Transmitter receptors on or near presynaptic terminals (or varicosities) which are sensitive to the transmitter(s) released by the terminal itself. Receptors for the hormones released by hormone-releasing cells are also included.
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.
A subclass of G-protein coupled SEROTONIN receptors that couple preferentially to GI-GO G-PROTEINS resulting in decreased intracellular CYCLIC AMP levels.
A serotonin 1A-receptor agonist that is used experimentally to test the effects of serotonin.
A serotonin receptor subtype found distributed through the CENTRAL NERVOUS SYSTEM where they are involved in neuroendocrine regulation of ACTH secretion. The fact that this serotonin receptor subtype is particularly sensitive to SEROTONIN RECEPTOR AGONISTS such as BUSPIRONE suggests its role in the modulation of ANXIETY and DEPRESSION.
Endogenous compounds and drugs that bind to and activate SEROTONIN RECEPTORS. Many serotonin receptor agonists are used as ANTIDEPRESSANTS; ANXIOLYTICS; and in the treatment of MIGRAINE DISORDERS.
Cell-surface proteins that bind SEROTONIN and trigger intracellular changes which influence the behavior of cells. Several types of serotonin receptors have been recognized which differ in their pharmacology, molecular biology, and mode of action.
A dopamine D2-receptor antagonist. It has been used therapeutically as an antidepressant, antipsychotic, and as a digestive aid. (From Merck Index, 11th ed)
Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT1 RECEPTORS. Included under this heading are agonists for one or more of the specific 5-HT1 receptor subtypes.
A dopamine D2/D3 receptor agonist.
A subfamily of G-PROTEIN-COUPLED RECEPTORS that bind the neurotransmitter DOPAMINE and modulate its effects. D2-class receptor genes contain INTRONS, and the receptors inhibit ADENYLYL CYCLASES.
Drugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or SEROTONIN RECEPTOR AGONISTS.
A biochemical messenger and regulator, synthesized from the essential amino acid L-TRYPTOPHAN. In humans it is found primarily in the central nervous system, gastrointestinal tract, and blood platelets. Serotonin mediates several important physiological functions including neurotransmission, gastrointestinal motility, hemostasis, and cardiovascular integrity. Multiple receptor families (RECEPTORS, SEROTONIN) explain the broad physiological actions and distribution of this biochemical mediator.
An antimuscarinic agent that inhibits gastric secretion at lower doses than are required to affect gastrointestinal motility, salivary, central nervous system, cardiovascular, ocular, and urinary function. It promotes the healing of duodenal ulcers and due to its cytoprotective action is beneficial in the prevention of duodenal ulcer recurrence. It also potentiates the effect of other antiulcer agents such as CIMETIDINE and RANITIDINE. It is generally well tolerated by patients.
A serotonin receptor subtype found at high levels in the BASAL GANGLIA and the frontal cortex. It plays a role as a terminal autoreceptor that regulates the rate of SEROTONIN release from nerve endings. This serotonin receptor subtype is closely related to and has similar drug binding properties as the 5-HT1D RECEPTOR. It is particularly sensitive to the agonist SUMATRIPTAN and may be involved in mediating the drug's antimigraine effect.
A specific subtype of muscarinic receptor found in the lower BRAIN, the HEART and in SMOOTH MUSCLE-containing organs. Although present in smooth muscle the M2 muscarinic receptor appears not to be involved in contractile responses.
A complex group of fibers arising from the basal olfactory regions, the periamygdaloid region, and the septal nuclei, and passing to the lateral hypothalamus. Some fibers continue into the tegmentum.
Endogenous compounds and drugs that bind to and activate GABA-B RECEPTORS.
Drugs that bind to and activate dopamine receptors.
Cell-surface proteins that bind dopamine with high affinity and trigger intracellular changes influencing the behavior of cells.
One of the catecholamine NEUROTRANSMITTERS in the brain. It is derived from TYROSINE and is the precursor to NOREPINEPHRINE and EPINEPHRINE. Dopamine is a major transmitter in the extrapyramidal system of the brain, and important in regulating movement. A family of receptors (RECEPTORS, DOPAMINE) mediate its action.
A benzodioxane alpha-adrenergic blocking agent with considerable stimulatory action. It has been used to diagnose PHEOCHROMOCYTOMA and as an antihypertensive agent.
A subtype of dopamine D2 receptors that are highly expressed in the LIMBIC SYSTEM of the brain.
Drugs that bind to but do not activate GABA-B RECEPTORS thereby blocking the actions of endogenous or exogenous GABA-B RECEPTOR AGONISTS.
The distal terminations of axons which are specialized for the release of neurotransmitters. Also included are varicosities along the course of axons which have similar specializations and also release transmitters. Presynaptic terminals in both the central and peripheral nervous systems are included.
Drugs that bind to but do not activate DOPAMINE RECEPTORS, thereby blocking the actions of dopamine or exogenous agonists. Many drugs used in the treatment of psychotic disorders (ANTIPSYCHOTIC AGENTS) are dopamine antagonists, although their therapeutic effects may be due to long-term adjustments of the brain rather than to the acute effects of blocking dopamine receptors. Dopamine antagonists have been used for several other clinical purposes including as ANTIEMETICS, in the treatment of Tourette syndrome, and for hiccup. Dopamine receptor blockade is associated with NEUROLEPTIC MALIGNANT SYNDROME.
A subclass of alpha-adrenergic receptors found on both presynaptic and postsynaptic membranes where they signal through Gi-Go G-PROTEINS. While postsynaptic alpha-2 receptors play a traditional role in mediating the effects of ADRENERGIC AGONISTS, the subset of alpha-2 receptors found on presynaptic membranes signal the feedback inhibition of NEUROTRANSMITTER release.
Neurotransmitter receptors located on or near presynaptic terminals or varicosities. Presynaptic receptors which bind transmitter molecules released by the terminal itself are termed AUTORECEPTORS.
Drugs that bind to but do not activate SEROTONIN 5-HT1 RECEPTORS, thereby blocking the actions of SEROTONIN 5-HT1 RECEPTOR AGONISTS. Included under this heading are antagonists for one or more of the specific 5-HT1 receptor subtypes.
A serotonin receptor subtype found in the BRAIN; HEART; LUNGS; PLACENTA and DIGESTIVE SYSTEM organs. A number of functions have been attributed to the action of the 5-HT2B receptor including the development of cardiac myocytes (MYOCYTES, CARDIAC) and the contraction of SMOOTH MUSCLE.
Use of electric potential or currents to elicit biological responses.
Compounds that specifically inhibit the reuptake of serotonin in the brain.
A derivative of morphine that is a dopamine D2 agonist. It is a powerful emetic and has been used for that effect in acute poisoning. It has also been used in the diagnosis and treatment of parkinsonism, but its adverse effects limit its use.
Drugs that bind to but do not activate MUSCARINIC RECEPTORS, thereby blocking the actions of endogenous ACETYLCHOLINE or exogenous agonists. Muscarinic antagonists have widespread effects including actions on the iris and ciliary muscle of the eye, the heart and blood vessels, secretions of the respiratory tract, GI system, and salivary glands, GI motility, urinary bladder tone, and the central nervous system.
Neurons whose primary neurotransmitter is SEROTONIN.
A class of histamine receptors discriminated by their pharmacology and mode of action. Histamine H3 receptors were first recognized as inhibitory autoreceptors on histamine-containing nerve terminals and have since been shown to regulate the release of several neurotransmitters in the central and peripheral nervous systems. (From Biochem Soc Trans 1992 Feb;20(1):122-5)
A genus in the subfamily CALLITRICHINAE consisting of 12 species and found in Panama as well as South America. Species seen most frequently in the literature are S. oedipus (cotton-top marmoset), S. nigricollis, and S. fusicollis.
A technique for measuring extracellular concentrations of substances in tissues, usually in vivo, by means of a small probe equipped with a semipermeable membrane. Substances may also be introduced into the extracellular space through the membrane.
Drugs that bind to and block the activation of ADRENERGIC ALPHA-2 RECEPTORS.
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.
Compounds with a six membered aromatic ring containing NITROGEN. The saturated version is PIPERIDINES.
The first highly specific serotonin uptake inhibitor. It is used as an antidepressant and often has a more acceptable side-effects profile than traditional antidepressants.
One of the two major classes of cholinergic receptors. Muscarinic receptors were originally defined by their preference for MUSCARINE over NICOTINE. There are several subtypes (usually M1, M2, M3....) that are characterized by their cellular actions, pharmacology, and molecular biology.
A subset of GABA RECEPTORS that signal through their interaction with HETEROTRIMERIC G-PROTEINS.
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.
Agents that inhibit the actions of the parasympathetic nervous system. The major group of drugs used therapeutically for this purpose is the MUSCARINIC ANTAGONISTS.
Semisynthetic derivative of ergot (Claviceps purpurea). It has complex effects on serotonergic systems including antagonism at some peripheral serotonin receptors, both agonist and antagonist actions at central nervous system serotonin receptors, and possibly effects on serotonin turnover. It is a potent hallucinogen, but the mechanisms of that effect are not well understood.
The middle of the three primitive cerebral vesicles of the embryonic brain. Without further subdivision, midbrain develops into a short, constricted portion connecting the PONS and the DIENCEPHALON. Midbrain contains two major parts, the dorsal TECTUM MESENCEPHALI and the ventral TEGMENTUM MESENCEPHALI, housing components of auditory, visual, and other sensorimoter systems.
An anxiolytic agent and serotonin receptor agonist belonging to the azaspirodecanedione class of compounds. Its structure is unrelated to those of the BENZODIAZAPINES, but it has an efficacy comparable to DIAZEPAM.
Inorganic or organic derivatives of phosphinic acid, H2PO(OH). They include phosphinates and phosphinic acid esters.
Drugs that bind to but do not activate GABA RECEPTORS, thereby blocking the actions of endogenous GAMMA-AMINOBUTYRIC ACID and GABA RECEPTOR AGONISTS.
A moderately lipophilic beta blocker (ADRENERGIC BETA-ANTAGONISTS). It is non-cardioselective and has intrinsic sympathomimetic actions, but little membrane-stabilizing activity. (From Martindale, The Extra Pharmocopoeia, 30th ed, p638)
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.
A group of compounds consisting in part of two rings sharing one atom (usually a carbon) in common.
A synthetic nondepolarizing blocking drug. The actions of gallamine triethiodide are similar to those of TUBOCURARINE, but this agent blocks the cardiac vagus and may cause sinus tachycardia and, occasionally, hypertension and increased cardiac output. It should be used cautiously in patients at risk from increased heart rate but may be preferred for patients with bradycardia. (From AMA Drug Evaluations Annual, 1992, p198)
Beta-Sulfoalanine. An amino acid with a C-terminal sulfonic acid group which has been isolated from human hair oxidized with permanganate. It occurs normally in the outer part of the sheep's fleece, where the wool is exposed to light and weather.
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.
Pinched-off nerve endings and their contents of vesicles and cytoplasm together with the attached subsynaptic area of the membrane of the post-synaptic cell. They are largely artificial structures produced by fractionation after selective centrifugation of nervous tissue homogenates.
A beta-hydroxylated derivative of phenylalanine. The D-form of dihydroxyphenylalanine has less physiologic activity than the L-form and is commonly used experimentally to determine whether the pharmacological effects of LEVODOPA are stereospecific.
Drugs that bind to but do not activate alpha-adrenergic receptors thereby blocking the actions of endogenous or exogenous adrenergic agonists. Adrenergic alpha-antagonists are used in the treatment of hypertension, vasospasm, peripheral vascular disease, shock, and pheochromocytoma.
Endogenous compounds and drugs that bind to and activate GAMMA-AMINOBUTYRIC ACID receptors (RECEPTORS, GABA).
Sodium chloride-dependent neurotransmitter symporters located primarily on the PLASMA MEMBRANE of noradrenergic neurons. They remove NOREPINEPHRINE from the EXTRACELLULAR SPACE by high affinity reuptake into PRESYNAPTIC TERMINALS. It regulates signal amplitude and duration at noradrenergic synapses and is the target of ADRENERGIC UPTAKE INHIBITORS.
Striped GRAY MATTER and WHITE MATTER consisting of the NEOSTRIATUM and paleostriatum (GLOBUS PALLIDUS). It is located in front of and lateral to the THALAMUS in each cerebral hemisphere. The gray substance is made up of the CAUDATE NUCLEUS and the lentiform nucleus (the latter consisting of the GLOBUS PALLIDUS and PUTAMEN). The WHITE MATTER is the INTERNAL CAPSULE.
A specific subtype of muscarinic receptor found in the CORPUS STRIATUM and the LUNG. It has similar receptor binding specificities to MUSCARINIC RECEPTOR M1 and MUSCARINIC RECEPTOR M2.
Drugs that block the transport of DOPAMINE into axon terminals or into storage vesicles within terminals. Most of the ADRENERGIC UPTAKE INHIBITORS also inhibit dopamine uptake.
Drugs that bind to and activate excitatory amino acid receptors.
Partially saturated 1,2,3,4-tetrahydronaphthalene compounds.
The making of a radiograph of an object or tissue by recording on a photographic plate the radiation emitted by radioactive material within the object. (Dorland, 27th ed)
Organic chemicals which have two amino groups in an aliphatic chain.
Cell surface proteins that bind glutamate and act through G-proteins to influence second messenger systems. Several types of metabotropic glutamate receptors have been cloned. They differ in pharmacology, distribution, and mechanisms of action.
A non-essential amino acid naturally occurring in the L-form. Glutamic acid is the most common excitatory neurotransmitter in the CENTRAL NERVOUS SYSTEM.
Precursor of epinephrine that is secreted by the adrenal medulla and is a widespread central and autonomic neurotransmitter. Norepinephrine is the principal transmitter of most postganglionic sympathetic fibers and of the diffuse projection system in the brain arising from the locus ceruleus. It is also found in plants and is used pharmacologically as a sympathomimetic.
A neurotransmitter found at neuromuscular junctions, autonomic ganglia, parasympathetic effector junctions, a subset of sympathetic effector junctions, and at many sites in the central nervous system.
Sodium chloride-dependent neurotransmitter symporters located primarily on the PLASMA MEMBRANE of dopaminergic neurons. They remove DOPAMINE from the EXTRACELLULAR SPACE by high affinity reuptake into PRESYNAPTIC TERMINALS and are the target of DOPAMINE UPTAKE INHIBITORS.
Drugs that selectively bind to and activate alpha adrenergic receptors.
Drugs that bind to but do not activate excitatory amino acid receptors, thereby blocking the actions of agonists.
Biogenic amines having only one amine moiety. Included in this group are all natural monoamines formed by the enzymatic decarboxylation of natural amino acids.
Tryptamine substituted with two hydroxyl groups in positions 5 and 7. It is a neurotoxic serotonin analog that destroys serotonergic neurons preferentially and is used in neuropharmacology as a tool.
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.
An imidazoline sympatholytic agent that stimulates ALPHA-2 ADRENERGIC RECEPTORS and central IMIDAZOLINE RECEPTORS. It is commonly used in the management of HYPERTENSION.
Sodium chloride-dependent neurotransmitter symporters located primarily on the PLASMA MEMBRANE of serotonergic neurons. They are different than SEROTONIN RECEPTORS, which signal cellular responses to SEROTONIN. They remove SEROTONIN from the EXTRACELLULAR SPACE by high affinity reuptake into PRESYNAPTIC TERMINALS. Regulates signal amplitude and duration at serotonergic synapses and is the site of action of the SEROTONIN UPTAKE INHIBITORS.
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 furancarbonitrile that is one of the SEROTONIN UPTAKE INHIBITORS used as an antidepressant. The drug is also effective in reducing ethanol uptake in alcoholics and is used in depressed patients who also suffer from tardive dyskinesia in preference to tricyclic antidepressants, which aggravate this condition.
A serotonin agonist that acts selectively at 5HT1 receptors. It is used in the treatment of MIGRAINE DISORDERS.
The relationship between the dose of an administered drug and the response of the organism to the drug.
A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.
Drugs that bind to but do not activate GABA-A RECEPTORS thereby blocking the actions of endogenous or exogenous GABA-A RECEPTOR AGONISTS.
Interstitial space between cells, occupied by INTERSTITIAL FLUID as well as amorphous and fibrous substances. For organisms with a CELL WALL, the extracellular space includes everything outside of the CELL MEMBRANE including the PERIPLASM and the cell wall.
The part of CENTRAL NERVOUS SYSTEM that is contained within the skull (CRANIUM). Arising from the NEURAL TUBE, the embryonic brain is comprised of three major parts including PROSENCEPHALON (the forebrain); MESENCEPHALON (the midbrain); and RHOMBENCEPHALON (the hindbrain). The developed brain consists of CEREBRUM; CEREBELLUM; and other structures in the BRAIN STEM.
A serotonin uptake inhibitor that is effective in the treatment of depression.
A non-hydrolyzed muscarinic agonist used as a research tool.
The black substance in the ventral midbrain or the nucleus of cells containing the black substance. These cells produce DOPAMINE, an important neurotransmitter in regulation of the sensorimotor system and mood. The dark colored MELANIN is a by-product of dopamine synthesis.
Bluish-colored region in the superior angle of the FOURTH VENTRICLE floor, corresponding to melanin-like pigmented nerve cells which lie lateral to the PERIAQUEDUCTAL GRAY.
Drugs that bind to and activate muscarinic cholinergic receptors (RECEPTORS, MUSCARINIC). Muscarinic agonists are most commonly used when it is desirable to increase smooth muscle tone, especially in the GI tract, urinary bladder and the eye. They may also be used to reduce heart rate.
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.
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.
One of the FURANS with a carbonyl thereby forming a cyclic lactone. It is an endogenous compound made from gamma-aminobutyrate and is the precursor of gamma-hydroxybutyrate. It is also used as a pharmacological agent and solvent.
A common name used for the genus Cavia. The most common species is Cavia porcellus which is the domesticated guinea pig used for pets and biomedical research.
The function of opposing or restraining the excitation of neurons or their target excitable cells.
Ovoid body resting on the CRIBRIFORM PLATE of the ethmoid bone where the OLFACTORY NERVE terminates. The olfactory bulb contains several types of nerve cells including the mitral cells, on whose DENDRITES the olfactory nerve synapses, forming the olfactory glomeruli. The accessory olfactory bulb, which receives the projection from the VOMERONASAL ORGAN via the vomeronasal nerve, is also included here.
A family of hexahydropyridines.
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.
The most common inhibitory neurotransmitter in the central nervous system.
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.
A class of ionotropic glutamate receptors characterized by their affinity for KAINIC ACID.
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.
Extensions of the nerve cell body. They are short and branched and receive stimuli from other NEURONS.
Collection of pleomorphic cells in the caudal part of the anterior horn of the LATERAL VENTRICLE, in the region of the OLFACTORY TUBERCLE, lying between the head of the CAUDATE NUCLEUS and the ANTERIOR PERFORATED SUBSTANCE. It is part of the so-called VENTRAL STRIATUM, a composite structure considered part of the BASAL GANGLIA.
Changes in the amounts of various chemicals (neurotransmitters, receptors, enzymes, and other metabolites) specific to the area of the central nervous system contained within the head. These are monitored over time, during sensory stimulation, or under different disease states.
The action of a drug that may affect the activity, metabolism, or toxicity of another drug.
One of the two major pharmacological subdivisions of adrenergic receptors that were originally defined by the relative potencies of various adrenergic compounds. The alpha receptors were initially described as excitatory receptors that post-junctionally stimulate SMOOTH MUSCLE contraction. However, further analysis has revealed a more complex picture involving several alpha receptor subtypes and their involvement in feedback regulation.
Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).
A class of ionotropic glutamate receptors characterized by their affinity for the agonist AMPA (alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid).

Somatic recording of GABAergic autoreceptor current in cerebellar stellate and basket cells. (1/158)

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)

S-16924 [(R)-2-[1-[2-(2,3-dihydro-benzo[1,4]dioxin-5-yloxy)-ethyl]- pyrrolidin-3yl]-1-(4-fluorophenyl)-ethanone], a novel, potential antipsychotic with marked serotonin1A agonist properties: III. Anxiolytic actions in comparison with clozapine and haloperidol. (2/158)

S-16924 is a potential antipsychotic that displays agonist and antagonist properties at serotonin (5-HT)1A and 5-HT2A/2C receptors, respectively. In a pigeon conflict procedure, the benzodiazepine clorazepate (CLZ) increased punished responses, an action mimicked by S-16924, whereas the atypical antipsychotic clozapine and the neuroleptic haloperidol were inactive. Similarly, in a Vogel conflict paradigm in rats, CLZ increased punished responses, an action shared by S-16924 but not by clozapine or haloperidol. This action of S-16924 was abolished by the 5-HT1A antagonist WAY-100,635. Ultrasonic vocalizations in rats were inhibited by CLZ, S-16924, clozapine, and haloperidol. However, although WAY-100,635 abolished the action of S-16924, it did not affect clozapine and haloperidol. In a rat elevated plus-maze, CLZ, but not S-16924, clozapine, and haloperidol, increased open-arm entries. Like CLZ, S-16924 increased social interaction in rats, whereas clozapine and haloperidol were inactive. WAY-100,635 abolished this action of S-16924. CLZ, S-16924, clozapine, and haloperidol decreased aggressive interactions in isolated mice, but this effect of S-16924 was not blocked by WAY-100, 635. All drugs inhibited motor behavior, but the separation to anxiolytic doses was more pronounced for S-16924 than for CLZ. Finally, in freely moving rats, CLZ and S-16924, but not clozapine and haloperidol, decreased dialysis levels of 5-HT in the nucleus accumbens: this action of S-16924 was blocked by WAY-100,165. In conclusion, in contrast to haloperidol and clozapine, S-16924 possessed a broad-based profile of anxiolytic activity at doses lower than those provoking motor disruption. Its principal mechanism of action was activation of 5-HT1A (auto)receptors.  (+info)

In vivo assessment of the midbrain raphe nuclear regulation of serotonin release in the hamster suprachiasmatic nucleus. (3/158)

Serotonin (5-HT) plays important regulatory roles in mammalian circadian timekeeping; however, little is known concerning the regulation of serotonergic activity in the circadian clock located in the suprachiasmatic nuclei (SCN). By using in vivo microdialysis to measure 5-HT release we demonstrated that electrical or pharmacological stimulations of the dorsal or median raphe nuclei (DRN and MRN, respectively) can alter basal release of 5-HT in the hamster SCN. There were similar increases in SCN 5-HT release after electrical stimulation of either the MRN or DRN, indicating that both could contribute to the serotonergic activity in the SCN. Systemic pretreatment with the 5-HT antagonist metergoline abolished DRN-induced SCN 5-HT release but had little effect on MRN-induced SCN 5-HT release, suggesting different pathways for these nuclei in regulating 5-HT output in the SCN. Microinjections of the 5-HT1A autoreceptor agonist 8-OH-DPAT or antagonist WAY 100635 into the MRN caused significant inhibition and stimulation of SCN 5-HT release, respectively. Both drugs had substantially less effect in the DRN. These differential drug actions indicate that somatodendritic 5-HT1A autoreceptors on MRN neurons provide the prominent raphe autoregulation of 5-HT output in the SCN. Collectively the current results are evidence that DRN as well as MRN neurons can contribute to the regulation of 5-HT release in the hamster SCN. On the basis of the current observations and those from recent anatomic tracing studies of serotonergic projections to SCN it is hypothesized that DRN input to the SCN could be mediated by a DRN --> MRN --> SCN pathway involving a 5-HT-sensitive multisynaptic interaction between the DRN and MRN neurons.  (+info)

Comparison of antagonist potencies at pre- and post-synaptic GABA(B) receptors at inhibitory synapses in the CA1 region of the rat hippocampus. (4/158)

Synaptic activation of gamma-aminobutyric acid (GABA)B receptors at GABA synapses causes (a) postsynaptic hyperpolarization mediating a slow inhibitory postsynaptic potential/current (IPSP/C) and (b) presynaptic inhibition of GABA release which depresses IPSPs and leads to paired-pulse widening of excitatory postsynaptic potentials (EPSPs). To address whether these effects are mediated by pharmacologically identical receptors the effects of six GABA(B) receptor antagonists of widely ranging potencies were tested against each response. Monosynaptic IPSP(B)s were recorded in the presence of GABA(A), AMPA/kainate and NMDA receptor antagonists. All GABA(B) receptor antagonists tested depressed the IPSP(B) with an IC50 based rank order of potency of CGP55679> or =CGP56433 = CGP55845A = CGP52432>CGP51176>CGP36742. Paired-pulse EPSP widening was recorded as an index of paired-pulse depression of GABA-mediated IPSP/Cs. A similar rank order of potency of antagonism of paired-pulse widening was observed to that for IPSP(B) inhibition. Comparison of the IC50 values for IPSP(B) inhibition and paired-pulse EPSP widening revealed a close correlation between the two effects in that their IC50s lay within the 95% confidence limits of a correlation line that described IC50 values for inhibition of paired-pulse EPSP widening that were 7.3 times higher than those for IPSP(B) inhibition. Using the compounds tested here it is not possible to assign different subtypes of GABA(B) receptor to pre- and post-synaptic loci at GABAergic synapses. However, 5-10 fold higher concentrations of antagonist are required to block presynaptic as opposed to postsynaptic receptors when these are activated by synaptically released GABA.  (+info)

Diurnal variation in 5-HT1B autoreceptor function in the anterior hypothalamus in vivo: effect of chronic antidepressant drug treatment. (5/158)

1. Intracerebral microdialysis was used to examine the function of the terminal 5-hydroxytryptamine (5-HT) autoreceptor in the anterior hypothalamus of anaesthetized rats at two points in the light phase of the light-dark cycle. 2. Infusion of the 5-HT1A/1B agonist 5-methoxy-3-(1,2,3,6-tetrahydro-4-pyridyl)-1H-indole (RU24969) 0.1, 1.0 and 10 microM through the microdialysis probe led to a concentration-dependent decrease (49, 56 and 65% respectively) in 5-HT output. The effect of RU24969 (1 and 5 microM) was prevented by concurrent infusion of methiothepin (1 and 10 microM) into the anterior hypothalamus via the microdialysis probe. Infusion of methiothepin alone (1.0 and 10 microM) increased (15 and 142% respectively) 5-HT output. 3. Infusion of RU24969 (5 microM) through the probe at mid-light and end-light resulted in a quantitatively greater decrease in 5-HT output at end-light compared with mid-light. 4. Following treatment with either paroxetine hydrochloride (10 mg kg(-1) i.p.) or desipramine hydrochloride (10 mg kg)(-1) i.p.) for 21 days the function of the terminal 5-HT1B autoreceptor was more markedly attenuated at end-light. 5. The data show that, as defined by the response to RU24969, the function of the 5-HT1B receptors that control 5-HT output in the anterior hypothalamus is attenuated following chronic desipramine or paroxetine treatment in a time-of-day-dependent manner.  (+info)

Differential cotransmission in sympathetic nerves: role of frequency of stimulation and prejunctional autoreceptors. (6/158)

Recent reports have suggested that sympathetic nerves may store separately and release independently the cotransmitters ATP and norepinephrine (NE). It is conceivable therefore that the quantity of each neurotransmitter that is released from the nerves is not fixed but rather may vary, possibly with the frequency of stimulation. To test this hypothesis we studied the concomitant release at various frequencies and cooperative postjunctional actions of ATP and NE during the first 10 s of electrical field stimulation of the guinea pig vas deferens. We found that at lower frequencies (8 Hz), prejunctional inhibition of the release of NE, which occurs via alpha2-adrenoceptors, modulates the ultimate composition of the cocktail of cotransmitters by limiting the amount of NE that is coreleased with ATP. As the frequency of stimulation increases (above 8 Hz), the autoinhibition of the release of NE is overridden and the amount of NE relative to ATP increases. The smooth muscle of the guinea pig vas deferens reacts to changes in composition of the sympathetic neurochemical messages by increasing the amplitude of its contractions due to the enhancement by NE of the contractile responses triggered by ATP. This evidence suggests that the prejunctional alpha2-adrenoceptor may function as a sensor that "reads" the frequency of action potentials produced during a burst of neuronal activity and converts that information into discrete neurochemical messages with varying proportions of cotransmitters. The mechanism for decoding the informational content of these messages is based on the cooperative postjunctional interactions of the participating cotransmitters.  (+info)

Moxonidine, a selective alpha2-adrenergic and imidazoline receptor agonist, produces spinal antinociception in mice. (7/158)

alpha2-Adrenergic receptor (AR)-selective compounds produce antihypertensive and antinociceptive effects. Moxonidine alleviates hypertension in multiple species, including humans. This study demonstrates that intrathecally administered moxonidine produces antinociception in mice. Antinociception was detected via the (52.5 degrees C) tail-flick and Substance P (SP) nociceptive tests. Moxonidine was intrathecally administered to ICR, mixed C57BL/6 x 129/Sv [wild type (WT)], or C57BL/6 x 129/Sv mice with dysfunctional alpha2aARs (D79N-alpha2a). The alpha2AR-selective antagonist SK&F 86466 and the mixed I1/alpha2AR-selective antagonist efaroxan were tested for inhibition of moxonidine-induced antinociception. Moxonidine prolonged tail-flick latencies in ICR (ED50 = 0.5 nmol; 0. 3-0.7), WT (0.17 nmol; 0.09-0.32), and D79N-alpha2a (0.32 nmol; 0. 074-1.6) mice. Moxonidine inhibited SP-elicited behavior in ICR (0. 04 nmol; 0.03-0.07), WT (0.4 nmol; 0.3-0.5), and D79N-alpha2a (1.1 nmol; 0.7-1.7) mice. Clonidine produced antinociception in WT but not D79N-alpha2a mice. SK&F 86466 and efaroxan both antagonized moxonidine-induced inhibition of SP-elicited behavior in all mouse lines. SK&F 86466 antagonism of moxonidine-induced antinociception implicates the participation of alpha2ARs. The comparable moxonidine potency between D79N-alpha2a and WT mice suggests that receptors other than alpha2a mediate moxonidine-induced antinociception. Conversely, absence of clonidine efficacy in D79N-alpha2a mice implies that alpha2aAR activation enables clonidine-induced antinociception. When clinically administered, moxonidine induces fewer side effects relative to clonidine; moxonidine-induced antinociception appears to involve a different alpha2AR subtype than clonidine-induced antinociception. Therefore, moxonidine may prove to be an effective treatment for pain with an improved side effect profile.  (+info)

Characterization of binding sequences for butyrolactone autoregulator receptors in streptomycetes. (8/158)

BarA of Streptomyces virginiae is a specific receptor protein for a member of butyrolactone autoregulators which binds to an upstream region of target genes to control transcription, leading to the production of the antibiotic virginiamycin M(1) and S. BarA-binding DNA sequences (BarA-responsive elements [BAREs]), to which BarA binds for transcriptional control, were restricted to 26 to 29-nucleotide (nt) sequences on barA and barB upstream regions by the surface plasmon resonance technique, gel shift assay, and DNase I footprint analysis. Two BAREs (BARE-1 and BARE-2) on the barB upstream region were located 57 to 29 bp (BARE-1) and 268 to 241 bp (BARE-2) upstream from the barB translational start codon. The BARE located on the barA upstream region (BARE-3) was found 101 to 76 bp upstream of the barA start codon. High-resolution S1 nuclease mapping analysis revealed that BARE-1 covered the barB transcription start site and BARE-3 covered an autoregulator-dependent transcription start site of the barA gene. Deletion and mutation analysis of BARE-2 demonstrated that at least a 19-nt sequence was required for sufficient BarA binding, and A or T residues at the edge as well as internal conserved nucleotides were indispensable. The identified binding sequences for autoregulator receptor proteins were found to be highly conserved among Streptomyces species.  (+info)

Dive into the research topics of Mobility of NMDA autoreceptors but not postsynaptic receptors at glutamate synapses in the rat entorhinal cortex. Together they form a unique fingerprint. ...
A heteroreceptor is a receptor regulating the synthesis and/or the release of mediators other than its own ligand. Heteroreceptors are receptors that respond to neurotransmitters, neuromodulators, or neurohormones released from adjacent neurons or cells; they are opposite to autoreceptors, which are sensitive only to neurotransmitters or hormones released by the cell in whose wall they are embedded. Norepinephrine can influence the release of acetylcholine from parasympathetic neurons by acting on α2 adrenergic (α2A, α2B, and α2C) heteroreceptors. Acetylcholine can influence the release of norepinephrine from sympathetic neurons by acting on muscarinic-2 and muscarinic-4 heteroreceptors. CB1 negatively modulates the release of GABA and glutamate, playing a crucial role in maintaining a homeostasis between excitatory and inhibitory transmission. Glutamate released from an excitatory neuron escapes from the synaptic cleft and preferentially affects mGluR III receptors on the presynaptic ...
SDZ 216,525 has been proposed to be a silent 5-HT1A receptor antagonist. The present study examined the potential intrinsic agonist action of SDZ 216,525 using two in vivo models of somatodendritic 5-HT1A autoreceptor function: 5-HT release using microdialysis and feeding behaviour of satiated animals. SDZ 216,525 (1 mg/kg s.c.) and the alpha 1-adrenoceptor antagonist prazosin (1 mg/kg s.c.) significantly decreased hippocampal 5-HT release. In addition, SDZ 216,525 (3 and 10 mg/kg s.c.) and prazosin (3 and 10 mg/kg s.c.) significantly increased food intake in satiated rats. The selective 5-HT1A receptor antagonist (RS)-WAY100135 (10 mg/kg s.c.) which has been demonstrated to block the effects of 8-OH-DPAT on 5-HT release and food intake had no significant effect on the response induced by SDZ 216,525. In contrast, the non-selective 5-HT1A receptor antagonist (-)-pindolol (8 mg/kg s.c.) attenuated both SDZ 216,525 responses. The decrease in hippocampal 5-HT release and increase in food intake induced by
I am not an expert either, but there are post-synaptic receptors (the ones that exert the main effect of the neurotransmitter) and there are pre-synaptic autoreceptors and heteroreceptors which affect the release of the neurotransmitter.. So, for example, if you take a reuptake inhibitor, you immediately increase the amount of neurotransmitter in the synapse. However, this activates the post-synaptic receptors and the autoreceptors. When the autoreceptors are activated, this slows the firing / release of the neurotransmitter from the presynaptic neuron.. Over time, the autoreceptors can desensitize which can result in increased firing.. Take, for example clonidine. It is a blood pressure medication which slows the release of norepinephrine. It does this by activating a specific norepinephrine autoreceptor (alpha-2). This receptor can also be activated by norepinephrine itself to slow the release of more neurotransmitter.. Mirtazapine and yohimbine block this same adrenaline receptor, which ...
I am not an expert either, but there are post-synaptic receptors (the ones that exert the main effect of the neurotransmitter) and there are pre-synaptic autoreceptors and heteroreceptors which affect the release of the neurotransmitter.. So, for example, if you take a reuptake inhibitor, you immediately increase the amount of neurotransmitter in the synapse. However, this activates the post-synaptic receptors and the autoreceptors. When the autoreceptors are activated, this slows the firing / release of the neurotransmitter from the presynaptic neuron.. Over time, the autoreceptors can desensitize which can result in increased firing.. Take, for example clonidine. It is a blood pressure medication which slows the release of norepinephrine. It does this by activating a specific norepinephrine autoreceptor (alpha-2). This receptor can also be activated by norepinephrine itself to slow the release of more neurotransmitter.. Mirtazapine and yohimbine block this same adrenaline receptor, which ...
TY - JOUR. T1 - Modulation of acetylcholine release by muscarinic autoreceptors in the CNS. T2 - Determination by in vivo and in vitro experimental systems. AU - Suzuki, T.. AU - Hayakawa, T.. AU - Kashima, Y.. AU - Fujimoto, K.. AU - Oohata, H.. AU - Kawashima, K.. PY - 1990/1/1. Y1 - 1990/1/1. UR - http://www.scopus.com/inward/record.url?scp=0024987967&partnerID=8YFLogxK. UR - http://www.scopus.com/inward/citedby.url?scp=0024987967&partnerID=8YFLogxK. U2 - 10.1016/0014-2999(90)92280-V. DO - 10.1016/0014-2999(90)92280-V. M3 - Article. AN - SCOPUS:0024987967. VL - 183. JO - European Journal of Pharmacology. JF - European Journal of Pharmacology. SN - 0014-2999. IS - 5. ER - ...
initially starts with bradycardia (because affecting M2 presynaptic autoreceptors, and then tachycardia when it starts to affect M2 postsynaptic) ...
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1. Gean CJ & Meyers FH: Pocket Drug Guide, 2nd ed. Williams & Wilkins, Baltimore, MD; 1997. 2. Tyler VE: The New Honest Herbal. GF Stickley Co, Philadelphia, PA; 1987. 3. Fleming T (ed): PDR for Herbal Medicines. Medical Economics Company, Montvale, NJ; 1998. 4. Anon: Yohimbine hydrochloride. Mosby Inc; 1998. Available at: http://www.Rxlist.com (cited 1/6/00). 5. McGuffin M, Hobbs C, Upton R et al: Botanical Safety Handbook. CRC Press, Boca Raton, FL; 1997. 6. Lacomblez L, Bensimon G, Isnard F et al: Effect of yohimbine on blood pressure in patients with depression and orthostatic hypotension induced by clomipramine. Clin Pharmacol Ther 1989; 45(3):241-251. 7. Charney DS, Heninger GR, & Sternberg DE: Assessment of alpha-2 adrenergic autoreceptor function in humans: effect of oral yohimbine. Life Sci 1982; 30(23):2033-2041. 8. Tyler VE: Herbs of Choice: The Therapeutic use of phytomedicinals. Pharmaceutical Products Press, New York, NY; 1991. 9. Price J & Grunhaus LJ: Treatment of ...
Several types of D2R and D1R heteroreceptor complexes were discovered in the indirect and direct pathways of the striatum, respectively. Changes in the functio...
We discuss the steady state of the model and the steady state distribution of extracellular serotonin under different hypotheses on the autoreceptors and we show the effect of tryptophan input on the steady state and the effect of meals. We use the deterministic model to interpret experimental data on the responses in the hippocampus of male and female mice, and to illustrate the short-time dynamics of the autoreceptors. We show there are likely two reuptake mechanisms for serotonin and that the autoreceptors have long-lasting influence and compare our results to measurements of serotonin dynamics in the substantia nigra pars reticulata. We also show how histamine affects serotonin dynamics. We examine experimental data that show very variable response curves in populations of mice and ask how much variation in parameters in the model is necessary to produce the observed variation in the data. Finally, we show how the systems population model can potentially be used to investigate specific ...
expression of D2S as the exclusive autoreceptor was insufficient for cocaine-induced plasticity, implying a functional role for the co-expression of D2S and D2L ...
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BACKGROUND AND PURPOSEF15599, a novel 5-hydroxytryptamine (5-HT)(1A) receptor agonist with 1000-fold selectivity for 5-HT compared with other monoamine receptors, shows antidepressant and procognitive activity at very low doses in animal models. We examined the in vivo activity of F15599 at somatodendritic autoreceptors and postsynaptic 5-HT(1A) heteroreceptors.EXPERIMENTAL APPROACHIn vivo single unit and local field potential recordings and microdialysis in the rat.KEY RESULTSF15599 increased the discharge rate of pyramidal neurones in medial prefrontal cortex (mPFC) from 0.2 microg x kg(-1) i.v and reduced that of dorsal raphe 5-hydroxytryptaminergic neurones at doses ,10-fold higher (minimal effective dose 8.2 microg x kg(-1) i.v.). Both effects were reversed by the 5-HT(1A) antagonist (+/-)WAY100635. F15599 did not alter low frequency oscillations (approximately 1 Hz) in mPFC. In microdialysis studies, F15599 increased dopamine output in mPFC (an effect dependent on the activation of ...
CB1 receptor je presinaptički heteroreceptor koji moduliše otpuštanje neurotransmitera kad je aktiviran. On funkcioniše na način koji je zavistan od doze, stereoselektivan i senzitivan na pertuzijski toksin.[3] CB1 receptor aktiviraju kanabinoidi, prirodno formirani u telu (Endokanabinoidi) ili uneseni kao kanabis ili srodno sintetičko jedinjenje.. Iz istraživanja proizilazi da je većina CB1 receptora spregnuta sa Gi/o proteinima. Pri aktivaciji, CB1 receptor deluje prvenstveno putem aktivacije Gi, čime se snižava intracelularna cAMP koncentracija putem inhibicije enzima za njegovu produkciju, adenilat ciklaze, i povišava koncentracija mitogenom-aktivirane proteinske kinaze (MAP kinaze). Alternativno, u nekim retkim slučajevima aktivacija CB1 receptora može da bude spregnuta sa Gs proteinima, koji stimulišu adenilat ciklazu.[2] Poznato je da cAMP služi kao sekundarni glasnik koji se spreže sa mnoštvom jonskih kanala, uključujući unutrašnje ispravljajuće kalijumske kanale ...
Fara efect de masca si fara a incarca pielea, crema nuantatoare pentru ten deschis acopera si camufleaza intr-un mod natural micile imperfectiuni, este antioxidanta si permite o hidratare optima a pielii. Confera un efect natural si asigura un ten mat si omogen.
Detalii Prezentare: 30 tablete Producator: Nature
Alcachofa de Laon reprezinta o modalitate simpla si inovatoare de detoxifiere care va ajuta sa slabiti sanatos intr-un timp scurt si fara efecte nocive asupra organismului.
Orexin B is a hypothalamatic neuropeptide stimulating food intake in rats. Orexin B activates OX2 receptors. Both OX1 and OX2 receptors are involved in maintaining arousal. OX2 receptors appear to be inhibitory autoreceptors on orexin-containing neurons. Orexin B stimulates food consumption i...
Masina multifunctionala MAKITA DUX18Z fara acumulator, compatibila cu LXT 18V, 430 W, 3.1 kg Masina multifunctionala DUX18Z MAKITA, fara acumulator Masina multifunctionala DUX18Z de la Makita este utilizata in regim profesional pentru defrisarea terenu
FARA members will automatically be assigned to the chapter where they are located. Alarm companies and vendors that do business throughout the chapters will be members of all Chapters. There is no charge for belonging to a chapter - it will be part of your FARA Membership.. Meetings will be virtual and open to any chapter member. More details and meeting schedules will be announced soon. ...
Produsul este un tonic general al organismului, datorita proprietatilor vitaminizante. Intareste imunitatea organismului si contribuie la reglarea metabolismului.
Dopamine (DA) transmission is governed by processes that regulate release from axonal boutons in the forebrain and the somatodendritic compartment in midbrain, and by clearance by the DA transporter, diffusion, and extracellular metabolism. We review how axonal DA release is regulated by neuronal activity and by autoreceptors and heteroreceptors, and address how quantal release events are regulated in size and frequency. In brain regions densely innervated by DA axons, DA clearance is due predominantly to uptake by the DA transporter, whereas in cortex, midbrain, and other regions with relatively sparse DA inputs, the norepinephrine transporter and diffusion are involved. We discuss the role of DA uptake in restricting the sphere of influence of DA and in temporal accumulation of extracellular DA levels upon successive action potentials. The tonic discharge activity of DA neurons may be translated into a tonic extracellular DA level, whereas their bursting activity can generate discrete extracellular DA
© 2017 Elsevier B.V. Dopamine (DA) transmission is governed by processes that regulate release from axonal boutons in the forebrain and the somatodendritic compartment in midbrain, and by clearance by the DA transporter, diffusion, and extracellular metabolism. We review how axonal DA release is regulated by neuronal activity and by autoreceptors and heteroreceptors, and address how quantal release events are regulated in size and frequency. In brain regions densely innervated by DA axons, DA clearance is due predominantly to uptake by the DA transporter, whereas in cortex, midbrain, and other regions with relatively sparse DA inputs, the noradrenaline transporter and diffusion are involved. We discuss the role of DA uptake in restricting the sphere of influence of DA and in temporal accumulation of extracellular DA levels upon successive action potentials. The tonic discharge activity of DA neurons may be translated into a tonic extracellular DA level, whereas their bursting activity can generate
Filmul Leatherface: Ucigasul fara chip (2017) Filme online subtitrate incepe la resedinta Sawyer , capul familiei , Verna Sawyer (Lili Taylor) , organizeaza o petrecere ocazionata de ziua de nastere a celui mai nou membru al familiei , Jedidiah . Drept cadou si pentru a-l introduce pe acesta ...
O echipa de cercetatori japonezi a creat prin tehnici de inginerie genetica un supersoarece care nu da niciun semn ca s-ar speria de prezenta unei pisici.
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As fara as I could know, it is an Innovative company, persuing and producing changes in models within the business. Processes developing Focused
Mod de prezentare: extract napraznic flacon 200ml Se utilizeaza ca adjuvant in: sterilitate masculina si feminina, impotenta, frigiditate, tulburari menstruale (amenoree, dismenoree), fibrom uterin, chisturi ovariene, hemoragii uterine, tumori (uterine, mamare, pulmonare, intestinale), iradiere, sechele dupa iradiere, astenie, anemie, diaree, colita de fermentatie. Nu contine alcool fiind un tip de tinctura fara alcool ...
The Bachelor of Science in Radiologic Sciences is offered through the California State University, Northridge (CSUN) Department of Health Sciences, part of the College of Health and Human Development, as a Bachelor Degree. Graduates of the CSUN RT Program receive a diverse educational background as well as greater opportunities for advancement and mobility within the profession of Radiologic Sciences. In addition to proficiency in general Medical Imaging, RS Program graduates are educated in a variety of specialized imaging procedures, including Computed Tomography, Cardiovascular Imaging and Magnetic Resonance Imaging.. The CSUN RS Program has received the maximum accreditation (8 years) by the Joint Review Committee of Education in Radiologic Technology -- November, 2018. Accreditation information can be found at www.JRCERT.org. The BSRS program is also approved by the California Department of Health - Radiologic Health Branch.. ...
5-HT1B receptors are widely distributed throughout the central nervous system with the highest concentrations found in the frontal cortex, basal ganglia, striatum, and the hippocampus.[8] The function of the 5-HT1B receptor differs depending upon its location. In the frontal cortex, it is believed to act as a postsynaptic receptor inhibiting the release of dopamine. In the basal ganglia and the striatum, evidence suggests 5-HT signaling acts on an autoreceptor, inhibiting the release of serotonin[9] and decreasing glutamatergic transmission by reducing miniature excitatory postsynaptic potential (mEPSP) frequency,[10] respectively. In the hippocampus, a recent study has demonstrated that activation of postsynaptic 5-HT1B heteroreceptors produces a facilitation in excitatory synaptic transmission which is altered in depression.[11] When the expression of 5-HT1B in human cortex was traced throughout life, significant changes during adolescence were observed, in a way that is strongly correlated ...
The mild neuroinflammation hypothesis of schizophrenia was introduced by Bechter in 2001.It has been hypothesized that a hypofunction of glutamatergic signaling via N-methyl-n-aspartate receptors (NMDARs) and hyperactivation of dopamine D2 receptors play a role in schizophrenia. The triplet puzzle theory states that sets of triplet amino acid homologies guide two different receptors towards each other and contributes to the formation of a receptor heteromer. It is therefore proposed that putative NMDAR- C-C chemokine receptor type 2 (CCR2), NMDAR- C-X-C chemokine receptor type 4 (CXCR4) and NMDAR- Interleukin 1 receptor type II (IL1R2) heteromers can be formed in the neuronal networks in mild neuroinflammation due to demonstration of Gly-Leu-Leu (GLL), Val-Ser-Thr (VST) and/or Ser-Val-Ser (SVS) amino acid homologies between these receptor protomers. This molecular process may underlie the ability to produce symptoms of schizophrenia in mild neuroinflammation. In this state volume transmission is
Copyright© Thomas Jefferson University. All Rights Reserved.. The Thomas Jefferson University web site, its contents and programs, is provided for informational and educational purposes only and is not intended as medical advice nor is it intended to create any physician-patient relationship. Please remember that this information should not substitute for a visit or a consultation with a health care provider. The views or opinions expressed in the resources provided do not necessarily reflect those of Thomas Jefferson University, Thomas Jefferson University Hospital, or the Jefferson Health System or staff ...
Mustar dulce Bavarez FARA GLUTEN zwergenwiese. Cumpără Mustar dulce Bavarez FARA GLUTEN, îl găsești în categoria Mustar si maioneza bio
Aceste fursecuri fara gluten mi-au depasit asteptarile: au iesit atat de aromate si moi de se topesc in gura. Le voi mai face cu siguranta ;-)
Cumpara Biobon - Jeleuri bio cu fructe fara gluten 100g la pretul de 9.24 lei ✅ Comanda confidentiala, produse verificate de farmacisti reali, impachetare sigura.
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In cazul interventiilor chirurgicale, cu sau fara regim alimentar in preoperator, nutritia enterala pe baza de proteine hidrolizate (peptide) permite reluarea precoce a alimentatiei, reduce riscul complicatiilor post-operatorii, scade riscul de aparitie. Continue reading. ...
In cazul interventiilor chirurgicale, cu sau fara regim alimentar in preoperator, nutritia enterala pe baza de proteine hidrolizate (peptide) permite reluarea precoce a alimentatiei, reduce riscul complicatiilor post-operatorii, scade riscul de aparitie. Continue reading. ...
Cumpara rapid si simplu Srot de seminte de struguri. Srot de seminte de struguri este un produs natural, fara aditivi sau conservanti.
While delayed onset of antidepressant action remains a shortcoming of current antidepressants, preliminary clinical data with newer antidepressants, including mirtazapine, show promise for a hastened onset. Several potential mechanisms have been postulated and investigated. Mirtazapine displays serotonin 5-HT2 and 5-HT3, receptor blocking properties, while its putative earlier onset of action is thought to be related to its 2-adrenoceptor lytic action (at 2-adrenergic autoreceptors and heteroreceptors), thereby modulating central serotonergic and noradrenergic neurotransmission. The current study investigated the role of 2-adrenoceptor antagonism for earlier onset of action in a rat model of depression. First of all, the treatment period necessary to produce antidepressant-like responses with fluoxetine (an antidepressant with a delayed onset of action) was established. Rats were treated for 3, 7, and 11 days with fluoxetine, whereafter the forced swim test (FST) was employed and ...
The neurotransmitter 5-hydroxytryptamine (5-HT, serotonin) mediates important brain functions and contributes to the pathophysiology and successful drug treatment of many common psychiatric disorders, especially depression. It is established that a key mechanism involved in the control of 5-HT neurones is feedback inhibition by presynaptic 5-HT autoreceptors, which are located on 5-HT cell bodies and nerve terminals. However, recent experiments have discovered an unexpected complexity of 5-HT neurone control, specifically in the form of postsynaptic 5-HT feedback mechanisms. These mechanisms have the physiological effects of 5-HT autoreceptors but use additional 5-HT receptor subtypes and operate through neural inputs to 5-HT neurones. A postsynaptic feedback system that excites 5-HT neurones has also been reported. This article discusses current knowledge of the pharmacology and physiology of these new found 5-HT feedback mechanisms and considers their possible contribution to depression
Dopaminergic stabilizers can be defined as drugs that stimulate or inhibit dopaminergic signalling depending on the dopaminergic tone. (-)-OSU6162 and ACR16 appear to possess such a profile. They have been proposed to act as partial dopamine receptor agonists or as antagonists with preferential action on dopaminergic autoreceptors. Previous studies have shown either stimulation or inhibition of behaviour in response to (-)-OSU6162 and ACR16, which has been suggested to reflect their dual effects on dopaminergic signalling. The aims of the present work are to (1) examine the relation between behavioural response to these drugs and activity baseline, and (2) test the suggested mechanisms of action by means of close comparisons with the known partial D2-receptor agonists (-)-3-PPP and aripiprazole, and the D2 autoreceptor preferring antagonist amisulpride with respect to effects on behaviour. From the results of these experiments it can be concluded that: (1) The direction of the response to ...
Serotoninergic pathways projecting from the median and dorsal raphe nuclei to the hippocampus, amygdala and other limbic structures play a major role in the control of mood (Coplan et al., 1995) and there is evidence that their overactivity contributes to anxious states (Barrett and Gleeson, 1991; Coplan et al., 1995; Lesch, 1991; Millan and Brocco, 1993). Correspondingly, a component of the anxiolytic action of BZPs can be attributed to a reinforcement of the inhibitory tone exerted by GABAergic neurons on these serotoninergic pathways (Lista et al., 1990; Pan and Williams, 1989). In analogy, the inhibition of ascending serotoninergic transmission via activation of inhibitory 5-HT1A autoreceptors localized on cell bodies by buspirone, for example, appears to underlie anxiolytic effects in both operant, conflict-based paradigms, such as the pigeon and rat conflict tests (Barrett and Gleeson, 1991; Cervo and Samanin, 1995a, b; Schefkeet al., 1989; Schreiber et al., 1995a), as well as in ...
CREATE TABLE [FARA_All_ForeignPrincipals] ( [Foreign_Principal_Termination_Date] TEXT, [Foreign_Principal] TEXT, [Foreign_Principal_Registration_Date] TEXT, [Country/Location_Represented] TEXT, [Registration_Number] INTEGER, [Registrant_Date] TEXT, [Registrant_Name] TEXT, [Address_1] TEXT, [Address_2] TEXT, [City] TEXT, [State] TEXT, [Zip] TEXT, FOREIGN KEY([Registration_Number]) REFERENCES [FARA_All_Registrants]([Registration_Number ...
You can raise awareness about the nature of FA and the work FARA is doing to raise funds for research by speaking about it in your community (school, church, library, place of employment). Such speaking engagements can also create opportunities to grow the FA communitys network of support. Much of FARAs success and speed of research is credited to collaboration and networking in the scientific and patient communities as well as with related disease groups. If youd like to speak with someone in the FARA office about how best to prepare for a speaking engagement, please contact [email protected] ...
FARA, based in Mandeville, La., announced the appointment of Todd Higley as vice president of sales and marketing. In this position, Higley is responsible
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Monoamine autoreceptors (e.g., D2 short, presynaptic α2, and presynaptic 5-HT1A) have the opposite effect of TAAR1, and ... TAAR1 forms GPCR oligomers with monoamine autoreceptors in neurons in vivo. These and other reported TAAR1 hetero-oligomers ... Notably, amphetamine and trace amines possess high binding affinities for TAAR1, but not for monoamine autoreceptors. The ... enhancement by monoamine transporters and attenuation by the D2 autoreceptor in vitro". The Journal of Pharmacology and ...
Monoamine autoreceptors (e.g., D2 short, presynaptic α2, and presynaptic 5-HT1A) have the opposite effect of TAAR1, and ... Notably, amphetamine and trace amines possess high binding affinities for TAAR1, but not for monoamine autoreceptors. Imaging ...
They appear to serve as autoreceptors. In addition, they modulate muscarinic potassium channels. In the heart, this contributes ... Douglas CL, Baghdoyan HA, Lydic R (December 2001). "M2 muscarinic autoreceptors modulate acetylcholine release in prefrontal ...
... stimulating autoreceptors, inhibiting neurotransmitter release; 7) blocking autoreceptors, increasing neurotransmitter release ...
... an autoreceptor heteromer) D4-adrenoceptor α1B D4-adrenoceptor β1 Dopamine receptor D1 and Dopamine receptor D5 are Gs coupled ... autoreceptors, which regulate neurotransmission via feedback mechanisms. It affects synthesis, storage, and release of dopamine ...
They function as inhibitory autoreceptors for acetylcholine. Activation of M4 receptors inhibits acetylcholine release in the ... The M2 subtype of acetylcholine receptor functions similarly as an inhibitory autoreceptor to acetylcholine release, albeit ...
Autoreceptor Millan, M. J.; Lejeune, F.; Gobert, A. (2000). "Reciprocal autoreceptor and heteroreceptor control of serotonergic ... they are opposite to autoreceptors, which are sensitive only to neurotransmitters or hormones released by the cell in whose ...
Bennett M (1999). "One hundred years of adrenaline: the discovery of autoreceptors". Clin Auton Res. 9 (3): 145-59. doi:10.1007 ...
Bennett MR (June 1999). "One hundred years of adrenaline: the discovery of autoreceptors". Clinical Autonomic Research. 9 (3): ...
Bennett MR (June 1999). "One hundred years of adrenaline: the discovery of autoreceptors". Clinical Autonomic Research. 9 (3): ...
Waters N, Lagerkvist S, Löfberg L, Piercey M, Carlsson A (September 1993). "The dopamine D3 receptor and autoreceptor ... Aretha CW, Sinha A, Galloway MP (August 1995). "Dopamine D3-preferring ligands act at synthesis modulating autoreceptors". The ... Lahti AC, Weiler M, Carlsson A, Tamminga CA (1998). "Effects of the D3 and autoreceptor-preferring dopamine antagonist (+)- ... and an antagonist at D2Sh autoreceptors on dopaminergic nerve terminals. This causes dopamine release in the brain and has a ...
Bennett, M. (1999). "One hundred years of adrenaline: the discovery of autoreceptors". Clinical Autonomic Research. 9 (3): 145- ...
ISBN 978-0-19-828802-2. Bennett M (1999). "One hundred years of adrenaline: the discovery of autoreceptors". Clin Auton Res. 9 ...
ISBN 0-444-80493-5. M. R. Bennett (1999). "One hundred years of adrenaline: the discovery of autoreceptors". Clinical Autonomic ... Klaus Starke (2001). "Presynaptic autoreceptors in the third decade: focus on α2-adrenoceptors". Journal of Neurochemistry. 78 ... presynaptic α-autoreceptors. Their existence was initially combated but is now established, for example by the demonstration of ...
H3 receptors function as presynaptic autoreceptors on histamine-containing neurons. The diverse expression of H3 receptors ... where they act as autoreceptors in presynaptic histaminergic neurons, and also control histamine turnover by feedback ...
One possible explanation for this lag is that the neurotransmitter activity enhancement is the result of auto receptor ... Hjorth, S; Bengtsson, HJ; Kullberg, A; Carlzon, D; Peilot, H; Auerbach, SB (June 2000). "Serotonin autoreceptor function and ... The therapeutic effect of antidepressants is thought to arise from autoreceptor desensitization over a period of time, ... as firing of serotonergic neurons in the dorsal raphe adapt via the activity of 5-HT1A autoreceptors. ...
This autoreceptor-mediated inhibition of serotonin release has been theorized to be a major factor in the therapeutic lag that ... The autoreceptors must first desensitize before the concentration of extracellular serotonin in the synapse can become elevated ... 5-HT1A autoreceptor desensitization and increased 5-HT1A receptor postsynaptic activation via general increases in serotonin ... The 5-HT1A receptors in the raphe nucleus are largely somatodendritic autoreceptors, whereas those in other areas such as the ...
This is likely due to preferential activation of D2/D3 autoreceptors versus postsynaptic receptors, the latter of which ... an extremely potent stimulant of dopamine autoreceptors". Brain Research. 231 (1): 109-16. doi:10.1016/0006-8993(82)90011-7. ...
In Hen's lab, Donaldson probed the role of the Serotonin 1A autoreceptor in behavior. She first examined how suppression of 5- ... "Developmental Effects of Serotonin 1A Autoreceptors on Anxiety and Social Behavior". Neuropsychopharmacology. 39 (2): 291-302. ...
In the brain, all autoreceptors appear to be of the α2 type. (The drug idazoxan blocks α2 autoreceptors and hence acts as an ... Adrenergic neurons, in particular the α2 autoreceptors found in the brain, are also involved in sexual behavior and in the ...
Gründer G, Wetzel H, Hammes E, Benkert O (1993). "Roxindole, a dopamine autoreceptor agonist, in the treatment of major ... Maj J, Kołodziejczyk K, Rogóz Z, Skuza G (March 1997). "Roxindole, a dopamine autoreceptor agonist with a potential ... Klimke A, Klieser E (July 1991). "Antipsychotic efficacy of the dopaminergic autoreceptor agonist EMD 49980 (Roxindol). Results ... Bartoszyk GD, Harting J, Minck KO (January 1996). "Roxindole: psychopharmacological profile of a dopamine D2 autoreceptor ...
The latter was thus demonstrated to be an autoreceptor on cells that release dopamine. TAAR1 is a presynaptic intracellular ... Dopamine autoreceptors also regulate DAT by directly opposing the effect of TAAR1 activation. The human dopamine transporter ( ... receptor that is also colocalized with DAT and which has the opposite effect of the D2 autoreceptor when activated; i.e., it ...
This delay is caused by the time it takes 5-HT to downregulate 5-HT1A autoreceptors and turn on the neuro impulse flow of the 5 ... When these 5-HT1A autoreceptors have been downregulated, they will no longer restrict the impulse flow of the 5-HT neuron. The ... desensitized somatodendritic 5-HT1A autoreceptors, (4) turned on the impulse flow and (5) increased the release of 5-HT from ... This increase in 5-HT concentration causes desensitization of somatodendritic 5-HT1A autoreceptors. ...
They function as autoreceptors in the brain and decrease the release of serotonin. The anxiolytic drug Buspirone acts as ...
It also appears to serve as a presynaptic serotonin autoreceptor. The neurotransmitter serotonin (5-hydroxytryptamine, 5-HT) ... Evidence for an autoreceptor role for the 5-ht5A receptor in guinea pig brain". Neuropharmacology. 51 (3): 566-77. doi:10.1016/ ...
The short form (D2Sh) is pre-synaptic and functions as an autoreceptor that regulates the levels of dopamine in the synaptic ... In flies, activation of the D2 autoreceptor protected dopamine neurons from cell death induced by MPP+, a toxin mimicking ... OSU-6162 - also 5-HT2A partial agonist, acts as "dopamine stabilizer" Roxindole (only at the D2 autoreceptors) RP5063 ... presynaptic autoreceptors) Amisulpride (low doses) UH-232 Homocysteine - negative allosteric modulator PAOPA SB-269,652 SB- ...
3. Autoreceptor. 4. Synapse with neurotransmitter released (serotonin). 5. Postsynaptic receptors activated by neurotransmitter ...
Norepinephrine interacts with postsynaptic α and β adrenergic receptor subtypes and presynaptic α2 autoreceptors. The α2 ... Formation of norepinephrine is reduced by autoreceptors through the rate-limiting enzyme tyrosine hydroxylase, an effect ... mediated through α2 autoreceptors), metabolic activity, and release of neurotransmitters. TCAs do not block dopamine transport ... receptors include presynaptic autoreceptors which limit the neurophysiological activity of noradrenergic neurons in the central ...
Lehmann, J; Langer, SZ (1982). "Dopamine autoreceptors differ pharmacologically from postsynaptic dopamine receptors: Effects ...
Paradoxically, SSRIs can increase anxiety initially due to negative feedback through the serotonergic autoreceptors. For this ...
Autoreceptors may be located in any part of the cell membrane: in the dendrites, the cell body, the axon, or the axon terminals ... An autoreceptor is a type of receptor located in the membranes of presynaptic nerve cells. It serves as part of a negative ... Autoreceptors are usually G protein-coupled receptors (rather than transmitter-gated ion channels) and act via a second ... Autoreceptor activity may also decrease paired-pulse facilitation (PPF).[citation needed] A feedback cell is activated by the ( ...
In contrast to non-NMDA autoreceptors, NMDA autoreceptors are almost exclusively located on secondary dendrites and their ... Dendritic glutamate autoreceptors modulate signal processing in rat mitral cells.. Salin PA1, Lledo PM, Vincent JD, Charpak S. ... It has been shown recently that in mitral cells of the rat olfactory bulb, N-methyl-D-aspartate (NMDA) autoreceptors are ... We show that both ionotropic NMDA and non-NMDA autoreceptors are activated by glutamate released from primary and secondary ...
Loss of autoreceptor functions in mice lacking the dopamine transporter.. Jones SR1, Gainetdinov RR, Hu XT, Cooper DC, Wightman ... Autoreceptors provide an important inhibitory feedback mechanism for dopamine neurons by altering neuronal functions in ... The function of dopamine autoreceptors was assessed in mice lacking the dopamine transporter (DAT). Genetic deletion of the DAT ... Direct assessment of impulse-, synthesis- and release-regulating autoreceptors in these mice reveals a nearly complete loss of ...
To investigate the modulation of histamine release by autoreceptors and heteroreceptors, the rat anterior hypothalamus was ... H3 Autoreceptors and muscarinic acetylcholine receptors modulate histamine release in the anterior hypothalamus of freely ... It is concluded that in the anterior hypothalamus the release of endogenous histamine is modulated by H3 autoreceptors. ... To investigate the modulation of histamine release by autoreceptors and heteroreceptors, the rat anterior hypothalamus was ...
2004) Acute treatment with the antidepressant fluoxetine internalizes 5-HT1A autoreceptors and reduces the in vivo binding of ... In any case, this result is consistent with previous findings showing an internalization of 5-HT1A autoreceptors but not ... Our data suggest that nicotine induces an indirect stimulation of 5-HT1A autoreceptors that limits serotonergic transmission ... MAOIs, because they enhance serotonergic tone, desensitize 5-HT1A autoreceptors and allow the stimulating effects of nicotine ...
Sustained depression of D2 autoreceptor signaling required activation of the type 2 NT receptor and the protein phosphatase ... Activity of midbrain dopaminergic neurons is under strict control of inhibitory D2 autoreceptors. Application of the modulatory ... Neurotensin Induces Presynaptic Depression of D2 Dopamine Autoreceptor-Mediated Neurotransmission in Midbrain Dopaminergic ... Neurotensin Induces Presynaptic Depression of D2 Dopamine Autoreceptor-Mediated Neurotransmission in Midbrain Dopaminergic ...
... autoreceptors originating in the caudal DRN regulate behavioral expression of helplessness and fear. Because systemic ... Serotonin 1B autoreceptors originating in the caudal dorsal raphe nucleus reduce expression of fear and depression-like ... Methods: We manipulated 5-HT(1B) autoreceptor function in rats using either viral-mediated gene transfer into the caudal DRN or ... Background: Serotonin 1B (5-HT(1B)) autoreceptors regulate release of serotonin from terminals of dorsal raphe nucleus (DRN) ...
... hypothesis that the release of glutamate and aspartate is regulated by the activation of excitatory amino acid autoreceptors. ... Autoreceptor regulation of glutamate and aspartate release from slices of the hippocampal CA1 area J Neurochem. 1991 May;56(5): ... These results suggest that glutamate can negatively modulate the release of aspartate by activating autoreceptors of the ... hypothesis that the release of glutamate and aspartate is regulated by the activation of excitatory amino acid autoreceptors. ...
The presynaptic alpha-2 autoreceptors in pig brain cortex are alpha-2A.. A U Trendelenburg, N Limberger and K Starke ... The presynaptic alpha-2 autoreceptors in pig brain cortex are alpha-2A.. A U Trendelenburg, N Limberger and K Starke ... The presynaptic alpha-2 autoreceptors in pig brain cortex are alpha-2A.. A U Trendelenburg, N Limberger and K Starke ... The presynaptic alpha-2 autoreceptors in pig brain cortex were subclassified in terms of alpha-2A, alpha-2B, alpha-2C and alpha ...
The monoamine autoreceptors are known to be presynaptic release regulators (Starke et al., 1989; Tavares et al., 1996; Gobert ... To block the autoreceptors, 10 μM raclopride (RAC), SKF86466 (SKF), or methiothepin (MET) was added during the exposure to the ... To block the autoreceptors, 10 μM raclopride (RAC), SKF86466 (SKF), or methiothepin (MET) was added during the exposure to ... To block the autoreceptors, 10 μM raclopride, SKF86466, or methiothepin was added during drug pretreatment or during uploading ...
Desensitization of the D2 autoreceptor is reduced following in vivo cocaine exposure due to plasticity in the D2S and not the ...
... caused by prior in vivo cocaine exposure may be conferred by an unexpected role of the D2L splice variant as an autoreceptor. ... The loss of calcium-dependent D2 autoreceptor desensitization ... desensitization of D2 autoreceptors reduces the D2 autoreceptor ... Both D2S and D2L function as autoreceptors. The D2S isoform has been thought to be the D2 autoreceptor due to preservation of ... "If some DA neurons express either D2S or D2L, they do not show cocaine-induced autoreceptor plasticity, and if D2L blocks ...
5-HT1A autoreceptor is known to play a role in mood disorders and their treatments. An increase in somatodendritic 5-HT1A ... Here we assessed the effects of sustained administration of the SSRI fluoxetine on 5-HT1A autoreceptor sensitivity in mice ... Functional Status of Somatodendritic 5-HT1A Autoreceptor after Chronic Treatment with Fluoxetine in a Mouse Model of Anxiety/ ... Functional Status of Somatodendritic 5-HT1A Autoreceptor after Chronic Treatment with Fluoxetine in a Mouse Model of Anxiety/ ...
Role of Presynaptic Acetylcholine Autoreceptors at Motor Nerve Endings on Tetanic and Train-of-four Fade Seen during a ... Role of Presynaptic Acetylcholine Autoreceptors at Motor Nerve Endings on Tetanic and Train-of-four Fade Seen during a ... Role of Presynaptic Acetylcholine Autoreceptors at Motor Nerve Endings on Tetanic and Train-of-four Fade Seen during a ... Malin Jonsson, Lars I. Eriksson; Role of Presynaptic Acetylcholine Autoreceptors at Motor Nerve Endings on Tetanic and Train-of ...
In an effort to localize the diminished APO response, DA autoreceptor sensitivity to APO was assessed in drug- and vehicle- ... the APO-induced reversal of DOPA elevation was used as an index of DA autoreceptor sensitivity. This GBL-stimulated in vivo ... in animals pretreated with antidepressants does not originate as a result of alterations in the sensitivity of DA autoreceptors ... Changes in dopamine autoreceptor sensitivity in an animal model of depression. *Richard Muscat, Anthony Towell, Paul Willner ...
Data underlying the autoreceptor hypothesis : The original finding, which led to the formulation of the autoreceptor hypothesis ... 4. reduction of synaptic DA levels should result in a potentiation of autoreceptor-mediated responses, or the autoreceptor- ... Do autoreceptors mediate dopamine agonist-induced yawning and suppression of exploration ? a critical review. Stahle Lars. ... mediated by stimulation of autoreceptors. In the following this hypothesis is referred to as "the autoreceptor hypothesis", a ...
"Autoreceptors" 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 "Autoreceptors" by people in this website by year, and whether ... Below are the most recent publications written about "Autoreceptors" by people in Profiles. ...
Autoreceptor control of serotonin dynamics: BackgroundSerotonin is a neurotransmitter that has been linked to a wide variety of ... Autoreceptor control of serotonin dynamics. Source. PubMed Central Date. Sep 23, 2020 ... We show there are likely two reuptake mechanisms for serotonin and that the autoreceptors have long-lasting influence and ... and autoreceptor function.ResultsWe discuss the steady state of the model and the steady state distribution of extracellular ...
Differential development of autoreceptor subsensitivity and enhanced dopamine release during amphetamine sensitization. / Wolf ... Wolf, M., White, F. J., Nassar, R., Brooderson, R. J., & Khansa, M. R. (1993). Differential development of autoreceptor ... Differential development of autoreceptor subsensitivity and enhanced dopamine release during amphetamine sensitization. Journal ... Wolf, Marina ; White, F. J. ; Nassar, R. ; Brooderson, R. J. ; Khansa, M. R. / Differential development of autoreceptor ...
Pre-junctional muscarinic autoreceptors in bovine airways. Oct 26, 2011·Respiratory Physiology & Neurobiology·Michele Baroffio ... Functional relevance of presynaptic muscarinic autoreceptors. Jan 1, 1993·Journal of Physiology, Paris·H KilbingerR S von ... Characterization of prejunctional muscarinic autoreceptors in the guinea-pig trachea. British Journal of Pharmacology ...
Dopamine autoreceptor down-regulation following repeated electroconvulsive shock. Dopamine autoreceptor down-regulation ...
Autoreceptors. 5-HT1A receptors can be located on the cell body, dendrites, axons, and both presynaptically and ... This autoreceptor-mediated inhibition of serotonin release has been theorized to be a major factor in the therapeutic lag that ... Stimulation of 5-HT1A autoreceptors inhibits the release of serotonin in nerve terminals. For this reason, 5-HT1A receptor ... Similarly to SRAs, sufficiently high doses of 5-HT1A receptor agonists also bypass the 5-HT1A autoreceptor-mediated inhibition ...
Yawo H, Chuhma N. Preferential inhibition of oω-conotoxin-sensitive presynaptic Ca 2+ channels by adenosine autoreceptors. ... Preferential inhibition of oω-conotoxin-sensitive presynaptic Ca 2+ channels by adenosine autoreceptors. :: Nature. 1993 ; 巻 ... The adenosine Al receptor is assumed to reside in presynaptic terminals and to function as a negative autoreceptor1. How ... フィンガープリント Preferential inhibition of oω-conotoxin-sensitive presynaptic Ca ,sup,2+,/sup, channels by adenosine autoreceptors の ...
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Monoamine autoreceptors (e.g., D2 short, presynaptic α2, and presynaptic 5-HT1A) have the opposite effect of TAAR1, and ... TAAR1 forms GPCR oligomers with monoamine autoreceptors in neurons in vivo. These and other reported TAAR1 hetero-oligomers ... Notably, amphetamine and trace amines possess high binding affinities for TAAR1, but not for monoamine autoreceptors. The ... enhancement by monoamine transporters and attenuation by the D2 autoreceptor in vitro". The Journal of Pharmacology and ...
3. Autoreceptor. 4. Synapse with neurotransmitter released (serotonin). 5. Postsynaptic receptors activated by neurotransmitter ...
Fingerprint Dive into the research topics of Abrogated freud-1/Cc2d1a repression of 5-HT1A autoreceptors induces fluoxetine- ... Freud-1/Cc2d1a represses the gene transcription of serotonin-1A (5-HT1A) autoreceptors, which negatively regulate 5-HT tone. To ... Abrogated freud-1/Cc2d1a repression of 5-HT1A autoreceptors induces fluoxetine-resistant anxiety/ depression-like behavior. ... N2 - Freud-1/Cc2d1a represses the gene transcription of serotonin-1A (5-HT1A) autoreceptors, which negatively regulate 5-HT ...
Autoreceptors • Bangladesh • Bees • Beetles • Behavior, Animal • Betaine • Biochemistry • Biological Evolution • Biological ...
Autoreceptors and Heteroreceptors Evidenced by Histamine H3 Receptor Ligands. Somato-Dendritic 5-HT1A Autoreceptors in the ... Autoreceptor Mediated Changes in Dopaminergic Terminal Excitability In Vivo. Prejunctional Autoreceptors in Mouse Vas Deferens ... The Third Dopamine Receptopr (D3) as an Autoreceptor. Terminal Dopaminergic Autoreceptors are of Minor Importance for the ... Receptor Type and Interaction with Autoreceptors. Presynaptic Autoreceptors May Control the Release of Metenkephalin from the ...
  • Autoreceptors provide an important inhibitory feedback mechanism for dopamine neurons by altering neuronal functions in response to changes in extracellular levels of dopamine. (nih.gov)
  • Activity of midbrain dopaminergic neurons is under strict control of inhibitory D 2 autoreceptors. (jneurosci.org)
  • Application of the modulatory peptide neurotensin (NT) to midbrain dopaminergic neurons transiently increases activity by decreasing D 2 dopamine autoreceptor function, yet little is known about the mechanisms that underlie long-lasting effects. (jneurosci.org)
  • Similarly, DA release and the firing of DA neurons are also modulated by the degree of stimulation of DA autoreceptors. (baillement.com)
  • First, single-unit recording was used to examine the sensitivity of impulse-regulating somatodendritic autoreceptors located on mesoaccumbens dopamine neurons in the rat ventral tegmental area. (elsevier.com)
  • Cultured rat fetal mesencephalic dopaminergic neurons exhibit specific high-affinity uptake for [3H]dopamine (DA) and express DA D-2 autoreceptors, functionally coupled to the inhibition of depolarization evoked [3H]DA release. (vumc.nl)
  • It is concluded that, while no functional desensitization of DA D-2 autoreceptors is apparent, the depolarization-induced release of DA from cultured fetal dopaminergic neurons is enhanced upon long-term sustained activation of DA D-2 receptors. (vumc.nl)
  • However, M 2 receptors act as autoreceptors on parasympathetic neurons to limit acetylcholine release, thus limiting vagal reflex-induced bronchoconstriction and mucus secretion [ 2 , 7 ]. (ersjournals.com)
  • Unlike subcortical dopamine projections, these neurons lack autoreceptors. (ect.org)
  • Autoreceptors are usually G protein-coupled receptors (rather than transmitter-gated ion channels) and act via a second messenger. (wikipedia.org)
  • To investigate the modulation of histamine release by autoreceptors and heteroreceptors, the rat anterior hypothalamus was superfused through a push-pull cannula with agonists or antagonists of histamine and acetylcholine muscarinic receptors. (springer.com)
  • Complementary experiments with 8-OHDPAT (8-hydroxy-dipropylamino-tetralin), a 5-HT 1A receptor agonist, and analysis of 5-HT 1A receptors expression in the dorsal raphe nucleus after a tranylcypromine injection indicate that MAOIs contained in tobacco desensitize 5-HT 1A autoreceptors to trigger the strong addictive properties of tobacco. (jneurosci.org)
  • The results reveal that D2S, but not D2L receptors, exhibited calcium-dependent desensitization similar to that exhibited by endogenous autoreceptors. (elifesciences.org)
  • The dopamine receptor transcripts encode receptors that function as autoreceptors. (acnp.org)
  • M2 muscarinic autoreceptors modulate acetylcholine release in prefrontal cortex of C57BL/6J mouse. (ebi.ac.uk)
  • Autoreceptors on the presynaptic neuron will also detect this neurotransmitter and often function to control internal cell processes, typically inhibiting further release or synthesis of the neurotransmitter. (wikipedia.org)
  • The feedback cell releases a neurotransmitter to which the autoreceptor of the presynaptic neuron is receptive. (wikipedia.org)
  • Monoamine autoreceptors provide feedback regulation in neurotransmitter release, and monoamine transporters clear the released neurotransmitters to control synaptic signaling. (aspetjournals.org)
  • 5 Altogether, a selective inhibition of the α 3 β 2 nAChR reduces the presynaptic acetylcholine release, thus working as an autoreceptor, and during conditions of reduced safety factor in the neuromuscular junction, produced a tetanic fade. (asahq.org)
  • Dendritic glutamate autoreceptors modulate signal processing in rat mitral cells. (nih.gov)
  • These results suggest that glutamate can negatively modulate the release of aspartate by activating autoreceptors of the quisqualate, and possibly also of the kainate, type. (nih.gov)
  • These data provide the first evidence that common biogenic amines modulate monoamine transporter function via both TAAR1 and monoamine autoreceptors, which may balance monoaminergic activity. (aspetjournals.org)
  • suggests that common biogenic amines may modulate monoamine transporter function via interacting with monoamine autoreceptors in the brain. (aspetjournals.org)
  • Dopamine release is negatively regulated by the activation of dopamine D2 autoreceptors on somatodendritic and axon terminals (reviewed in Ford, 2014 ). (elifesciences.org)
  • An increase in somatodendritic 5-HT 1A autoreceptor density in the dorsal raphe (DR) attenuates the therapeutic activity of selective serotonin reuptake inhibitors (SSRIs), whereas their functional desensitization promotes activation of brain serotonergic transmission, thereby representing an adaptive change relevant to their therapeutic effect. (aspetjournals.org)
  • 7 Consequently, the reduction in 5-HT cell firing by risperidone appears to be related to increased availability of 5-HT in the somatodendritic region of the neurones leading to an enhanced 5-HT 1A autoreceptor activation and, in turn, to inhibition of firing, and is probably only to a minor extent caused by its α 1 -adrenoceptor antagonistic action. (wiley.com)
  • Callahan, PM , Piercey, MF & Cunningham, KA 1992, ' Effects of the putative dopamine autoreceptor antagonists (+)-AJ 76 and (+)-UH 232 on the discriminative stimulus properties of cocaine ', Psychopharmacology , vol. 107, no. 1, pp. 73-77. (elsevier.com)
  • Thus activation of excitatory autoreceptors is a major function of action potentials backpropagating in mitral cell dendrites, which results in an immediate positive feedback counteracting recurrent inhibition and increasing the signal-to-noise ratio of olfactory inputs. (nih.gov)
  • Slices of hippocampal area CA1 were employed to test the hypothesis that the release of glutamate and aspartate is regulated by the activation of excitatory amino acid autoreceptors. (nih.gov)
  • It is only sensitive to the neurotransmitters or hormones released by the neuron on which the autoreceptor sits. (wikipedia.org)
  • This publication is a good reference for students and individuals researching on the presynaptic autoreceptors and neurotransmitters. (elsevier.com)
  • The autoreceptor causes the inhibition of calcium channels (slowing calcium ion influx) and the opening of potassium channels (increasing potassium ion efflux) in the presynaptic membrane. (wikipedia.org)
  • Dopamine (DA) synthesis is generally assumed to bc controlled by end-product inhibition and is autoreceptors. (baillement.com)
  • At 3 to 4 days off, autoreceptor subsensitivity was observed in the ventral tegmental area of amphetamine-treated rats, but there was no significant change in the ability of amphetamine to increase extracellular dopamine levels in nucleus accumbens. (elsevier.com)
  • In the last few years, we have studied the presence and involvement in synaptogenesis and mature transmitter release of the adenosine autoreceptors (AR) in the mammalian neuromuscular junction (NMJ). (frontiersin.org)
  • examined mice lacking serotonin autoreceptors that inhibited serotonin secretion. (healthline.com)
  • Loss of autoreceptor functions in mice lacking the dopamine transporter. (nih.gov)
  • The function of dopamine autoreceptors was assessed in mice lacking the dopamine transporter (DAT). (nih.gov)
  • Direct assessment of impulse-, synthesis- and release-regulating autoreceptors in these mice reveals a nearly complete loss of function. (nih.gov)
  • Previous in vivo cocaine exposure removed calcium-dependent D2 autoreceptor desensitization in wild type, but not D2S-only mice. (elifesciences.org)
  • Here we assessed the effects of sustained administration of the SSRI fluoxetine on 5-HT 1A autoreceptor sensitivity in mice administered with corticosterone. (aspetjournals.org)
  • The original finding, which led to the formulation of the autoreceptor hypothesis (as defined in the introduction), was that APO inhibits tyrosine hydroxylation (dopa accumulation in NSD 1015 - treated mice) in the same doses as motor activity of mice is suppressed. (baillement.com)
  • We use the deterministic model to interpret experimental data on the responses in the hippocampus of male and female mice, and to illustrate the short-time dynamics of the autoreceptors. (mysciencework.com)
  • In cF1ko mice, 5-HT1A autoreceptor protein, binding and hypothermia response were increased, with reduced 5-HT content and neuronal activity in the dorsal raphe. (elsevier.com)
  • Here, we demonstrate that region-specific contributions of D 2 autoreceptors (D2AR) to presynaptic DA homeostasis dictate the consequences of Val559 expression in adolescent male mice. (cdc.gov)
  • Without these autoreceptors, the mice had higher levels of serotonin available in their brains. (healthline.com)
  • All subtypes seem to serve as autoreceptors [ PMID: 11714883 ], and knockout mice reveal the important neuromodulatory role played by this receptor family [ PMID: 14744253 , PMID: 15474550 , PMID: 17762886 ]. (ebi.ac.uk)
  • We manipulated 5-HT(1B) autoreceptor function in rats using either viral-mediated gene transfer into the caudal DRN or systemic injections of the 5-HT(1B) agonist 3-(1,2,5,6-tetrahydro-4-pyridyl)-5-propoxypyrrolo[3,2-b]pyridine (CP-94253). (nih.gov)
  • alpha2-adrenergic agonist that stimulates autoreceptors and inhibits noradrenergic cell firing. (studystack.com)
  • Dopamine D 2 autoreceptor agonist. (tocris.com)
  • Bartoszyk et al (1996) Roxindole: psychopharmacological profile of a DA D 2 autoreceptor agonist. (tocris.com)
  • We show that both ionotropic NMDA and non-NMDA autoreceptors are activated by glutamate released from primary and secondary dendrites. (nih.gov)
  • One of the simulated mechanisms consists in a feedback of released transmitter on ionotropic autoreceptors. (hu-berlin.de)
  • These results suggest that GABA inhibits its own release via ionotropic autoreceptors. (hu-berlin.de)
  • Dopamine autoreceptor down-regulation following repeated electroconvulsive shock. (bvsalud.org)
  • Region-Specific Regulation of Presynaptic Dopamine Homeostasis by D2 Autoreceptors Shapes the In Vivo Impact of the Neuropsychiatric Disease-Associ. (cdc.gov)
  • Autoreceptors called 5-HT1a are strongly involved in the regulation of serotonin neurotransmission. (clinicaltrials.gov)
  • An autoreceptor is a type of receptor located in the membranes of presynaptic nerve cells. (wikipedia.org)
  • A given receptor can act as either an autoreceptor or a heteroreceptor, depending upon the type of transmitter released by the cell on which it is embedded. (wikipedia.org)
  • The D2sh autoreceptor interacts with the trace amine-assorted receptor 1 (TAAR1), a recently discovered GPCR, to regulate monoaminergic systems in the brain. (wikipedia.org)
  • Sustained depression of D 2 autoreceptor signaling required activation of the type 2 NT receptor and the protein phosphatase calcineurin. (jneurosci.org)
  • Two pathways of calcium signaling that regulated D2 autoreceptor-dependent GIRK signaling were identified, which distinctly affected desensitization and the magnitude of D2S and D2L receptor-dependent GIRK currents. (elifesciences.org)
  • The adenosine Al receptor is assumed to reside in presynaptic terminals and to function as a negative autoreceptor 1 . (elsevier.com)
  • Drug action at the 5-HT(1A) receptor in vivo: autoreceptor and postsynaptic receptor occupancy examined with PET and [carbonyl-(11)C]WAY-100635. (ox.ac.uk)
  • In this qualitative study, positron emission tomography (PET) and [carbonyl-(11)C]WAY-100635 were used to assess 5-HT(1A) autoreceptor and postsynaptic receptor occupancy in man in vivo by five different compounds with nanomolar affinity for this site. (ox.ac.uk)
  • Pindolol demonstrated a preferential occupancy at the autoreceptor compared to the postsynaptic receptor over a plasma range of about 10-20 ng/mL. (ox.ac.uk)
  • The H3 histamine receptor is a presynaptic autoreceptor found on nerve cells that contain histamine. (news-medical.net)
  • Serotonin 1B (5-HT(1B)) autoreceptors regulate release of serotonin from terminals of dorsal raphe nucleus (DRN) projections. (nih.gov)
  • The 5-HT(1B) autoreceptors originating in the caudal DRN regulate behavioral expression of helplessness and fear. (nih.gov)
  • D2 autoreceptors regulate dopamine release throughout the brain. (elifesciences.org)
  • Freud-1/Cc2d1a represses the gene transcription of serotonin-1A (5-HT1A) autoreceptors, which negatively regulate 5-HT tone. (elsevier.com)
  • In their review of TAAR1 in monoaminergic systems, Xie and Miller proposed this schematic: synaptic dopamine binds to the dopamine autoreceptor, which activates the DAT. (wikipedia.org)
  • Thus, it bas been hypothesized that yawning and suppression of exploration induced by DA agonists are mediated by a reduction of synaptic levels of DA which, in turn, is mediated by stimulation of autoreceptors. (baillement.com)
  • 4. reduction of synaptic DA levels should result in a potentiation of autoreceptor-mediated responses, or the autoreceptor-mediated response should be abolislied, if the levels are too low. (baillement.com)
  • An atypical example is given by the β-adrenergic autoreceptor in the sympathetic peripheral nervous system, which acts to increase transmitter release. (wikipedia.org)
  • However, after 10 to 14 days off, autoreceptor subsensitivity was no longer observed, but amphetamine challenge resulted in a significantly greater increase in extracellular dopamine levels in amphetamine-treated as compared to saline-treated rats. (elsevier.com)
  • These findings suggest that autoreceptor subsensitivity is a transient effect which may be related to the development of sensitization, whereas enhancement of amphetamine-stimulated dopamine release does not accompany early stages of behavioral sensitization, but may be involved in the persistance of the phenomenon after longer withdrawal periods. (elsevier.com)
  • It has repeatedly been observed that signs of DA autoreceptor stimulation in vivo are seen with relativ y small doses of DA agonists. (baillement.com)
  • It has been shown recently that in mitral cells of the rat olfactory bulb, N-methyl-D-aspartate (NMDA) autoreceptors are activated during mitral cell firing. (nih.gov)
  • In contrast to non-NMDA autoreceptors, NMDA autoreceptors are almost exclusively located on secondary dendrites and their activation generates a large and sustained self-excitation. (nih.gov)
  • It is concluded that in the anterior hypothalamus the release of endogenous histamine is modulated by H 3 autoreceptors. (springer.com)
  • These findings demonstrate that the evidence used to formulate the autoreceptor hypothesis in the first place is indirect and relies upon the assumption that changes in synthesis are followed by similar changes in release. (baillement.com)
  • This study used transfected cells and brain synaptosomes to evaluate the interaction of common biogenic amines with TAAR1 and monoamine autoreceptors and explore their modulatory effects on monoamine transporters. (aspetjournals.org)
  • By comparing the effects of dopamine, norepinephrine, and serotonin in monkey and wild-type mouse synaptosomes to their effects in TAAR1 knockout mouse synaptosomes, we deduced that TAAR1 activity inhibited uptake and promoted efflux by monoamine transporters and that monoamine autoreceptors exerted opposite effects. (aspetjournals.org)
  • Autoreceptor activity may also decrease paired-pulse facilitation (PPF). (wikipedia.org)
  • However, the synthesis of DA in these terminals does not seem to be modulated by DA autoreceptors. (aspetjournals.org)
  • It's found throughout the brain, sometimes as an autoreceptor on a serotonin neuron (such as in the dorsal raphe region of the brain) to provide feedback to the cell. (scientificamerican.com)
  • is a modulator of the dopamine D2 autoreceptor-activated trafficking of the dopamine transporter. (rehabcentersnetwork.com)
  • Moreover, the investigators recently demonstrated the ability of this brain functional imaging method to investigate, in healthy volunteers, the functional properties of 5-HT1a autoreceptors through an evaluation of their desensitization after a single oral dose of fluoxetine. (clinicaltrials.gov)
  • We confirmed that TAAR1 was activated by dopamine, norepinephrine, and serotonin and demonstrated that TAAR1 signaling was attenuated by monoamine autoreceptors at exposure to dopamine, norepinephrine, and serotonin. (aspetjournals.org)
  • Here, we performed patch-clamp electrophysiology and fast-scan cyclic voltammetry in mouse brain slices to determine the effects of NT on dopamine autoreceptor-mediated neurotransmission. (jneurosci.org)
  • The presynaptic alpha-2 autoreceptors in pig brain cortex are alpha-2A. (aspetjournals.org)
  • The presynaptic alpha-2 autoreceptors in pig brain cortex were subclassified in terms of alpha-2A, alpha-2B, alpha-2C and alpha-2D to test the hypothesis that alpha-2 autoreceptors belong predominantly to the alpha-2A/D pair of orthologous alpha-2 adrenoceptors. (aspetjournals.org)
  • The pKd values at the presynaptic alpha-2 autoreceptors in pig brain cortex correlated excellently with pKd values at previously subclassified alpha-2A sites but did not correlate significantly or correlated much less well with pKd values at alpha-2B, alpha-2C and alpha-2D sites. (aspetjournals.org)
  • Also, ratios of Kd values of the antagonists at the presynaptic alpha-2 autoreceptors in pig brain cortex agreed well with ratios at previously subclassified alpha-2A sites but not with those at previously subclassified alpha-2B-D sites. (aspetjournals.org)
  • It is concluded that the alpha-2 autoreceptors in pig brain cortex are alpha-2A, in accordance with the hypothesis mentioned. (aspetjournals.org)
  • There is, however, some controversy as to whether or not all brain regions possess autoreceptors. (baillement.com)
  • The fact that neurochemical and electrophysiological signs of DA autoreceptor stimulation can be induced in approximately the same dose range by DA agonists as the doses required to induce yawning and suppression of exploration has been interpreted as a causal connection. (baillement.com)
  • Recently, considerable efforts have been made to find drugs that are selective agonists on DA autoreceptors which have been motivated by reports on clinical effects of low doses of APO, or other DA agonists, on schizophrenia and hyperkinetic disorders. (baillement.com)
  • The aim of this review is to critically examine the hypothesis that DA autoreceptor stimulation mediate yawning and suppression of exploration . (baillement.com)
  • In the following this hypothesis is referred to as "the autoreceptor hypothesis", a simplified illustration of which is given in Fig. (baillement.com)
  • However, the autoreceptor hypothesis (vide supra) lias recently been questioned by several research groups. (baillement.com)
  • abstract = "Recent evidence suggests that the putative dopamine (DA) autoreceptor antagonists, (+)-AJ 76 and (+)-UH 232, share some neurochemical and behavioral effects with both psychostimulants and neuroleptics. (elsevier.com)
  • Autoreceptors may be located in any part of the cell membrane: in the dendrites, the cell body, the axon, or the axon terminals. (wikipedia.org)
  • In this study, we used transfected cells to evaluate the interaction of the common biogenic amines with TAAR1 and monoamine autoreceptors and clarify whether TAAR1 function is influenced by monoamine autoreceptors at exposure to the common biogenic amines. (aspetjournals.org)
  • Differential roles of these isoforms as autoreceptors are poorly understood. (elifesciences.org)
  • Thus, expression of D2S as the exclusive autoreceptor was insufficient for cocaine-induced plasticity, implying a functional role for the co-expression of D2S and D2L autoreceptors. (elifesciences.org)