whole-cell recordings. The principal effect of BIC-Mel (10-100 microM) on NMDA channels was a dose-dependent decrease in mean channel open time (tau o), accompanied by the introduction of a new closed time (tau B) of 14.0 +/- 3.5 msec (mean +/- standard deviation; n = 14) in closed time distributions, which was independent of BIC-Mel concentration. BIC-Mel (10-100 microM) increased the frequency of NMDA channel opening in a dose-dependent manner, offsetting the decrease in tau o, such that the total time spent in the open state per minute was unchanged, and thus the total charge/min through NMDA channels was unchanged. Similarly, the amplitudes of NMDA whole-cell current responses were not noticeably affected by 10-80 microM BIC-Mel, even though power spectra density analysis of the whole-cell NMDA-stimulated noise revealed changes in the underlying channel ...
Toward a Cure for Tinnitus [media] Thanos Tzounopoulos, Ph.D., assistant professor of otolaryngology and neurobiology at the University of Pittsburgh...
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TY - JOUR. T1 - Enhancement of NMDA receptor-mediated synaptic potential evoked in rat medial-amygdala neuron following olfactory bulbectomy. AU - Nakanishi, Hiroshi. AU - Ukai, Kiyoharu. AU - Nakagawa, Terutake. AU - Watanabe, Shigenori. AU - Kamata, Osamu. AU - Yamamoto, Kenji. PY - 1990/11/5. Y1 - 1990/11/5. N2 - Synaptic potentials evoked in the medial amygdala (m-AMG) neurons were studied in in vitro slice preparations obtained from normal and olfactory bulbectomized rats. Local stimulation induced a sequence of responses: a fast EPSP, a fast IPSP and a slow EPSP. The fast EPSP was suppressed by kynurenic acid (KYN) at a concentration of 1 mM but not by 3-[(±)-2-carboxypiperazin-4-yl-]-propyl-1-phosphonic acid (CPP) at a concentrations up to 20 μM. The slow EPSP was reversibly blocked by both KYN (1 mM) and CPP (5-10 μM). Addition of bicuculline methiodide (50 μM) to the bath suppressed the fast IPSP and augmented both the fast and slow EPSPs leading to burst discharges. In a small ...
Banerjee, Probal and lyengar, Raghu R and Ayyer, Jayalekshmy and Bhattacharyya, PK (1984) Carbonation of Phenol: A Novel Reaction Involving Enzyme Model Catalysis. In: Current Science, 53 (23). pp. 1226-1228. Bhattacharyya, PK and Samanta, TB and Ullah, AHJ and Gunsalus, IC (1984) Chemical probes into the active centre of a heme thiolate monoxygenase. In: Journal of Chemical Sciences, 93 (8). pp. 1289-1304. Bhattacharyya, PK and Bhattacharyya, Apares (1981) Fluorescent labelling of strychnine: A novel approach for recognition of strychnine binding sites on neuronal membrane. In: Biochemical and Biophysical Research Communications, 101 (1). pp. 273-280. Ramanjaneyulu, R. and Madyastha, KM and Bhattacharyya, PK (1981) Chemical approach to aspirin hypersensitivity. In: Biochemical and Biophysical Research Communications, 101 (1). pp. 258-264. Bhattacharyya, Apares and Madyastha,, KM and Bhattacharyya, PK and Devanandan, MS (1981) Studies on bicuculline binding sites on neuronal membrane using ...
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We previously reported that oroxylin A, a γ-aminobutyric acid A (GABAA) receptor antagonist, ameliorates drugs-induced memory impairments. We synthesized several oroxylin A derivatives in efforts to find a substance that has pro-cognitive effects as well as improves sensorimotor gating. The aim of the present study is to investigate the effect of a novel oroxylin A derivative, 5,7-dihydroxy-6-meth ...
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Antibodies for proteins involved in gamma-aminobutyric acid receptor clustering pathways, according to their Panther/Gene Ontology Classification
This is the first electrophysiological study to examine the cellular effects of the RFamide group of peptides on hypothalamic parvocellular PVN neurons. We found that NPFF and NPVF, which belong to the RFamide peptide family, significantly inhibited the evoked GABAergic IPSCs in a concentration-dependent manner. NPFF-induced reduction in inhibitory synaptic responses could be abolished by RF9, a NPFF receptor antagonist, which has been recently reported to block opioid-induced hyperalgesia and elevations in blood pressure and heart rate evoked by NPFF (35). Also, NPFF and NPVF decreased the frequency of GABAergic mIPSCs without affecting the amplitude or decay time constant of mIPSCs, indicating a presynaptic locus for the actions of these peptides. Furthermore, we observed that NPFF and NPVF caused depolarization of parvocellular PVN neurons. This excitatory effect was present in TTX but eliminated in the presence of bicuculline (and TTX). Collectively, these results indicate that NPFF and the ...
Although agarwood has been used as a tranquilizer in Asian countries for hundreds of years, the underlying pharmacological basis is still unclear. This study investigated the sedative-hypnotic effect of agarwood essential oil (AEO) using locomotor activity and pentobarbital-induced sleeping assays in mice. Single (1-day) and multiple (7- and 14-days) administrations of 60 mg/kg AEO generated significant sedative effect on inhibiting locomotor activity and hypnotic effect on pentobarbital-induced sleeping in mice. Interestingly, prolonged AEO treatment did not result in obvious desensitization. Concoitant measurement of the levels of brain neurotransmitters using ultrafast liquid chromatography-tandem mass spectrometry (UFLC-MS/MS) indicated that AEO had no significant effect on the levels of glutamic acid (Glu) and γ-aminobutyric acid (GABA) in the brain. However, the sedative-hypnotic effects were blocked by the type A GABA (GABAA) receptor antagonists bicuculline and flumazenil. In addition, AEO
Description: Gamma-Aminobutyric Acid Receptor Subunit Alpha 5 (GABA(A) Receptor Subunit Alpha 5 or GABRA5) - Gamma-aminobutyric acid A receptor, alpha 5 or
Introduction. Interictal spikes, identifiable as sharp transient deflections (30-50 ms) in electroencephalographic recordings, are electrographic markers of epilepsy (Pedley, 1984). Recordings during epileptic surgery operations show that up to 50% of cells exhibit burst discharge in the focus during interictal spikes (Wyler & Ward, 1981). These studies demonstrate directly that synchronized burst firing in populations of cortical neurons sustains the epileptiform activity. Clearly, information concerning the mechanisms underlying synchronized burst discharge are of fundamental importance to the understanding of epileptogenesis.. That GABAergic (GABA is γ-aminobutyric acid) inhibitory transmission regulates epileptiform activity is indicated by the action of several convulsant compounds. Analogues of interictal spikes can be produced experimentally with agents such as penicillin, bicuculline, and picrotoxin. These agents are all potent blockers of GABAA receptor function (see e.g., Macdonald, ...
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gamma-aminobutyric acid definition: An amino acid, C4H9NO2, that isnt present in proteins, but takes place when you look at the nervous system and is linked to the transmission of neurological impulses.;…
Strychnine is a alkaloid poisoning is manifested by Central nervous system damage - impaired sensation, spasms of skeletal muscles and internal organs. To avoid the unfavorable outcome care is provided in intensive care.
Strychnine is a chemical used in rat poison and is easily separated from the rest of the chemicals. When mixed with LSD, it creates a substance that is easily absorbed into the human flesh, and highly fatal. Please be careful if you are using a pay phone anywhere. You may want to wipe it off, or just not use one at all. If you have any ...
The effects of N‐(4,4‐diphenyl‐3‐butenyl) derivatives of nipecotic acid (SKF‐89976‐A and SKF‐100844‐A) and guvacine (SKF‐100330‐A… Expand ...
Who are the threads of color weaving together in your world? Hello, Bright Light. I hope this finds you and yours well in all ways. As we move through these intense times and energetic upswings, I would like to share something we created last month. Its a short meditation-y video message that came through after…
... and bicuculline. The protein also contains a number of different allosteric binding sites which modulate the activity of the ... bicuculline, gabazine. Positive allosteric modulators: barbiturates, benzodiazepines, certain carbamates (ex. carisoprodol, ...
Bicuculline (very similar in structure) Perrins JD (July 1862). "On Hydrastine, an Alkaloid Occurring in Hydrastis Canadensis ...
Johnston GA (May 2013). "Advantages of an antagonist: bicuculline and other GABA antagonists". British Journal of Pharmacology ... GABAA receptor antagonists, inverse agonists or negative allosteric modulators Bemegride Bicuculline Cicutoxin Cyclothiazide ... Thujone GABA synthesis inhibitors 3-Mercaptopropionic acid Allylglycine Glycine receptor antagonists Bicuculline Brucine ...
All SK channels can be pharmacologically blocked by quaternary ammonium salts of a plant-derived neurotoxin bicuculline. In ... Quaternary ammonium salts like bicuculline and tetraethylammonium (TEA) enter the pore via the selectivity filter by acting as ... Khawaled R, Bruening-Wright A, Adelman JP, Maylie J (August 1999). "Bicuculline block of small-conductance calcium-activated ... Lei-Dab7 N-methyl-laudanosine N-Me-bicuculline Pancuronium Atracurium 1-ethyl-1H-benzo[d]imidazol-2(3H)-on 6,7-dichloro-3-( ...
Bicuculline Strychnine Gähwiler BH, Maurer R, Wüthrich HJ (April 1984). "Pitrazepin, a novel GABAA antagonist". Neuroscience ...
It has long been recognized that the fast response of neurons to GABA that is stimulated by bicuculline and picrotoxin is due ... ISBN 3-456-00390-0. Hill DR, Bowery NG (March 1981). "3H-baclofen and 3H-GABA bind to bicuculline-insensitive GABA B sites in ... This ability of GABA to inhibit neurotransmitter release from these preparations was not blocked by bicuculline, was not ... Takeuchi A, Onodera K (March 1972). "Effect of bicuculline on the GABA receptor of the crayfish neuromuscular junction". Nature ...
Ueno S, Bracamontes J, Zorumski C, Weiss DS, Steinbach JH (15 January 1997). "Bicuculline and gabazine are allosteric ...
Ueno, S; Bracamontes, J; Zorumski, C; Weiss, DS; Steinbach, JH (1997). "Bicuculline and gabazine are allosteric inhibitors of ...
Behrens, CJ; Van Den Boom, LP; Heinemann, U (2007). "Effects of the GABA(A) receptor antagonists bicuculline and gabazine on ... Ueno, S; Bracamontes, J; Zorumski, C; Weiss, DS; Steinbach, JH (1997). "Bicuculline and gabazine are allosteric inhibitors of ...
Drew CA, Johnston GA, Weatherby RP (December 1984). "Bicuculline-insensitive GABA receptors: studies on the binding of (−)- ... not sensitive to the GABAB agonist baclofen nor the GABAA receptor antagonist bicuculline; not modulated by many GABAA receptor ... gamma-Aminobutyric acid rho 1 receptor RNA induces bicuculline-, barbiturate-, and benzodiazepine-insensitive gamma- ...
Examples include bicuculline, securinine and metrazol, and the benzodiazepine GABAA receptor antagonist flumazenil. Other ...
... and bicuculline. Wangchuk, P.; Keller, P. A.; Pyne, S. G.; Sastraruji, T.; Taweechotipatr, M.; Rattanajak, R.; Tonsomboon, A.; ...
Woodward, RM; Polenzani, L; Miledi, R (1993). "Characterization of bicuculline/baclofen-insensitive (rho-like) gamma- ...
... whereas bicuculline is a weak one. Glycine is a required co-agonist along with glutamate for NMDA receptors. In contrast to the ...
CS1 maint: discouraged parameter (link) Hill, DR; Bowery, NG (12 March 1981). "3H-baclofen and 3H-GABA bind to bicuculline- ...
"The pentylenetetrazol-like interoceptive stimulus produced by ethanol withdrawal is potentiated by bicuculline and picrotoxinin ...
Hill DR, Bowery NG (March 1981). "3H-baclofen and 3H-GABA bind to bicuculline-insensitive GABA B sites in rat brain". Nature. ...
Selective Brucine Strychnine Tutin Non-selective Bicuculline Caffeine Picrotoxin Pitrazepin Thiocolchicoside Glycine receptor ...
GABA-T inhibitor Bamaluzole Bicuculline Deramciclane Ethanol Fengabine Gabapentinoid Loreclezole Propofol Retigabine/ezogabine ...
Unlike bicuculline, ROD-188 acts as an agonist at GABAA receptors, being a positive allosteric modulator acting at a novel ... Bicuculline US Patent 6649626 N-substituted 1-(lactone) isoquinolones for treating nervous disorders Thomet U, Baur R, Razet R ... ROD-188 is a sedative drug that was structurally derived from the GABAA antagonist bicuculline by a team at Roche. ...
When tested in mice, denatured venom from P. occidentalis inhibited convulsions during seizures induced by bicuculline, ...
... bicuculline, and picrotoxin". Physiol. Behav. 61 (3): 411-418. doi:10.1016/s0031-9384(96)00452-0. PMID 9089760. India portal ...
... inhibited seizures evoked by bicuculline, pentylenetetrazole, and kainic acid as well as increasing the latency of ...
Gamma-aminobutyric acid receptor subunit alpha-4 is a protein that in humans is encoded by the GABRA4 gene.[5][6] GABA is the major inhibitory neurotransmitter in the mammalian brain where it acts at GABA-A receptors, which are ligand-gated chloride channels. Chloride conductance of these channels can be modulated by agents such as benzodiazepines that bind to the GABA-A receptor. At least 16 distinct subunits of GABA-A receptors have been identified.[6] ...
... is a nootropic drug invented in 2009 by a team working for Hoffmann-La Roche, which acts as a subtype-selective inverse agonist at the α5 subtype of the benzodiazepine binding site on the GABAA receptor. It has good selectivity for the α5 subtype and did not produce convulsant or anxiogenic effects in animal studies, making it a promising potential nootropic.[1][2][3] Ro4938581 and a related derivative basmisanil (RG-1662, RO5186582) have subsequently been investigated for the alleviation of cognitive dysfunction in Down syndrome.[4][5] ...
... also binds to and blocks α2δ subunit-containing VDCCs, similarly to gabapentin and pregabalin, and hence is a gabapentinoid.[9][16] Both (R)-phenibut and (S)-phenibut display this action with similar affinity (Ki = 23 and 39 μM, respectively).[9] Moreover, (R)-phenibut possesses 4-fold greater affinity for this site than for the GABAB receptor (Ki = 92 μM), while (S)-phenibut does not bind significantly to the GABAB receptor (Ki , 1 mM).[9] As such, based on the results of this study, phenibut would appear to have much greater potency in its interactions with α2δ subunit-containing VDCCs than with the GABAB receptor (between 5- to 10-fold).[9] For this reason, the actions of phenibut as a α2δ subunit-containing voltage-gated calcium channel blocker or gabapentinoid may be its true primary mechanism of action, and this may explain the differences between phenibut and its close relative baclofen (which, in contrast, has essentially insignificant activity as a gabapentinoid; Ki = 6 ...
Text is available under the Creative Commons Attribution-ShareAlike License; additional terms may apply. By using this site, you agree to the Terms of Use and Privacy Policy. Wikipedia® is a registered trademark of the Wikimedia Foundation, Inc., a non-profit organization ...
... , also known as eltanolone (INN), is an endogenous neurosteroid that is biosynthesized from progesterone.[1] It is a positive allosteric modulator of the GABAA receptor,[1] as well as a negative allosteric modulator of the glycine receptor,[2] and is known to have sedative, anxiolytic, anesthetic, and anticonvulsant effects.[1][2][3] It was investigated for clinical use as a general anesthetic, but produced unwanted side effects such as convulsions on occasion, and for this reason was never marketed.[2][4] During pregnancy, pregnanolone and allopregnanolone are involved in sedation and anesthesia of the fetus.[5][6] ...
... is used to treat a wide variety of infections, including infections of bones and joints, endocarditis, gastroenteritis, malignant otitis externa, respiratory tract infections, cellulitis, urinary tract infections, prostatitis, anthrax, and chancroid.[2]. Ciprofloxacin only treats bacterial infections; it does not treat viral infections such as the common cold. For certain uses including acute sinusitis, lower respiratory tract infections and uncomplicated gonorrhea, ciprofloxacin is not considered a first-line agent.. Ciprofloxacin occupies an important role in treatment guidelines issued by major medical societies for the treatment of serious infections, especially those likely to be caused by Gram-negative bacteria, including Pseudomonas aeruginosa. For example, ciprofloxacin in combination with metronidazole is one of several first-line antibiotic regimens recommended by the Infectious Diseases Society of America for the treatment of community-acquired abdominal infections in ...
... bicuculline can be used to block Ca2+-activated potassium channels. Sensitivity to bicuculline is defined by IUPHAR as a major ... The action of bicuculline is primarily on the ionotropic GABAA receptors, which are ligand-gated ion channels concerned chiefly ... Bicuculline is a phthalide-isoquinoline compound that is a light-sensitive competitive antagonist of GABAA receptors. It was ... The half-maximal inhibitory concentration (IC50) of bicuculline on GABAA receptors is 3 μM.[citation needed] In addition to ...
Behavioral Consequences of Bicuculline Injection in the Subthalamic Nucleus and the Zona Incerta in Rat Céline Périer, Léon ...
Bicuculline*Bicuculline. *6-(5,6,7,8-Tetrahydro-6-methyl-1,3-dioxolo(4,5-g)isoquinolin-5-yl)furo(3,4-e)1,3-benzodioxol-8(6H)one ... "Bicuculline" is a descriptor in the National Library of Medicines controlled vocabulary thesaurus, MeSH (Medical Subject ... This graph shows the total number of publications written about "Bicuculline" by people in Harvard Catalyst Profiles by year, ... Below are the most recent publications written about "Bicuculline" by people in Profiles. ...
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Naloxone reversed the effects of the higher doses of morphine and fentanyl in all models except bicuculline induced seizures. ... The activity of opioid analgesics in seizure models utilizing N-methyl-DL-aspartic acid, kainic acid, bicuculline and ... pethidine exhibited a biphasic dose response relationship with respect to their effects on seizure thresholds to bicuculline, ...
... Birnir, Bryndis John ... Exposure of the patches to 100 microM bicuculline caused a gradual decrease on the single-channel conductance of the ...
The delivery time for this item is approximately 5-8 business days. If other deviations occur, this will be noted on the order confirmation or communicated via email. Please note, we do reserve the right to select the best packaging and shipping method in order to insure the stability of the product and allow efficient order tracking ...
... ... Treatment with the GABAA antagonist, bicuculline, resulted in increased levels of MMP-9, 12 h after drug administration, but no ... No obvious degeneration was detected in kainate-treated, non-convulsive rats or bicuculline-treated animals. These data ...
At the highest bicuculline doses (0.25 mg/animal) the maximum values recorded were: ΔHbO2 = +19 ± 7 μM; ΔHHb = -12 ± 4 μM; ... Bicuculline-Induced Seizures: A Challenge for Optical and Biochemical Modeling of the Cytochrome Oxidase CuA Nirs Signal. ... Cooper C.E., Cope M., Elwell C.E., Delpy D.T. (2009) Bicuculline-Induced Seizures: A Challenge for Optical and Biochemical ... The changes induced by bicuculline provide an interesting challenge to the physics and biochemistry of using NIRS to study ...
GABA binding and bicuculline in spinal cord and cortical membranes from adult rat and from mouse neurons in cell culture. Brain ... GABA binding and bicuculline in spinal cord and cortical membranes from adult rat and from mouse neurons in cell culture. ... GABA binding and bicuculline in spinal cord and cortical membranes from adult rat and from mouse neurons in cell culture. ...
Bicuculline is a neuromodulatory GABA-A receptor antagonist used to study regional variation of GABA receptors and the role of ... Coadministration of bicuculline and NMDA induces paraplegia in the rat. Brain Res. 2012 Apr 27;1451:27-33. PMID: 22445063 ... Through its inhibition of GABA-A receptors, bicuculline potentiates activation at NMDA receptors and produces membrane ... bicuculline and penicillin. Brain Res. 1982 Jan 28;232(1):41-56. PMID: 7055710. ...
Curtis DR, Felix D (1971) The effect of bicuculline upon synaptic inhibition in the cerebral and cerebellar cortices of the cat ... Sillito AM (1975) The effectiveness of bicuculline as an antagonist of GABA and visually evoked inhibition in the cats striate ... Alloway, K.D., Burton, H. Differential effects of GABA and bicuculline on rapidly- and slowly-adapting neurons in primary ... Alloway KD, Burton H (1986) Bicuculline-induced alterations in neuronal responses to controlled tactile stimuli in the second ...
Effects of low doses of bicuculline on N-methyl-D-aspartate single-channel kinetics are not evident in whole-cell currents.. J ... Effects of low doses of bicuculline on N-methyl-D-aspartate single-channel kinetics are not evident in whole-cell currents.. J ... Effects of low doses of bicuculline on N-methyl-D-aspartate single-channel kinetics are not evident in whole-cell currents.. J ... Bicuculline methiodide (BIC-Mel) (10-100 microM) altered the kinetics of N-methyl-D-aspartate (NMDA) responses in single- ...
Characterization of bicuculline/baclofen-insensitive (rho-like) gamma-aminobutyric acid receptors expressed in Xenopus oocytes ... Characterization of bicuculline/baclofen-insensitive (rho-like) gamma-aminobutyric acid receptors expressed in Xenopus oocytes ... Characterization of bicuculline/baclofen-insensitive (rho-like) gamma-aminobutyric acid receptors expressed in Xenopus oocytes ... Characterization of bicuculline/baclofen-insensitive (rho-like) gamma-aminobutyric acid receptors expressed in Xenopus oocytes ...
... bicuculline explanation free. What is bicuculline? Meaning of bicuculline medical term. What does bicuculline mean? ... Looking for online definition of bicuculline in the Medical Dictionary? ... Bicuculline , definition of bicuculline by Medical dictionary https://medical-dictionary.thefreedictionary.com/bicuculline ... bicuculline. Also found in: Encyclopedia, Wikipedia. bi·cu·cul·line. (bīkū-kyūlēn), An alkaloid naturally occurring in the d- ...
Likewise, bicuculline and strychnine suppressed the MLR-induced inhibition of transmission of group III afferent input to ... Likewise, bicuculline and strychnine suppressed the MLR-induced inhibition of transmission of group III afferent input to ... Likewise, bicuculline and strychnine suppressed the MLR-induced inhibition of transmission of group III afferent input to ... Likewise, bicuculline and strychnine suppressed the MLR-induced inhibition of transmission of group III afferent input to ...
Bicuculline, pentobarbital and diazepam modulate spontaneous GABA(A) channels in rat hippocampal neurons. Research output: ... title = "Bicuculline, pentobarbital and diazepam modulate spontaneous GABA(A) channels in rat hippocampal neurons", ... Exposure of the patches to 100 microM bicuculline caused a gradual decrease on the single-channel conductance of the ...
We offer qualified products for 485-49-4((+)-Bicuculline),please inquire us for 485-49-4((+)-Bicuculline). ... Bicuculline (CAS: 485-49-4) (+)-Bicuculline is a competitive antagonist of GABAA receptors with IC50 of 2 μM, also blocks Ca(2+ ... Bicuculline is a competitive antagonist of GABAA receptors with IC50 of 2 μM, also blocks Ca(2+)-activated potassium channels. ... present study was to examine panic-like elaborated defensive behaviour evoked through GABAA receptor blockade with bicuculline ...
bicuculline ligand page. Quantitative data and detailed annnotation of the targets of licensed and experimental drugs. ...
... bicuculline (0.4 mm), was microinjected into the vlPAG (n = 25). Injection of bicuculline caused inhibition of firing of Aδ- ... Bicuculline methiodide, 0.4 mm, pH 6.0, and a 2% solution of Pontamine Sky Blue (both Sigma-Aldrich) were diluted in aqueous ... The effects of bicuculline are transient and reversed after 30 min, and a further 30 min washout period was allowed. After ... Bicuculline injection into the vlPAG. To identify functional inhibitory projections from the vlPAG to the TCC and to indicate ...
Bicuculline,引用Abcams (+)-Bicuculline (ab120107)的参考文献列表。为您列举引用本产品
... and bicuculline. The protein also contains a number of different allosteric binding sites which modulate the activity of the ... bicuculline, gabazine. Positive allosteric modulators: barbiturates, benzodiazepines, certain carbamates (ex. carisoprodol, ...
Gamma-aminobutyric acid receptor subunit alpha-4 is a protein that in humans is encoded by the GABRA4 gene.[5][6] GABA is the major inhibitory neurotransmitter in the mammalian brain where it acts at GABA-A receptors, which are ligand-gated chloride channels. Chloride conductance of these channels can be modulated by agents such as benzodiazepines that bind to the GABA-A receptor. At least 16 distinct subunits of GABA-A receptors have been identified.[6] ...
Ro4938581 is a nootropic drug invented in 2009 by a team working for Hoffmann-La Roche, which acts as a subtype-selective inverse agonist at the α5 subtype of the benzodiazepine binding site on the GABAA receptor. It has good selectivity for the α5 subtype and did not produce convulsant or anxiogenic effects in animal studies, making it a promising potential nootropic.[1][2][3] Ro4938581 and a related derivative basmisanil (RG-1662, RO5186582) have subsequently been investigated for the alleviation of cognitive dysfunction in Down syndrome.[4][5] ...
The effect in behavioral output may be due to disrupted GABAergic regulation of SNc as bicuculline infusion into vSub, which ... Activation of AIH in MAM rats is blocked by vSub bicuculline infusions. Bicuculline (Bicuc; 12.5 ng in 0.5 µL) infusion into ... The MS activation-induced increase in SNc DA neuron activity was prevented by vSub bicuculline infusion. Bicuculline (Bicuc; ... Bicuculline infusion also prevented the MS activation-induced increase in DA activity in the SNc of MAM rats (N = 7 rats; Fig. ...
The effect of bicuculline (Bic; 10 μM) on the inhibitory effect of pentobarbitone (300 μM) on glutamate efflux is also shown. ... Bicuculline (10 μM) did not antagonize the inhibition of glutamate efflux induced by clomethiazole (Figure 4). In contrast, ... The experiments with bicuculline and picrotoxin further demonstrate that the effect is not due to an action of clomethiazole at ... Results shown as mean±s.e.mean (n=4-9). **Different from Ischaemia (P,0.01). Addition of bicuculline or picrotoxin abolished ...
bicuculline Mass :367.35210 Formula : C20H17NO6 copper(I) chloride Mass :98.99900 Formula : ClCu ...
Bicuculline / pharmacology * Calcium Signaling * Cells, Cultured * Cyclic AMP Response Element-Binding Protein / metabolism* ...
Bicuculline Bicuculline is a naturally occurring GABA antagonist. Procedures for the preparation of bicuculline are described ... Bicuculline has the chemical name (6R)-6-[(5S)-5,6,7,8-tetahydro-6-methyl-1,3-dioxolo[4,5-g]isoquinolin-5-yl]furo[3,4-e]1,3- ... The inhibitory action of gaboxadol on central neurones was reversibly antagonized by the specific GABA antagonist bicuculline ... 2 hours after administration of the bicuculline (control batch: 100% mortality). For each product, the 50% active dose (AD 50 ...
Bicuculline / pharmacology * Calcium-Binding Proteins * Carrier Proteins / genetics * Carrier Proteins / metabolism * Cell ...
  • Bicuculline, pentobarbital and diazepam modulate spontaneous GABA(A) channels in rat hippocampal neurons. (diva-portal.org)
  • We used near infrared spectroscopy (NIRS) to study hemoglobin and cytochrome oxidase changes during seizures, induced by the GABA antagonist bicuculline, in the adult rat. (springer.com)
  • GABA binding and bicuculline in spinal cord and cortical membranes from adult rat and from mouse neurons in cell culture. (harvard.edu)
  • Bicuculline is a neuromodulatory GABA-A receptor antagonist used to study regional variation of GABA receptors and the role of GABA-A receptors in motor disorders, pain, seizure, nociception, anxiety, and memory. (lktlabs.com)
  • Through its inhibition of GABA-A receptors, bicuculline potentiates activation at NMDA receptors and produces membrane depolarization, inhibiting K+ conductance and prolonging Ca2+-dependent action potentials in neurons. (lktlabs.com)
  • In cortical area 3b of monkeys, responses of 71 single neurons to controlled indentations of glabrous skin were recorded before and during iontophoretic application of GABA and bicuculline methiodide (BMI), a GABA receptor antagonist. (springer.com)
  • Poly(A)+ RNA from mammalian retina expresses bicuculline/baclofen-insensitive gamma-aminobutyric acid (GABA) receptors in Xenopus oocytes with properties similar to those of homooligomeric GABA rho 1 receptors. (aspetjournals.org)
  • 100 microM, bicuculline did have some weak competitive inhibitory effects on the GABA rho-like receptors (Kb congruent to 6000), but it was at least 5000 times more potent at GABAA receptors. (aspetjournals.org)
  • Bicuculline insensitive GABA receptors: studies on the binding of (-)-baclofen to rat cerebellar membranes. (thefreedictionary.com)
  • Bicuculline (BIC) is a selective antagonist of GABA[sub]A R, which can inhibit the influence of chloride ions. (thefreedictionary.com)
  • Antagonism of [gamma]-aminobutyric acid (GABA) receptors with bicuculline (BIC) phenocopied the dendrite-promoting effects of PCB-95, and pharmacological antagonism or siRNA knockdown of RyR blocked BIC-induced dendritic growth in dissociated and slice cultures of hippocampal neurons. (thefreedictionary.com)
  • Bicuculline (10 μ M ) abolished the inhibitory effect of GABA (100 μ M ) but not clomethiazole (100 μ M ). Picrotoxin (100 μ M ) abolished the action of both GABA and clomethiazole. (wiley.com)
  • 3. Bicuculline (50 microM) reduced the effects of GABA and abolished the response to isoguvacine without affecting the response to baclofen. (nih.gov)
  • 4. This novel bicuculline-insensitive GABA response was chloride dependent and was blocked by picrotoxin (10-100 microM) in an uncompetitive way. (nih.gov)
  • 5. Towards the end of the second postnatal week, bicuculline blocked the GABA-induced depolarization and revealed a small hyperpolarizing response which was blocked by the GABAB antagonist CGP 35348 (0.5-1 mM). 6. (nih.gov)
  • It is suggested that, during development, the GABA response was mediated through the conventional GABAA and GABAB receptors as well as a new bicuculline-baclofen-insensitive type of receptor. (nih.gov)
  • CryoEM structure of human full-length alpha1beta3gamma2L GABA(A)R in complex with bicuculline and megabody Mb38. (pdbj.org)
  • The active site of the GABAA receptor is the binding site for GABA and several drugs such as muscimol, gaboxadol, and bicuculline. (wikipedia.org)
  • However, seizure aggravation was blocked when the GABA A receptor antagonist, bicuculline (BIC, 0.04 μg in 0.2 μl), was coinjected with CBZ into the VB. (aspetjournals.org)
  • Chorea and related hyperbehavioral disorders may be induced in behaving primates by local microinjections of the GABA A antagonist bicuculline to the globus pallidus externus (GPe). (physiology.org)
  • Treatment of PKCε-null mice with the GABA A receptor antagonist bicuculline restored corticosterone levels and anxiety-like behavior to wild-type levels. (pubmedcentralcanada.ca)
  • It has long been recognized that the fast response of neurons to GABA that is blocked by bicuculline and picrotoxin is due to direct activation of an anion channel. (wikipedia.org)
  • Bicuculline, a convulsant alkaloid, is the antagonist of GABA. (medchemexpress.com)
  • Bicuculline methiodide (BIC-Mel) (10-100 microM) altered the kinetics of N-methyl-D-aspartate (NMDA) responses in single-channel and whole-cell recordings. (aspetjournals.org)
  • We examined the effect of iontophoretic application of bicuculline methiodide and strychnine hydrochloride on the mesencephalic locomotor region (MLR)-induced inhibition of dorsal horn cells in paralyzed cats. (elsevier.com)
  • The protective effects of a series of stable adenosine analogs against generalized seizures inititated by focal injection of bicuculline methiodide into the rat prepiriform cortex (PPC) were studied by microinjection of these compounds into this brain area. (elsevier.com)
  • Quantitative autoradiographic analysis of the distribution of tritiated adenosine agonists 30 min after microinjection in the PPC reveals that [ 3 H]NECA diffuses to a significantly greater extent than R-[ 3 H]PIA, which may contribute to the relatively greater potency of the former compound in suppressing bicuculline methiodide-induced seizures. (elsevier.com)
  • Bicuculline is a phthalide-isoquinoline compound that is a light-sensitive competitive antagonist of GABAA receptors. (wikipedia.org)
  • The action of bicuculline is primarily on the ionotropic GABAA receptors, which are ligand-gated ion channels concerned chiefly with the passing of chloride ions across the cell membrane, thus promoting an inhibitory influence on the target neuron. (wikipedia.org)
  • The half-maximal inhibitory concentration (IC50) of bicuculline on GABAA receptors is 3 μM. (wikipedia.org)
  • Sensitivity to bicuculline is defined by IUPHAR as a major criterion in the definition of GABAA receptors Picrotoxin Hydrastine (very similar in structure) Johnston, Graham AR (2013). (wikipedia.org)
  • Characterization of bicuculline/baclofen-insensitive (rho-like) gamma-aminobutyric acid receptors expressed in Xenopus oocytes. (aspetjournals.org)
  • Bicuculline is a competitive antagonist of GABAA receptors with IC50 of 2 μM, also blocks Ca(2+)-activated potassium channels. (bocsci.com)
  • Pharmacologically, these receptors are antagonized by bicuculline. (utah.edu)
  • Pharmacologically, GABAc receptors are bicuculline- and baclofen-insensitive, and are not modulated by many GABAA receptor modulators (such as benzodiazepines and barbiturates). (utah.edu)
  • citation needed] In addition to being a potent GABAA receptor antagonist, bicuculline can be used to block Ca2+-activated potassium channels. (wikipedia.org)
  • Treatment with the GABAA antagonist, bicuculline, resulted in increased levels of MMP-9, 12 h after drug administration, but no change in levels of MMP-2 up to 3 days following treatment. (ovid.com)
  • In bicuculline and picrotoxin, a GABAB-mediated hyperpolarization appeared. (nih.gov)
  • Picrotoxin, bicuculline, and strychnine are drugs that block inhibitory systems in the brain, leading to a generalized increase in excitability. (encyclopedia.com)
  • Inhibited by the antagonist bicuculline (By similarity). (uniprot.org)
  • Curtis DR, Felix D (1971) The effect of bicuculline upon synaptic inhibition in the cerebral and cerebellar cortices of the cat. (springer.com)
  • Iontophoretic application (10-50 nA) of bicuculline and strychnine (5-10 mM) suppressed the MLR-induced inhibition of transmission of group III afferent input to laminae I and II cells by 69±5% (n=10) and 29±7% (n=7), respectively. (elsevier.com)
  • Likewise, bicuculline and strychnine suppressed the MLR-induced inhibition of transmission of group III afferent input to lamina V cells by 59±13% (n=14) and 39±11% (n=10), respectively. (elsevier.com)
  • Degtyarenko, AM & Kaufman, MP 2003, ' Bicuculline and strychnine suppress the mesencephalic locomotor region-induced inhibition of group III muscle afferent input to the dorsal horn ', Neuroscience , vol. 118, no. 3, pp. 779-788. (elsevier.com)
  • Home Research Outputs Bicuculline, pentobarbital and diazepam modulate spontaneous. (lu.se)
  • To this purpose, bilateral microinjections (30-50 nl) of bicuculline or muscimol were performed into the cVRG of pentobarbital sodium-anesthetized, spontaneously breathing rabbits. (frontiersin.org)
  • Membrane depolarization and prolongation of calcium-dependent action potentials of mouse neurons in cell culture by two convulsants: bicuculline and penicillin. (lktlabs.com)
  • Bicuculline led to an increase in the firing rate and a change in the firing pattern of GPe neurons. (physiology.org)
  • Two types of abnormal neuronal firing patterns were detected in GPe neurons close to the bicuculline microinjection site: continuous high-frequency activity and bistable activity, in which neurons transitioned between high-frequency and complete cessation of firing. (physiology.org)
  • Despite reduction in the information capacity of bicuculline-affected GPe neurons, the ability to encode behavioral events was maintained. (physiology.org)
  • We found similar responses of GPe neurons to bicuculline in vitro in the rat, suggesting a basic cellular mechanism underlying these abnormal firing patterns. (physiology.org)
  • Under voltage-clamp conditions, NPFF and NPVF reversibly and in a concentration-dependent manner reduced the evoked bicuculline-sensitive inhibitory postsynaptic currents (IPSCs) in parvocellular PVN neurons by 25 and 31%, respectively. (physiology.org)
  • Under current-clamp conditions, NPVF and NPFF caused depolarization (6-9 mV) of neurons that persisted in the presence of TTX but was abolished in the presence of bicuculline. (physiology.org)
  • The sneeze reflex induced by mechanical stimulation of the nasal mucosa persisted following bicuculline and muscimol microinjections. (frontiersin.org)
  • However, the number and intensity of expiratory thrusts were enhanced by bicuculline and suppressed by muscimol. (frontiersin.org)
  • Exposure of the patches to 100 microM bicuculline caused a gradual decrease on the single-channel conductance of the spontaneous channels. (diva-portal.org)
  • Naloxone reversed the effects of the higher doses of morphine and fentanyl in all models except bicuculline induced seizures. (nih.gov)
  • We focused on the initial seizures post-bicuculline addition during which oxyhemoglobin (HbO2) increased, deoxyhemoglobin (HHb) decreased and total hemoglobin (Hbtot) increased. (springer.com)
  • Moreover, seizures induce IL-1 (3 release in cortex and hippocampus in bicuculline rat model and further cause blood-brain barrier damage with protein extravasation (Li et al. (thefreedictionary.com)
  • Seizures were induced by intravenous bicuculline. (ahajournals.org)
  • The activity of opioid analgesics in seizure models utilizing N-methyl-DL-aspartic acid, kainic acid, bicuculline and pentylenetetrazole. (nih.gov)
  • Morphine, fentanyl and pethidine exhibited a biphasic dose response relationship with respect to their effects on seizure thresholds to bicuculline, pentylenetetrazole, N-methyl-DL-aspartate (NMDLA) and kainic acid in mice. (nih.gov)
  • Synaptic human full-length a1b3g2L GABAAR in complex with bicuculline and megabody Mb38. (pdbj.org)
  • A similar migration pattern occurred following treatment with bicuculline, which induces synaptic activity. (alzforum.org)
  • Partial recovery of cough responses was achieved after ~3 h or within ~5 min following bicuculline microinjections at the same locations. (frontiersin.org)
  • We performed multielectrode extracellular recordings in the GPe and in the globus pallidus internus (GPi) before, during, and after bicuculline microinjections. (physiology.org)
  • Ionov ID, Roslavtseva LA. Coadministration of bicuculline and NMDA induces paraplegia in the rat. (lktlabs.com)
  • Effects of low doses of bicuculline on N-methyl-D-aspartate single-channel kinetics are not evident in whole-cell currents. (aspetjournals.org)
  • Bicuculline" is a descriptor in the National Library of Medicine's controlled vocabulary thesaurus, MeSH (Medical Subject Headings) . (harvard.edu)
  • Alloway KD, Burton H (1986) Bicuculline-induced alterations in neuronal responses to controlled tactile stimuli in the second somatosensory cortex of the cat: a microiontophoretic study. (springer.com)
  • Bicuculline (1 mM) increased peak abdominal activity and respiratory frequency due to decreases in T E . Cough responses were potentiated mainly owing to increases in the cough number. (frontiersin.org)
  • Electrophysiological recordings of bicuculline- and low Mg 2+ -induced neuronal firing. (sciencemag.org)
  • No obvious degeneration was detected in kainate-treated, non-convulsive rats or bicuculline-treated animals. (ovid.com)
  • Bicuculline infusions advance the timing of luteinizing hormone surge in proestrous rats: comparisons with naloxone effects. (thefreedictionary.com)
  • The effect in behavioral output may be due to disrupted GABAergic regulation of SNc as bicuculline infusion into vSub, which selectively prevented the MS activation-induced decrease in SNc DA activity in intact rats, prevented the increase in AIH and SNc DA activity in MAM rats. (nature.com)
  • Bicuculline (10 μ M ) abolished this effect. (wiley.com)
  • Time-course experiments showed that it took NAC1 as long as 6 hours after bicuculline treatment to reach the dendrites and that levels of the translocated proteins remained elevated for 48 hours after treatment. (alzforum.org)
  • Further, by knocking out NAC1 and also by mutating its binding site, the researchers found that treatments of MG132 and bicuculline no longer budged proteasomes from the nucleus. (alzforum.org)
  • This graph shows the total number of publications written about "Bicuculline" by people in Harvard Catalyst Profiles by year, and whether "Bicuculline" was a major or minor topic of these publication. (harvard.edu)