Dopamine Antagonists
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.
Dopamine
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.
Domperidone
Receptors, Dopamine D2
Haloperidol
A phenyl-piperidinyl-butyrophenone that is used primarily to treat SCHIZOPHRENIA and other PSYCHOSES. It is also used in schizoaffective disorder, DELUSIONAL DISORDERS, ballism, and TOURETTE SYNDROME (a drug of choice) and occasionally as adjunctive therapy in INTELLECTUAL DISABILITY and the chorea of HUNTINGTON DISEASE. It is a potent antiemetic and is used in the treatment of intractable HICCUPS. (From AMA Drug Evaluations Annual, 1994, p279)
Flupenthixol
Spiperone
Receptors, Dopamine
Pimozide
A diphenylbutylpiperidine that is effective as an antipsychotic agent and as an alternative to HALOPERIDOL for the suppression of vocal and motor tics in patients with Tourette syndrome. Although the precise mechanism of action is unknown, blockade of postsynaptic dopamine receptors has been postulated. (From AMA Drug Evaluations Annual, 1994, p403)
Receptors, Dopamine D1
Trifluperidol
Sulpiride
Butaclamol
Fluphenazine
Ergotism
Tiapamil Hydrochloride
Bromocriptine
Receptors, Dopamine D3
Acremonium
Dopamine Plasma Membrane Transport Proteins
Prolactin
A lactogenic hormone secreted by the adenohypophysis (PITUITARY GLAND, ANTERIOR). It is a polypeptide of approximately 23 kD. Besides its major action on lactation, in some species prolactin exerts effects on reproduction, maternal behavior, fat metabolism, immunomodulation and osmoregulation. Prolactin receptors are present in the mammary gland, hypothalamus, liver, ovary, testis, and prostate.
Dopamine Agents
Antipsychotic Agents
Agents that control agitated psychotic behavior, alleviate acute psychotic states, reduce psychotic symptoms, and exert a quieting effect. They are used in SCHIZOPHRENIA; senile dementia; transient psychosis following surgery; or MYOCARDIAL INFARCTION; etc. These drugs are often referred to as neuroleptics alluding to the tendency to produce neurological side effects, but not all antipsychotics are likely to produce such effects. Many of these drugs may also be effective against nausea, emesis, and pruritus.
Rats, Sprague-Dawley
Dose-Response Relationship, Drug
Receptors, Dopamine D5
Dopamine Uptake Inhibitors
Corpus Striatum
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.
Rats, Inbred Strains
Hormone Antagonists
Raclopride
Nucleus Accumbens
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.
Excitatory Amino Acid Antagonists
Apomorphine
Cocaine
An alkaloid ester extracted from the leaves of plants including coca. It is a local anesthetic and vasoconstrictor and is clinically used for that purpose, particularly in the eye, ear, nose, and throat. It also has powerful central nervous system effects similar to the amphetamines and is a drug of abuse. Cocaine, like amphetamines, acts by multiple mechanisms on brain catecholaminergic neurons; the mechanism of its reinforcing effects is thought to involve inhibition of dopamine uptake.
Neurokinin-1 Receptor Antagonists
Neostriatum
Histamine H2 Antagonists
Drugs that selectively bind to but do not activate histamine H2 receptors, thereby blocking the actions of histamine. Their clinically most important action is the inhibition of acid secretion in the treatment of gastrointestinal ulcers. Smooth muscle may also be affected. Some drugs in this class have strong effects in the central nervous system, but these actions are not well understood.
Levodopa
The naturally occurring form of DIHYDROXYPHENYLALANINE and the immediate precursor of DOPAMINE. Unlike dopamine itself, it can be taken orally and crosses the blood-brain barrier. It is rapidly taken up by dopaminergic neurons and converted to DOPAMINE. It is used for the treatment of PARKINSONIAN DISORDERS and is usually given with agents that inhibit its conversion to dopamine outside of the central nervous system.
Muscarinic Antagonists
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.
Microdialysis
Amphetamine
A powerful central nervous system stimulant and sympathomimetic. Amphetamine has multiple mechanisms of action including blocking uptake of adrenergics and dopamine, stimulation of release of monamines, and inhibiting monoamine oxidase. Amphetamine is also a drug of abuse and a psychotomimetic. The l- and the d,l-forms are included here. The l-form has less central nervous system activity but stronger cardiovascular effects. The d-form is DEXTROAMPHETAMINE.
Interleukin 1 Receptor Antagonist Protein
GABA Antagonists
Neurons
Tyrosine 3-Monooxygenase
Nicotinic Antagonists
Rats, Wistar
Ventral Tegmental Area
A region in the MESENCEPHALON which is dorsomedial to the SUBSTANTIA NIGRA and ventral to the RED NUCLEUS. The mesocortical and mesolimbic dopaminergic systems originate here, including an important projection to the NUCLEUS ACCUMBENS. Overactivity of the cells in this area has been suspected to contribute to the positive symptoms of SCHIZOPHRENIA.
Substantia Nigra
Dopamine and cAMP-Regulated Phosphoprotein 32
A phosphoprotein that was initially identified as a major target of DOPAMINE activated ADENYLYL CYCLASE in the CORPUS STRIATUM. It regulates the activities of PROTEIN PHOSPHATASE-1 and PROTEIN KINASE A, and it is a key mediator of the biochemical, electrophysiological, transcriptional, and behavioral effects of DOPAMINE.
Purinergic P1 Receptor Antagonists
Histamine H1 Antagonists
Drugs that selectively bind to but do not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine. Included here are the classical antihistaminics that antagonize or prevent the action of histamine mainly in immediate hypersensitivity. They act in the bronchi, capillaries, and some other smooth muscles, and are used to prevent or allay motion sickness, seasonal rhinitis, and allergic dermatitis and to induce somnolence. The effects of blocking central nervous system H1 receptors are not as well understood.
Serotonin
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.
Adenosine A2 Receptor Antagonists
Oxidopamine
Histamine Antagonists
Mesencephalon
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.
Radioligand Assay
Adrenergic alpha-1 Receptor Antagonists
Serotonin 5-HT2 Receptor Antagonists
Brain
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.
Norepinephrine
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.
Purinergic P2 Receptor Antagonists
Caudate Nucleus
Drug Interactions
alpha-Methyltyrosine
Serotonin 5-HT3 Receptor Antagonists
Adrenergic alpha-Antagonists
Adrenergic alpha-2 Receptor Antagonists
Nomifensine
An isoquinoline derivative that prevents dopamine reuptake into synaptosomes. The maleate was formerly used in the treatment of depression. It was withdrawn worldwide in 1986 due to the risk of acute hemolytic anemia with intravascular hemolysis resulting from its use. In some cases, renal failure also developed. (From Martindale, The Extra Pharmacopoeia, 30th ed, p266)
Reward
Adenosine A1 Receptor Antagonists
Receptors, Serotonin
Receptors, N-Methyl-D-Aspartate
A class of ionotropic glutamate receptors characterized by affinity for N-methyl-D-aspartate. NMDA receptors have an allosteric binding site for glycine which must be occupied for the channel to open efficiently and a site within the channel itself to which magnesium ions bind in a voltage-dependent manner. The positive voltage dependence of channel conductance and the high permeability of the conducting channel to calcium ions (as well as to monovalent cations) are important in excitotoxicity and neuronal plasticity.
Binding, Competitive
Dihydroxyphenylalanine
Synaptic Transmission
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.
Adrenergic Antagonists
Methamphetamine
GABA-A Receptor Antagonists
Leukotriene Antagonists
Angiotensin Receptor Antagonists
Vesicular Monoamine Transport Proteins
Biogenic Monoamines
Putamen
Dizocilpine Maleate
A potent noncompetitive antagonist of the NMDA receptor (RECEPTORS, N-METHYL-D-ASPARTATE) used mainly as a research tool. The drug has been considered for the wide variety of neurodegenerative conditions or disorders in which NMDA receptors may play an important role. Its use has been primarily limited to animal and tissue experiments because of its psychotropic effects.
Analysis of Variance
Prefrontal Cortex
The rostral part of the frontal lobe, bounded by the inferior precentral fissure in humans, which receives projection fibers from the MEDIODORSAL NUCLEUS OF THE THALAMUS. The prefrontal cortex receives afferent fibers from numerous structures of the DIENCEPHALON; MESENCEPHALON; and LIMBIC SYSTEM as well as cortical afferents of visual, auditory, and somatic origin.
Cells, Cultured
Histamine H3 Antagonists
Self Administration
Glutamic Acid
Serotonin Receptor Agonists
Central Nervous System Stimulants
Signal Transduction
The intracellular transfer of information (biological activation/inhibition) through a signal pathway. In each signal transduction system, an activation/inhibition signal from a biologically active molecule (hormone, neurotransmitter) is mediated via the coupling of a receptor/enzyme to a second messenger system or to an ion channel. Signal transduction plays an important role in activating cellular functions, cell differentiation, and cell proliferation. Examples of signal transduction systems are the GAMMA-AMINOBUTYRIC ACID-postsynaptic receptor-calcium ion channel system, the receptor-mediated T-cell activation pathway, and the receptor-mediated activation of phospholipases. Those coupled to membrane depolarization or intracellular release of calcium include the receptor-mediated activation of cytotoxic functions in granulocytes and the synaptic potentiation of protein kinase activation. Some signal transduction pathways may be part of larger signal transduction pathways; for example, protein kinase activation is part of the platelet activation signal pathway.
Pyridines
Catalepsy
A condition characterized by inactivity, decreased responsiveness to stimuli, and a tendency to maintain an immobile posture. The limbs tend to remain in whatever position they are placed (waxy flexibility). Catalepsy may be associated with PSYCHOTIC DISORDERS (e.g., SCHIZOPHRENIA, CATATONIC), nervous system drug toxicity, and other conditions.
Conditioning, Operant
Guinea Pigs
Disease Models, Animal
Calcium Channel Blockers
Serotonin 5-HT1 Receptor Antagonists
Reserpine
An alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria. Reserpine inhibits the uptake of norepinephrine into storage vesicles resulting in depletion of catecholamines and serotonin from central and peripheral axon terminals. It has been used as an antihypertensive and an antipsychotic as well as a research tool, but its adverse effects limit its clinical use.
Stereotyped Behavior
Naloxone
Indoles
Naltrexone
Derivative of noroxymorphone that is the N-cyclopropylmethyl congener of NALOXONE. It is a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction. The FDA has approved naltrexone for the treatment of alcohol dependence.
Parkinsonian Disorders
A group of disorders which feature impaired motor control characterized by bradykinesia, MUSCLE RIGIDITY; TREMOR; and postural instability. Parkinsonian diseases are generally divided into primary parkinsonism (see PARKINSON DISEASE), secondary parkinsonism (see PARKINSON DISEASE, SECONDARY) and inherited forms. These conditions are associated with dysfunction of dopaminergic or closely related motor integration neuronal pathways in the BASAL GANGLIA.
Brain Chemistry
Clozapine
A tricylic dibenzodiazepine, classified as an atypical antipsychotic agent. It binds several types of central nervous system receptors, and displays a unique pharmacological profile. Clozapine is a serotonin antagonist, with strong binding to 5-HT 2A/2C receptor subtype. It also displays strong affinity to several dopaminergic receptors, but shows only weak antagonism at the dopamine D2 receptor, a receptor commonly thought to modulate neuroleptic activity. Agranulocytosis is a major adverse effect associated with administration of this agent.
Antiparkinson Agents
Calcium
A basic element found in nearly all organized tissues. It is a member of the alkaline earth family of metals with the atomic symbol Ca, atomic number 20, and atomic weight 40. Calcium is the most abundant mineral in the body and combines with phosphorus to form calcium phosphate in the bones and teeth. It is essential for the normal functioning of nerves and muscles and plays a role in blood coagulation (as factor IV) and in many enzymatic processes.
Synaptosomes
Neurotransmitter Agents
Receptors, Endothelin
Cyclic AMP
Adrenergic beta-2 Receptor Antagonists
Plasticity of first-order sensory synapses: interactions between homosynaptic long-term potentiation and heterosynaptically evoked dopaminergic potentiation. (1/1654)
Persistent potentiations of the chemical and electrotonic components of the eighth nerve (NVIII) EPSP recorded in vivo in the goldfish reticulospinal neuron, the Mauthner cell, can be evoked by afferent tetanization or local dendritic application of an endogenous transmitter, dopamine (3-hydroxytyramine). These modifications are attributable to the activation of distinct intracellular kinase cascades. Although dopamine-evoked potentiation (DEP) is mediated by the cAMP-dependent protein kinase (PKA), tetanization most likely activates a Ca2+-dependent protein kinase via an increased intracellular Ca2+ concentration. We present evidence that the eighth nerve tetanus that induces LTP does not act by triggering dopamine release, because it is evoked in the presence of a broad spectrum of dopamine antagonists. To test for interactions between these pathways, we applied the potentiating paradigms sequentially. When dopamine was applied first, tetanization produced additional potentiation of the mixed synaptic response, but when the sequence was reversed, DEP was occluded, indicating that the synapses potentiated by the two procedures belong to the same or overlapping populations. Experiments were conducted to determine interactions between the underlying regulatory mechanisms and the level of their convergence. Inhibiting PKA does not impede tetanus-induced LTP, and chelating postsynaptic Ca2+ with BAPTA does not block DEP, indicating that the initial steps of the induction processes are independent. Pharmacological and voltage-clamp analyses indicate that the two pathways converge on functional AMPA/kainate receptors for the chemically mediated EPSP and gap junctions for the electrotonic component or at intermediaries common to both pathways. A cellular model incorporating these interactions is proposed on the basis of differential modulation of synaptic responses via receptor-protein phosphorylation. (+info)Measurement of striatal D2 dopamine receptor density and affinity with [11C]-raclopride in vivo: a test-retest analysis. (2/1654)
Subacute and long-term stability of measurements of D2 dopamine receptor density (Bmax), affinity (Kd) was studied with positron emission tomography in eight healthy male volunteers. [11C]-Raclopride and the transient equilibrium method were used to measure D2 receptor characteristics. The interval between measurements (scan pairs) was 3 to 7 weeks (subacute) for four subjects and 6 to 11 months (long-term) for four subjects. A test-retest analysis of quantitative measurements of D2 receptor Bmax and Kd was compared with that done on binding potential (BP, Bmax/Kd) measures. In addition, the effect of error in defining the transient equilibrium time (tmax) in the parameter estimation procedure was explored with simulations. The subacute test-retest indicates good reproducibility of D2 receptor density, affinity, and BP ratio measurements with intraclass correlation coefficients of 0.90, 0.96, and 0.86, respectively. The variability of the measurements after 6 to 11 months was slightly higher than that seen in a subacute testing for Kd and more clearly so for binding potential and Bmax. The absolute variability in Bmax (14.5%) measurements was consistently higher than that of Kd (8.4%) or BP (7.9%) both in subacute and long-term measurements. Simulations indicated that the Bmax and Kd estimation procedure is more sensitive to error in the tmax than that for the BP. The results indicate a good overall stability of the equilibrium method with [11C]raclopride for measuring dopamine D2 receptor binding characteristics in the striatum. The BP approach is more stable than Kd and especially Bmax measurements. Error in defining the tmax in particular in the low specific radioactivity scan may be one source of greater variability in Bmax versus BP. However, a higher intraindividual variability in measurements of the D2 receptor Bmax also may include a component of continuous regulation of this parameter over time. These methodologic aspects should be considered in the design and interpretation of longitudinal studies on D2 dopamine receptor characteristics with [11C]-raclopride. (+info)Behavioral, toxic, and neurochemical effects of sydnocarb, a novel psychomotor stimulant: comparisons with methamphetamine. (3/1654)
Sydnocarb (3-(beta-phenylisopropyl)-N-phenylcarbamoylsydnonimine) is a psychostimulant in clinical practice in Russia as a primary and adjunct therapy for a host of psychiatric disorders, including schizophrenia and depression. It has been described as a stimulant with an addiction liability and toxicity less than that of amphetamines. The present study undertook to evaluate the psychomotor stimulant effects of sydnocarb in comparison to those of methamphetamine. Sydnocarb increased locomotor activity of mice with reduced potency (approximately 10-fold) and efficacy compared with methamphetamine. Sydnocarb blocked the locomotor depressant effects of haloperidol at doses that were inactive when given alone. The locomotor stimulant effects of both methamphetamine and sydnocarb were dose-dependently blocked by the dopamine D1 and D2 antagonists SCH 39166 and spiperone, respectively; blockade generally occurred at doses of the antagonists that did not depress locomotor activity when given alone. In mice trained to discriminate methamphetamine from saline, sydnocarb fully substituted for methamphetamine with a 9-fold lower potency. When substituted for methamphetamine under self-administration experiments in rats, 10-fold higher concentrations of sydnocarb maintained responding by its i.v. presentation. Sydnocarb engendered stereotypy in high doses with approximately a 2-fold lower potency than methamphetamine. However, sydnocarb was much less efficacious than methamphetamine in inducing stereotyped behavior. Both sydnocarb and methamphetamine increased dialysate levels of dopamine in mouse striatum; however, the potency and efficacy of sydnocarb was less than methamphetamine. The convulsive effects of cocaine were significantly enhanced by the coadministration of nontoxic doses of methamphetamine but not of sydnocarb. Taken together, the present findings indicate that sydnocarb has psychomotor stimulant effects that are shared by methamphetamine while demonstrating a reduced behavioral toxicity. (+info)Depression of peripheral chemosensitivity by a dopaminergic mechanism in patients with obstructive sleep apnoea syndrome. (4/1654)
In the present study, respiratory drives to chemical stimuli and peripheral chemosensitivity were evaluated in patients with obstructive sleep apnoea (OSAS). The effects of oral administration of domperidone, a selective dopamine D2-receptor antagonist, were also examined, to study the respiratory effects of endogenous dopamine on peripheral chemoreceptors. Sixteen patients with OSAS and nine normal control subjects were studied. Respiratory responses to hypercapnia and hypoxia were measured using the rebreathing method and isocapnic progressive hypoxia method, respectively. The hypoxic withdrawal test, which measures the decrease in ventilation caused by two breaths of 100% O2 under mild hypercapnic hypoxic conditions (end-tidal oxygen and carbon dioxide tensions approximately 8.0 kPa and 5.3-6.7 kPa, respectively), was used to evaluate peripheral chemosensitivity. In the patients with OSAS, ventilatory responses to hypercapnia and hypoxia were significantly decreased compared with those of control subjects. Hypoxic withdrawal tests showed that peripheral chemosensitivity was significantly lower in patients with OSAS than in normal subjects. Hypercapnic ventilatory response and peripheral chemosensitivity were enhanced by administration of domperidone in the patients with OSAS, although no changes in either of these were observed in the control subjects. The hypoxic ventilatory response and peripheral chemosensitivity in the patients with OSAS were each significantly correlated with severity of hypoxia during sleep. These findings suggest that peripheral chemosensitivity in patients with obstructive sleep apnoea syndrome may be decreased as a result of abnormality in dopaminergic mechanisms and that the reduced chemosensitivity observed in patients with obstructive sleep apnoea syndrome may affect the severity of hypoxia during sleep. (+info)(-)-Stepholidine enhances K+ depolarization-induced activation of synaptosomal tyrosine 3-monooxygenase from rat striatum. (5/1654)
AIM: To study the mechanism of K+ depolarization-induced activation of synaptosomal tyrosine 3-monooxygenase (TM) in rat striatum and the effect of (-)-stepholidine (SPD) on this activation. METHODS: The TM was assayed for DOPA by HPLC-ECD; the activities of Ca2+/calmodulin (CaM)-dependent protein kinase (PK II) and Ca2+/phosphoinositide-dependent protein kinase (PKC) were assayed using histidine as substrate. RESULTS: The incubation of striatal synaptosomes in K(+)-riched (60 mmol.L-1) medium resulted in a marked activation of TM. PKC inhibitor polymyxin B (PMB) completely blocked the activation of K+ 60 mmol.L-1 on TM. Selective D2 receptor agonist quinpirole (QP), Ca2+ removal from incubation medium and CaM antagonist W7 failed to affect the activation. However, SPD enhanced the activation of K+ 60 mmol.L-1 on TM. Meanwhile, the incubation in K+ 60 mmol.L-1 also activated PKC. Neither QP nor SPD affected K+ depolarization-induced activation of PKC. CONCLUSION: The activation of K+ depolarization on synaptosomal TM is enhanced by SPD and this activation is mediated by PKC rather than by PK II. (+info)Preproopiomelanocortin and preprodynorphin mRNA expressions in rat brain after electroacupuncture + droperidol. (6/1654)
AIM: To study the expression of preproopiomelanocortin (POMC) and preprodynorphin (PPD) mRNA following the combination of electroacupuncture (EA) with droperidol (Dro), a dopamine receptor antagonist. METHODS: The brains and spinal cords of Sprague-Dawley rats were sectioned after combination of EA with Dro, and the gene expression was investigated using nonradioactive in situ hybridization histochemistry (ISHH). RESULTS: Ten hours after EA, the POMC mRNA expression was enhanced; the expression was further enhanced when EA was combined with Dro. The expression of PPD mRNA showed regional difference in central nervous system (CNS): in spinal cord, EA enhanced the PPD mRNA expression and the combination of EA with Dro further promoted the expression; in the brain, the PPD mRNA expression after EA or combination of EA with Dro showed no obvious change in most regions (caudate-putamen, accumbens, arcuate nucleus of hypothalamus) or was decreased in supraoptic nucleus. CONCLUSION: Dro combined with EA promoted the expression of POMC mRNA in CNS and PPD mRNA in spinal cord, but reduced or had no effect on PPD mRNA expression in the brain. (+info)Chimeric dopamine D2/angiotensin AT1 receptors: role of the length of third intracellular loop of D2 receptors in conferring specificity of receptor binding and G-protein coupling. (7/1654)
AIM: To define roles of the third intracellular loop (IL3) length of G-protein coupled receptors in conferring the specificity for receptor binding and G-protein coupling. METHODS: By polymerase chain reaction (PCR), the IL3 of D2 receptor was replaced with the counter part of AT1 receptor which has the shortest loop among all G-protein coupled receptors. D2/AT1 receptor cDNA was then stably transfected into Chinese hamster ovary cells and a clone with high level expression was obtained for receptor binding and agonist-induced phosphatidylinositols (PI) turnover experiments. RESULTS: Comparing to the D2 receptor, D2/AT1 chimeric receptor had lower affinities for all D2 receptor antagonists tested (spiperone, haloperidol, (+)-butaclamol, chlopromazine, clozapine, trifluoperdazine) and different affinity profiles to agonists (apomorphine, dopamine, quinpirole, bromocriptine). But the chimeric receptor failed to couple to G-protein and subsequent stimulation of PI turnover. CONCLUSION: The length of IL3 of D2 receptor participates defining recpetor binding sites conformation, and structure beyond IL3 may affect receptor G-protein coupling. (+info)Characteristics of tetrahydroprotoberberines on dopamine D1 and D2 receptors in calf striatum. (8/1654)
AIM: To study the characteristics of tetrahydroprotoberberines (THPB) on dopamine D1 and D2 receptors and elucidate their structure-activity relationship. METHODS: Radioligand assay in vitro with a two-site model program analysis. RESULTS: Four THPB with two hydorxyl groups on C2 and C9 or C2 and C10 exhibited RH and RL two binding sites to D1 receptors and guanosine triphosphate regulated the RH binding site of SPD and THPB-132A in competition assay, while eleven THPB including nonhydroxy-THPB, monohydroxy-THPB, and THPB with two hydroxyl groups attaching to C3 and C10 showed one binding site to D1 receptors under the same conditions. However, the tested eleven THPB all manifested one binding site to D2 receptors in competition assay, and the 2-hydroxy-THPB had the most potent affinity for D2 receptors. CONCLUSION: Dihydroxy-THPB with two hydroxyl groups attaching to C2 and C9 or C2 and C10 possess the intrinsic activity of agonist to D1 receptors, while the other THPB do not. The tested eleven THPB all are the antagonists of D2 receptors. (+info)Antidopaminergic therapy for managing comorbidities in patients with Parkinsons disease.
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Trimethobenzamide
"Dopamine receptor antagonists". Ann Palliat Med. 1 (2): 137-42. doi:10.3978/j.issn.2224-5820.2012.07.09. PMID 25841474. Waknine ... Trimethobenzamide is an antagonist of the D2 receptor. It is believed to affect the chemoreceptor trigger zone (CTZ) of the ...
Abulia
... dopamine antagonists). Treat depression efficaciously when both DDM and depression are present. Increase motivation through use ... As a result of more and more evidence showing that the mesolimbic and the mesocortical dopamine system are key to motivation ... of stimulants, dopamine agonists, or other agents such as cholinesterase inhibitors. A case of abulia after a transient ... and responsiveness to reward, abulia may be a dopamine-related dysfunction. Abulia may also result from a variety of brain ...
SB-277,011-A
SB-277,011A is a drug which acts as a potent and selective dopamine D3 receptor antagonist, which is around 80-100x selective ... Malik P, Andersen MB, Peacock L (August 2004). "The effects of dopamine D3 agonists and antagonists in a nonhuman primate model ... Ross JT, Corrigall WA, Heidbreder CA, LeSage MG (March 2007). "Effects of the selective dopamine D3 receptor antagonist SB- ... September 2000). "Pharmacological actions of a novel, high-affinity, and selective human dopamine D(3) receptor antagonist, SB- ...
Piribedil
Dopamine antagonists reduce the effect of piribedil. Dopamine receptor agonist, selective for subtypes D2 and D3. Dopamine ... Agonist and Antagonist Properties at Subtypes of Dopamine D2-Like Receptor and α1/α2-Adrenoceptor" (PDF). J. Pharmacol. Exp. ... Adrenergic receptor antagonist, subtypes α2A and α2C: could be the reason why piribedil seems to cause less drowsiness than ... As with other dopamine agonists (like pramipexole and ropinirole), compulsive behavior like pathological gambling, overeating, ...
Dystonia
In contrast, dopamine antagonists can sometimes cause dystonia.)[citation needed] Ketogenic diet One complex case study found ... Parkinsonian drugs Dopamine agonists: One type of dystonia, dopamine-responsive dystonia, can be completely treated with ... dopamine agonists (such as ropinirole and bromocriptine), and muscle relaxants (such as diazepam).[citation needed] ... called myoclonic dystonia where some cases are hereditary and have been associated with a missense mutation in the dopamine-D2 ...
Iloperidone
The older typical antipsychotics are primarily dopamine antagonists. Iloperidone has been shown to act as an antagonist at all ... It exhibits high (nM) affinity to serotonin 5HT2A (Ki value of 5.6 nM), dopamine D2 (6.3 nM) and D3 (7.1 nM) and noradrenaline ... Iloperidone exerts its effects by acting upon and antagonizing specific neurotransmitters, particularly multiple dopamine and ... dopamine D1 and histamine H1 receptors. In addition, pharmacogenomic studies identified single nucleotide polymorphisms ...
General anaesthetic
Dopamine receptor antagonists have sedative and antiemetic properties. Previously, they were used in parallel with opioids to ... an NMDA receptor antagonist, is used primarily for its analgesic effects and in an off-label capacity for its anti-depressant ...
Azapride
... is the azide derivative of the dopamine antagonist clebopride synthesized in order to label dopamine receptors. It is ... Dopamine antagonists, Organoazides, Chlorobenzenes, Salicylamide ethers, Piperidines, Irreversible antagonists, All stub ... an irreversible dopamine antagonist. Niznik HB, Guan JH, Neumeyer JL, Seeman P (February 1985). "A photoaffinity ligand for ... Wouters W, Van Dun J, Laduron PM (December 1984). "Photoaffinity labelling of dopamine receptors. Synthesis and binding ...
Andre Soriano
"Dopamine Antagonist - Andre Soriano Bridal Campaign". YouTube. July 26, 2013. "Not For the Classic Princess: Extreme Bridal by ...
Zuclopenthixol
As with other dopamine antagonists, zuclopenthixol may sometimes elevate prolactin levels; this may occasionally result in ... Zuclopenthixol is a D1 and D2 antagonist, α1-adrenergic and 5-HT2 antagonist. While it is approved for use in Australia, Canada ... An increase in the incidence of pancreatic islet cell tumours has been observed for some other D2 antagonists. The ... An increase in the incidence of mammary adenocarcinomas is a common finding for D2 antagonists which increase prolactin ...
Antagonism (chemistry)
Antagonists such as dopamine antagonist slow down movement in lab rats. Although they hinder the joining of enzymes to ... Claussen, C. M.; Witte, L. J.; Dafny, N (2015). "Single exposure of dopamine D1 antagonist prevents and D2 antagonist ... For instance, a receptor antagonist is an agent that reduces the response that a ligand produces when the receptor antagonist ... The effects of antagonists can be seen after they have encountered an agonist, and as a result, the effects of the agonist is ...
Sonepiprazole
Arnsten AF, Murphy B, Merchant K (October 2000). "The selective dopamine D4 receptor antagonist, PNU-101387G, prevents stress- ... Mansbach RS, Brooks EW, Sanner MA, Zorn SH (January 1998). "Selective dopamine D4 receptor antagonists reverse apomorphine- ... June 1996). "(S)-(−)-4-[4-[2-(isochroman-1-yl)ethyl]-piperazin-1-yl] benzenesulfonamide, a selective dopamine D4 antagonist". ... August 1997). "Chromeno[3,4-c]pyridin-5-ones: selective human dopamine D4 receptor antagonists as potential antipsychotic ...
PNU-99,194
Carr KD, Yamamoto N, Omura M, Cabeza de Vaca S, Krahne L (August 2002). "Effects of the D(3) dopamine receptor antagonist, ... Rodríguez-Arias M, Felip CM, Broseta I, Miñarro J (May 1999). "The dopamine D3 antagonist U-99194A maleate increases social ... Rogóz Z, Kłodzińska A, Maj J (2000). "Anxiolytic-like effect of nafadotride and PNU 99194A, dopamine D3 receptor antagonists in ... Gyertyán I, Sághy K (July 2004). "Effects of dopamine D3 receptor antagonists on spontaneous and agonist-reduced motor activity ...
Cabergoline
Agonist and antagonist properties at subtypes of dopamine D(2)-like receptor and alpha(1)/alpha(2)-adrenoceptor". J Pharmacol ... Dopamine antagonists such as antipsychotics and metoclopramide counteract some effects of cabergoline. The use of ... March 2010). "Can dopamine agonists reduce the incidence and severity of OHSS in IVF/ICSI treatment cycles? A systematic review ... Agonist and antagonist properties at serotonin, 5-HT(1) and 5-HT(2), receptor subtypes". J Pharmacol Exp Ther. 303 (2): 815-22 ...
Tiapride
... is a dopamine D2 and D3 receptor antagonist. It is more selective than other neuroleptic drugs such as haloperidol and ... This is because dopamine plays a primary role in regulating prolactin release by binding to D2 receptors on prolactin-secreting ... Tiapride is a drug that selectively blocks D2 and D3 dopamine receptors in the brain. It is used to treat a variety of ... Dopamine hyperactivity has been linked with alcohol withdrawal syndrome (AWS), suggesting that tiapride's antidopaminergic ...
Chloroethylnorapomorphine
... is a chemical once thought to be an irreversible dopamine D2 receptor antagonist; however, it was ... Lehmann, J; Langer, SZ (1982). "Dopamine autoreceptors differ pharmacologically from postsynaptic dopamine receptors: Effects ... an irreversible dopamine receptor antagonist". Journal of Medicinal Chemistry. 26 (10): 1348-53. doi:10.1021/jm00364a003. PMID ... an irreversible ligand for dopamine receptors: synthesis and application". Journal of Medicinal Chemistry. 27 (6): 806-10. doi: ...
Paroxysmal sympathetic hyperactivity
Chlorpromazine and haloperidol, both dopamine antagonists, in some cases have worsened PSH symptoms. These drugs are in use ... It may also increase sympathetic inhibition in the brainstem.[medical citation needed] Bromocriptine is a dopamine agonist that ... Other drugs that have been used and have in some cases been helpful are dopamine agonists, other various opiates, ...
UH-232
"Effects of intrastriatal infusion of D2 and D3 dopamine receptor preferring antagonists on dopamine release in rat dorsal ... UH-232 ((+)-UH232) is a drug which acts as a subtype selective mixed agonist-antagonist for dopamine receptors, acting as a ... Lahti AC, Weiler M, Carlsson A, Tamminga CA (1998). "Effects of the D3 and autoreceptor-preferring dopamine antagonist (+)- ... "The dopamine D3 receptor and autoreceptor preferring antagonists (+)-AJ76 and (+)-UH232; a microdialysis study". European ...
Allyl cyanide
Treatment by serotonin and dopamine antagonists caused a reduction in the behavioral abnormalities. Ataxia, trembling, ... The serotonin and dopamine systems are thought to be involved in the behavioral abnormalities caused by allyl cyanide. ...
Complications of pregnancy
Second-line treatments include vitamin B6 +/- doxylamine, antihistamines, dopamine antagonists, and serotonin antagonists. ...
Vomiting
Hence, anticholinergics, antihistamines, dopamine antagonists, serotonin antagonists, and cannabinoids are used as antiemetics ... The chemoreceptor trigger zone at the base of the fourth ventricle has numerous dopamine D2 receptors, serotonin 5-HT3 ...
Pimavanserin
... pimavanserin is not a dopamine receptor antagonist. Pimavanserin acts as an inverse agonist and antagonist at serotonin 5-HT2A ... dopamine (including D2), muscarinic acetylcholine, histamine, or adrenergic receptors, or to calcium channels. Pimavanserin has ... 5-HT2A antagonists, Atypical antipsychotics, Fluoroarenes, Phenol ethers, Piperidines, Ureas, Breakthrough therapy). ... selectivity for this site over the 5-HT2C receptor and no significant affinity or activity at the 5-HT2B receptor or dopamine ...
Ecopipam
... is a selective dopamine D1 and D5 receptor antagonist. It shows little affinity for either dopamine D2-like or 5-HT2 ... Ecopipam acts as a selective dopamine D1 and D5 receptor antagonist. It is orally active, has an elimination half-life of 10 ... Haney M, Ward AS, Foltin RW, Fischman MW (June 2001). "Effects of ecopipam, a selective dopamine D1 antagonist, on smoked ... Ecopipam (development codes SCH-39166, EBS-101, and PSYRX-101) is a dopamine antagonist which is under development for the ...
L-745,870
... is a drug which acts as a dopamine receptor antagonist selective for the D4 subtype, and has antipsychotic effects in ... Moustgaard A, Hau J, Lind NM (2008). "Effects of dopamine D4 receptor antagonist on spontaneous alternation in rats". ... a novel dopamine D4 receptor antagonist". Trends in Pharmacological Sciences. 18 (6): 186-8. doi:10.1016/s0165-6147(97)01066-3 ... D4 antagonists, Pyrrolopyridines, Phenylpiperazines, Chloroarenes, All stub articles, Nervous system drug stubs). ...
Raclopride
It acts as a selective antagonist on D2 dopamine receptors. It has been used in trials studying Parkinson Disease. Its ... A potent substituted benzamide drug with high affinity for dopamine D-2 receptors in the rat brain". Biochemical Pharmacology. ... Ishibashi K, Ishii K, Oda K, Mizusawa H, Ishiwata K (2010). "Competition between 11C-raclopride and endogenous dopamine in ... Farde L, Gustavsson JP, Jönsson E (1997). "D2 dopamine receptors and personality traits". Nature. 385 (6617): 590. doi:10.1038/ ...
Nociceptin receptor
Nociceptin is thought to be an endogenous antagonist of dopamine transport that may act either directly on dopamine or by ... Liu Z, Wang Y, Zhang J, Ding J, Guo L, Cui D, Fei J (March 2001). "Orphanin FQ: an endogenous antagonist of rat brain dopamine ... Antagonists targeting NOP are under investigation for their role as treatments for depression and Parkinson's disease, whereas ... Administration of the NOPr antagonist SB-612,111 has been shown to inhibit this process. More recently a range of selective ...
Postcholecystectomy syndrome
Treatment for EPS and PDS can both include proton pump inhibitors and dopamine antagonists. Tricyclic antidepressants have also ...
Atypical antipsychotic
This brake is disrupted through action of a 5-HT2A antagonist, which disinhibits the dopamine neuron, stimulating dopamine ... Miyake, N; Miyamoto, S; Jarskog, LF (October 2012). "New serotonin/dopamine antagonists for the treatment of schizophrenia: are ... The atypical antipsychotics (AAP), also known as second generation antipsychotics (SGAs) and serotonin-dopamine antagonists ( ... "Modulation of striatal dopamine release by 5-HT2A and 5-HT2C receptor antagonists: [11C]raclopride PET studies in the rat". ...
Excoriation disorder
Opioid antagonists work by affecting dopamine circuitry, thereby decreasing the pleasurable effects of picking. Another class ... Studies have shown a linkage between dopamine and the urge to pick. Drugs such as cocaine and methamphetamine, which increase ... While there have been no human studies of opioid antagonists for the treatment of excoriation disorder, there have been studies ... Thus, excoriation disorder could result from a dysfunction in the dopamine reward functions. There may be another neurological ...
Domperidone
... acts as a peripherally selective antagonist of the dopamine D2 and D3 receptors. Due to its low entry into the ... Domperidone, sold under the brand name Motilium among others, is a dopamine antagonist medication which is used to treat nausea ... Domperidone is a peripherally selective dopamine D2 and D3 receptor antagonist. It has no clinically significant interaction ... and started searching for a dopamine antagonist that would not pass the blood-brain barrier, thereby being free of the ...
Holecistokininski receptor B
Holecistokininski antagonist. Reference[uredi - уреди , uredi kôd]. *↑ Noble F, Roques BP (July 1999). „CCK-B receptor: ... Altar CA, Boyar WC (April 1989). „Brain CCK-B receptors mediate the suppression of dopamine release by cholecystokinin". Brain ... Boyce S, Rupniak NM, Tye S, Steventon MJ, Iversen SD (August 1990). „Modulatory role for CCK-B antagonists in Parkinson's ... Dourish CT, O'Neill MF, Coughlan J, Kitchener SJ, Hawley D, Iversen SD (January 1990). „The selective CCK-B receptor antagonist ...
BMY-7378
BMY-7,378 is a 5-HT1A receptor weak partial agonist/antagonist and α1D-adrenergic receptor antagonist.[1] ... Dopamine. *Ebalzotan. *Eltoprazine. *Enciprazine. *Ergolines (e.g., bromocriptine, cabergoline, dihydroergotamine, ergotamine, ... Antagonists: AR-A000002. *Beta blockers (e.g., alprenolol, carteolol, isamoltane, oxprenolol, penbutolol, propranolol, ... Antagonists: ABT-354. *Atypical antipsychotics (e.g., aripiprazole, asenapine, clorotepine, clozapine, fluperlapine, ...
Cannabinoid
N-Arachidonoyl dopamine (NADA)Edit. Main article: N-Arachidonoyl dopamine. Discovered in 2000, NADA preferentially binds to the ... Although it is a full agonist at CB2 and a partial agonist at CB1, it behaves as a CB1 antagonist in vivo. In rats, virodhamine ... Although in this intercellular signaling role they are similar to the well-known monoamine neurotransmitters such as dopamine, ... Cannabidiol has little affinity for CB1 and CB2 receptors but acts as an indirect antagonist of cannabinoid agonists.[24] It ...
അഡിനോസിൻ ഡൈഫോസ്ഫേറ്റ് - വിക്കിപീഡിയ
Dopamine. *Epinephrine (adrenaline). *NAS (normelatonin). *Norepinephrine (noradrenaline). *Serotonin (5-HT); Trace amines: 3- ... Antagonists: 8-Chlorotheophylline. *8-Phenyl-1,3-dipropylxanthine. *8-Phenyltheophylline. *Acefylline. *Aminophylline ...
Dopamine agonist
NMDA receptor antagonists (e.g., DXM, ketamine, methoxetamine, nitrous oxide, phencyclidine, inhalants) ... Dopamine agonists act directly on the dopamine receptors and mimic dopamine's effect.[1] Dopamine agonists have two subclasses ... A dopamine agonist (DA) is a compound that activates dopamine receptors. There are two families of dopamine receptors, D2-like ... Dopamine[edit]. When dopamine interacts with ATP, which is a component of some dopamine receptors, it has a significant ...
A-967079
... is a drug which acts as a potent and selective antagonist for the TRPA1 receptor. It has analgesic and ... N-Arachidonoyl dopamine. *N-Oleoyldopamine. *N-Oleoylethanolamide. *Nonivamide (PAVA) (PAVA spray). *Nordihydrocapsaicin (chili ... a single amino acid dictates species-specific actions of the most potent mammalian TRPA1 antagonist". The Journal of Biological ... "TRPA1 and CGRP antagonists counteract vesicant-induced skin injury and inflammation". Toxicology Letters. 293: 140-148. doi ...
Neurotoxin
Ben-Shachar D, Zuk R, Glinka Y (1995). "Dopamine neurotoxicity: inhibition of mitochondrial respiration". J. Neurochem. 64 (2 ... Cruz, Lourdes J.; Olivera, Baldomero M. (1987). "Calcium Channel Antagonists ω-Conotoxin Defines a New High Affinity Site". The ... Receptor agonists and antagonistsEdit. Anatoxin-aEdit. .mw-parser-output .infobox-subbox{padding:0;border:none;margin:-3px; ... The use of the acetylcholinesterase inhibitor Neostigmine or the muscarinic acetylcholine antagonist atropine (which will ...
Substance dependence
In rat models, the separate use of CRF inhibitors and CRF receptor antagonists both decreased self-administration of the drug ... dynorphin peptides reduce dopamine release into the NAcc by temporarily inhibiting the reward pathway. A sustained activation ... Expression of CaMKII and c-fos is attenuated by NMDA receptor antagonists, which is associated with blunted withdrawal in adult ... which is supported by the attenuation of withdraw by NMDA receptor antagonists.[23] Physical dependence on opioids has been ...
Trifluoromethylphenylpiperazine
Antagonists: AR-A000002. *Beta blockers (e.g., alprenolol, carteolol, isamoltane, oxprenolol, penbutolol, propranolol, ... and dopamine levels produced by the BZP/TFMPP combination, this mixture of drugs produces effects which crudely mimic those of ... Antagonists: ABT-354. *Atypical antipsychotics (e.g., aripiprazole, asenapine, clorotepine, clozapine, fluperlapine, ... Antagonists: Agomelatine. *Atypical antipsychotics (e.g., amisulpride, aripiprazole, asenapine, brexpiprazole, cariprazine, ...
HS665
Also indirect D2 agonists, such as dopamine reuptake inhibitors (cocaine, methylphenidate), releasing agents (amphetamine, ... Antagonists: (3S,4S)-Picenadol. *2-(S)-N,N-(R)-Viminol. *3CS-nalmefene ...
G protein
These include receptor antagonists, neurotransmitters, neurotransmitter reuptake, G protein-coupled receptors, G proteins, ... for research on neurotransmitters such as dopamine, which act via GPCRs. ...
LY-456220
Antagonists: AR-A000002. *Beta blockers (e.g., alprenolol, carteolol, isamoltane, oxprenolol, penbutolol, propranolol, ... LY-456220 lacks significant affinity for the 5-HT1B, α1 adrenergic, and dopamine D2 receptors.[1][2] ... Antagonists: ABT-354. *Atypical antipsychotics (e.g., aripiprazole, asenapine, clorotepine, clozapine, fluperlapine, ... LY-456220 is a potent and selective serotonin 5-HT1D receptor antagonist which has been used in research to study the function ...
Taranabant
Cannabinoid receptor antagonist. References[edit]. .mw-parser-output .reflist{font-size:90%;margin-bottom:0.5em;list-style-type ... N-Arachidonoyl dopamine (NADA). *N-Arachidonylglycine (NAGly). *2-Arachidonoyl lysophosphatidylinositol (2-ALPI) ...
Tetrahydrocannabiphorol
"Manipulation of the tetrahydrocannabinol side chain delineates agonists, partial agonists, and antagonists". The Journal of ... N-Arachidonoyl dopamine (NADA). *N-Arachidonylglycine (NAGly). *2-Arachidonoyl lysophosphatidylinositol (2-ALPI) ...
Stuttering - Simple English Wikipedia, the free encyclopedia
Dopamine antagonists. Prognosis. Usually resolves by late childhood; 20% of cases last into adulthood. ...
Ligand-gated ion channel
Dopamine receptor agonist. *Dopamine receptor antagonist. *Dopamine reuptake inhibitor (DRI). Histaminergic. *Histamine ... Antagonists: ketamine, PCP, dextropropoxyphene, ketobemidone, tramadol, kynurenic acid (endogenous), etc.. ATP-gated channels[ ... Antagonists: CNQX, Kynurenic acid, NBQX, Perampanel, Piracetam, etc.. *Positive allosteric modulators: Aniracetam, ... The AMPA receptor bound to a glutamate antagonist showing the amino terminal, ligand binding, and transmembrane domain, PDB ...
Lisdexamfetamine
... whereas antagonists of D2 type dopamine receptors typically slow timing;... Depletion of dopamine in healthy volunteers impairs ... Dopamine-β-hydroxylase catalyzed the removal of the pro-R hydrogen atom and the production of 1-norephedrine, (2S,1R)-2-amino-1 ... CYP2D6, dopamine β-hydroxylase (DBH), flavin-containing monooxygenase 3 (FMO3), butyrate-CoA ligase (XM-ligase), and glycine N- ... The metabolism of p-OHA to p-OHNor is well documented and dopamine-β hydroxylase present in noradrenergic neurons could easily ...
Benperidol
... is a strong dopamine receptor antagonist (D2 (Ki 0.027 nM) and D4 (Ki 0.066 nM)) with weaker serotonin receptor ... Li P, Snyder GL, Vanover KE (December 2016). "Dopamine Targeting Drugs for the Treatment of Schizophrenia: Past, Present and ...
Budipine
While its exact mechanism of action is not well characterized, it is believed to be an NMDA receptor antagonist, but also ... "Effects of amantadine and budipine on antidepressant drug-evoked changes in extracellular dopamine in the frontal cortex of ... Palmer GC (September 2001). "Neuroprotection by NMDA receptor antagonists in a variety of neuropathologies". Current Drug ... promoting the synthesis of dopamine. Because it provides additional benefits relative to existing treatments, it probably does ...
List of investigational anxiolytics
... orexin OX1 receptor antagonist [7] NBTX-001 (Xenon) - NMDA receptor antagonist [8] 7-Oxoprasterone (7-keto-DHEA; HBL-9001) - " ... serotonin-norepinephrine-dopamine releasing agent and 5-HT1 and 5-HT2 receptor agonist - specifically under development as an ... Agomelatine (AGO-178; Valdoxan) - melatonin MT1 and MT2 receptor agonist, 5-HT2C receptor antagonist[1] Riluzole sublingual ( ... orexin OX1 receptor antagonist [25] MP-20X - CB1 and 5-HT1A receptor modulator [26] SRX-246 - vasopressin V1A receptor ...
Threohydrobupropion
Nicotinic antagonists, Phenylethanolamines, Serotonin-norepinephrine-dopamine reuptake inhibitors, Substituted amphetamines, ... Moreover, threohydrobupropion has been reported to weakly inhibit the reuptake of norepinephrine, dopamine, and serotonin with ... Bupropion is a norepinephrine-dopamine reuptake inhibitor and nicotinic acetylcholine receptor negative allosteric modulator, ...
Pre-Bötzinger complex
These include norepinephrine, serotonin, acetylcholine, substance P, ATP, TRH, somatostatin, dopamine, endorphins, and ... most being selective agonists or antagonists to receptor subtypes on neurons in the vicinity. Since many of these neurons ...
SoRI-20041
... is an "antagonist-like" allosteric modulator of amphetamine-induced dopamine release (in contrast to the related ... Identification of "agonist" and "antagonist" allosteric modulators of amphetamine-induced dopamine release". The Journal of ... Conventional dopamine re-uptake inhibitors (such as cocaine or methylphenidate) would otherwise ineffectively target such a ... This increases the inhibition of re-uptake at synaptic dopamine concentrations without interfering in the flow of release of ...
Histamine H3 receptor
... silent antagonist) A-349,821 ABT-239 Betahistine (also weak H1 agonist) Burimamide (also weak H2 antagonist) Ciproxifan ... because of H3 receptor-modulation of dopamine and GABA in the basal ganglia), schizophrenia and ADHD (again because of dopamine ... histamine receptor antagonists H3-receptor antagonist Histamine H1-receptor Histamine H2-receptor Histamine H4-receptor GRCh38 ... Some examples are: (R)-α-methylhistamine Cipralisant (initially assessed as H3 antagonist, later found to be an agonist, shows ...
SDA
... omega-3 fatty acid Serotonin-dopamine antagonist, atypical antipsychotic Space domain awareness, the ability to detect, track, ...
Sigma-1 receptor
Links between σ1 receptors and G-proteins have been suggested such as σ1 receptor antagonists showing GTP-sensitive high- ... Attenuates Dopamine Toxicity and Potentiates Neurite Outgrowth in Various Cultured Cell Lines". Neurotoxicity Research. 34 (2 ... Brimson JM, Brown CA, Safrany ST (September 2011). "Antagonists show GTP-sensitive high-affinity binding to the sigma-1 ... putative antagonist, selective against 5-HT1A, 5-HT6, 5-HT7, α1A and α2 adrenergic, and NMDA receptors NE-100 Positive ...
Sympathoadrenal system
In these cases, curative agents such as adrenergic agonists and antagonists are used to modify epinephrine and norepinephrine ... dopamine-β-hydroxylase, and phenylethanolamine N-methyltransferase. The release of adrenocorticotropic hormone is usually ...
Huda Akil
In 1977, they discovered that the narcotic antagonist naloxone partially reverses analgesia produced by focal electrical ... dopamine, noradrenaline, and serotonin. Akil and colleagues used four different approaches to alter transmission in monoamine ... a narcotic antagonist". Science. 191 (4230): 961-962. Bibcode:1976Sci...191..961A. doi:10.1126/science.1251210. ISSN 0036-8075 ...
Doxepin
Muscarinic antagonists, Sedatives, Serotonin receptor antagonists, Serotonin-norepinephrine reuptake inhibitors, Sodium channel ... There is negligible influence on dopamine reuptake. The major metabolite of doxepin, nordoxepin (desmethyldoxepin), is ... In fact, doxepin has been said to be the most or one of the most potent H1 receptor antagonists available, with one study ... It is specifically an antagonist of the histamine H1 and H2 receptors, the serotonin 5-HT2A and 5-HT2C receptors, the α1- ...
Male Infertility Medication: Estrogen receptor blockers, Dopamine antagonists, Gonadotropins
Dopamine antagonists. Class Summary. These agents are ergot derivatives and dopamine receptor agonists. They act on ... Semisynthetic ergot alkaloid derivative with strong dopamine D2-receptor agonist and partial dopamine D1-receptor effects. ... Chua ME, Escusa KG, Luna S, Tapia LC, Dofitas B, Morales M. Revisiting oestrogen antagonists (clomiphene or tamoxifen) as ... postsynaptic dopamine receptors while causing no effect on other anterior pituitary functions. Mimic dopamine action of ...
Browsing by Subject "Dopamine Antagonists"
Obesity Medication: Gastrointestinal Agents, Other, CNS Stimulants, Anorexiants, Glucagonlike Peptide-1 Agonists,...
Antidepressants, dopamine reuptake inhibitors; opioid antagonists. Class Summary. These agents may cause a reduction in ... Bupropion: Increases dopamine activity in the brain, which appears to lead to a reduction in appetite and increase in energy ... Cannabinoid receptor antagonists and obesity. Curr Opin Investig Drugs. 2004 Apr. 5(4):389-94. [QxMD MEDLINE Link]. ... Combination may regulate activity in the dopamine reward system of the brain that helps control food cravings and overeating ...
Dopamine Antagonist Withdrawal Syndrome (DAAWS) | RxISK
This weeks features the equally grim horror of dopamine antagonist withdrawal syndrome (DAAWS). The dopamine antagonists ... Stopped a dopamine antagonist (antiemetic) cold turkey 9 months ago (I only had that Med for 3 months). Now I am still having ... My first brush with the fact that dopamine antagonists can cause withdrawal came when Carole came to see me in 1996. ... Im going through a similar experience after taking Domperidone (dopamine antagonist/antiemetic) for 2 yrs. It is absolutely ...
JCI Insight -
Striatal TRPV1 activation by acetaminophen ameliorates dopamine D2 receptor antagonist-induced orofacial...
Increased ROR of dyskinesia with the use of dopamine D2R antagonists and confounding effects of concomitant drugs on the drug- ... Striatal TRPV1 activation by acetaminophen ameliorates dopamine D2 receptor antagonist-induced orofacial dyskinesia. Koki ... that occurs due to long-term use of dopamine D2 receptor (D2R) antagonists, such as antipsychotics. Dyskinesia also occurs ... In these matched cohorts taking D2R antagonists, daily and cumulative doses, and the administration period of D2R antagonists, ...
Identification of Drugs Including a Dopamine Receptor Antagonist that Selectively Target Cancer Stem Cells - McMaster Experts
Effects of dopamine agonists and antagonists in variable reinforcing environments
BALDERRAMA-TRAPAGA, Jorge Arturo e APARICIO-NARANJO, Carlos Fernando. Effects of dopamine agonists and antagonists in variable ... The cumulative body of empirical evidence shows that dopamine agonists and antagonists (e.g., Methylphenidate and Haloperidol, ... Palavras-chave : Methylphenidate; Haloperidol; Choice; Motivation; Reinforcement; Rats; Laboratory research; Dopamine; Dopamine ... The anhedonia hypothesis maintains that pleasure for food-reward is determined by dopamine activity in the brain. ...
Tardive Dyskinesia: Overview, Pathophysiology, Etiology
... and extremities that occur in patients treated with long-term dopaminergic antagonist medications. Although they are associated ... Use of potent dopamine antagonists, prolonged exposure to dopamine antagonists, and prior occurrence of acute movement ... Some patients need a small dose of dopamine antagonists on a long-term basis. They may require hospitalization if the dopamine ... long-term blockade of dopamine D2 receptors in the basal ganglia by dopamine D2 antagonists (eg, neuroleptics) may produce TD ...
IMSEAR at SEARO: Antagonism of bromocriptine-induced cage climbing behaviour in mice by the selective D-2 dopamine receptor...
... an antagonist of both D-1 and D-2 dopamine receptors, metoclopramide and molindone, the selective D-2 dopamine receptor ... Antagonism of bromocriptine-induced cage climbing behaviour in mice by the selective D-2 dopamine receptor antagonists, ... Antagonism of bromocriptine-induced cage climbing behaviour in mice by the selective D-2 dopamine receptor antagonists, ... antagonists, effectively antagonised bromocriptine-induced climbing behaviour. The results indicate that bromocriptine most ...
Bio-Domperidone - Uses, Side Effects, Interactions - MedBroadcast.com
Effects of the putative dopamine autoreceptor antagonists (+)-AJ 76 and (+)-UH 232 on the discriminative stimulus properties of...
Dive into the research topics of Effects of the putative dopamine autoreceptor antagonists (+)-AJ 76 and (+)-UH 232 on the ... Callahan, P. M., Piercey, M. F., & Cunningham, K. A. (1992). Effects of the putative dopamine autoreceptor antagonists (+)-AJ ... Callahan, PM, Piercey, MF & Cunningham, KA 1992, Effects of the putative dopamine autoreceptor antagonists (+)-AJ 76 and (+)- ... N2 - Recent evidence suggests that the putative dopamine (DA) autoreceptor antagonists, (+)-AJ 76 and (+)-UH 232, share some ...
Parkinson's disease: A new dopamine D3 receptor antagonist mesdopetam!
... to obtain a new dopamine D3 receptor antagonist mesdopetam! ... A new dopamine D3 receptor antagonist mesdopetam! Parkinsons ... Parkinsons disease: A new dopamine D3 receptor antagonist mesdopetam!. 1 year ago ... Mesdopetam (IRL790) is a new type of dopamine D3 receptor antagonist, developed for PD patients to prevent and treat LID, and ... Parkinsons disease: A new dopamine D3 receptor antagonist mesdopetam!. Parkinsons disease (PD) new drug! Ipsen and IRLAB ...
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Plus it
... in that these phenomena are blocked by NMDA antagonists, protein synthesis inhibitors, and dopamine D1 antagonists. The same ... Modulation of cocaine effects by AMPA, opiate, or dopamine D1 receptor antagonists. FR and FH animals previously treated with ... In the present study, neither the D1 antagonist SCH23390 nor the D2/D3 antagonist sulpiride reliably suppressed the expression ... Two more FR and FH (n = 7-9) groups were constituted from naive animals to test the effects of the D2/D3 receptor antagonist ...
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... dopamine agonists, bisphosphonates, estrogen receptor antagonists, antithyroid agents, and metabolic agents. ... Antiparkinson Agents, Dopamine Agonists. Class Summary. Dopamine receptor agonists have been used as adjuncts to octreotide for ... Estrogen Receptor Antagonists. Class Summary. Estrogen receptor antagonist therapy represents a newer approach to the treatment ... Bromocriptine is a semisynthetic ergot alkaloid derivative that is a strong dopamine D2-receptor agonist and a partial dopamine ...
Modulation of lipopolysaccharide-induced tumor necrosis factor-α and nitric oxide production by dopamine receptor agonists and...
Sulpiride, an antagonist of dopamine D2 receptors, decreased the LPS-induced TNF-α plasma levels in a dose-dependent manner and ... SCH-23390, an antagonist of dopamine D1 receptors did not alter LPS-induced TNF-α production, but inhibited LPS-induced NO ... Sulpiride, an antagonist of dopamine D2 receptors, decreased the LPS-induced TNF-α plasma levels in a dose-dependent manner and ... SCH-23390, an antagonist of dopamine D1 receptors did not alter LPS-induced TNF-α production, but inhibited LPS-induced NO ...
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Olanzapine, 5-HT, dopamine, histamine and muscarinic antagonist (ab120736) Description:. Non-selective 5-HT, dopamine, ... Agonists, activators, antagonists and inhibitors. Cell lines and Lysates. Multiplex miRNA assays. Multiplex Assays. By research ... Spiperone hydrochloride, 5-HT and D2-like receptor antagonist (ab120549) Specific References (2) ...
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... to their use in the treatment and/or prevention of conditions which require modulation of dopamine receptor and to ... The method according to claim 11 wherein the dopamine receptor is a dopamine D3 and/or dopamine D2 receptor. ... 9. The use according to claim 8 wherein the dopamine receptor is dopamine D3 and/or dopamine D2 receptor. ... Cyclohexylamides as dopamine d3 , d2 and 5ht1a antagonists NZ544999A (en) 2009-07-31. (Thio) carbamoyl-cyclohexane derivatives ...
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7.3 Dopamine Antagonists. Because ropinirole is a dopamine agonist, it is possible that dopamine antagonists such as ... 7.3 Dopamine Antagonists 8 USE IN SPECIFIC POPULATIONS 8.1 Pregnancy 8.2 Lactation 8.4 Pediatric Use 8.5 Geriatric Use 8.6 ... Dopamine antagonists (e.g., neuroleptics, metoclopramide): May reduce efficacy of ropinirole. ( 7.3) ... Ropinirole tablets are dopamine agonist medicines. Dopamine agonist medicines, including ropinirole tablets can cause ...
ReceptorsAgonistAgonists and antagonistsMetoclopramideCalled dopamine receptorDopaminergic antagonistNMDAReceptor agonistsAction of dopamineMuscarinicNeurolepticsRelease of dopamineIncrease in dopaminePartialAntipsychoticsSchizophreniaAntipsychotic agentsSelectivePrecursorStriatalNorepinephrineInhibitor1996NeurotransmitterModulationSulpiridePotentTransporterDomperidoneInhibitionRatsHypothesisProlactinSynapticRisperidoneNeuronsEffectsCocaineDrugsAcuteNucleus accumbensChemicalTransportersClinicalWithdrawalVitroBlockadeMicePleasurableHydrochlorideBrain
Receptors27
- They act on postsynaptic dopamine receptors while causing no effect on other anterior pituitary functions. (medscape.com)
- Pretreatment with haloperidol, an antagonist of both D-1 and D-2 dopamine receptors, metoclopramide and molindone, the selective D-2 dopamine receptor antagonists, effectively antagonised bromocriptine-induced climbing behaviour. (who.int)
- The results indicate that bromocriptine most probably induces climbing behaviour in mice by stimulating the postsynaptic striatal D-2 dopamine receptors. (who.int)
- The effects of various agonists and antagonists of dopamine D 1 and D 2 receptors on lipopolysaccharide (LPS)-induced tumor necrosis factor-α (TNF-α) and nitric oxide (NO) production was investigated in mice. (elsevier.com)
- Pretreatment of animals with bromocryptine or quinpirole, agonists of dopamine D 2 receptors caused a blunting of both the TNF-α and MO responses to LPS injected intraperitoneally. (elsevier.com)
- Sulpiride, an antagonist of dopamine D 2 receptors, decreased the LPS-induced TNF-α plasma levels in a dose-dependent manner and inhibited the LPS-induced NO production by peritoneal macrophages. (elsevier.com)
- SCH-23390, an antagonist of dopamine D 1 receptors did not alter LPS-induced TNF-α production, but inhibited LPS-induced NO production. (elsevier.com)
- These results indicate that while the D 2 subtype of dopamine receptors is involved in the modulation of both LPS-induced TNF-α and NO production, dopamine D 1 receptors only regulate the production of NO. Since several drugs possess effect on dopamine D 2 receptors, the present observations may be of clinical relevance. (elsevier.com)
- All current FDA-approved medications for the treatment of schizophrenia antagonize dopamine type 2 receptors-but that is where their similarity ends. (psychiatrictimes.com)
- Additionally, as we see with the DR2, a gene product can be further processed by post-transcriptional editing (introns and exons) to provide a range of sub-sub-receptors with different binding affinities and circuitry locations (for example, the differing dopamine receptor 2 long [DR2L], which is postsynaptic, versus dopamine receptor 2 short [DR2S], which is presynaptic). (psychiatrictimes.com)
- This new study, led by neuroscientist Paul Stokes , tested dopamine levels by using a type of PET brain scan where participants are injected with a radioactive tracer that binds to free dopamine receptors. (mindhacks.com)
- Higher dopamine levels will mean that there are less free dopamine receptors and, therefore, lower tracer levels. (mindhacks.com)
- For about 15 years now, the PCP/NMDA model has been an alternative to the straight dopamine theory of schizophrenia (reviewed by Javitt 2008 http://www.ncbi.nlm.nih.gov/pubmed/18497092 ) - "PCP) and ketamine induce psychotic symptoms and neurocognitive disturbances similar to those of schizophrenia by blocking neurotransmission at N-methyl-D-aspartate (NMDA)-type glutamate receptors. (mindhacks.com)
- For antiemetics which don't affect dopamine receptors, see the antiemetics chapter. (emcrit.org)
- The action of dopamine occurs via dopamine receptors, D1-5. (news-medical.net)
- D1 receptors and D4 receptors are responsible for the cognitive-enhancing effects of dopamine. (news-medical.net)
- Solvay and Lundbeck are developing bifeprunox (DU 127090), a partial dopamine D 2 receptor antagonist that also has agonist effects at serotonin 1a receptors. (pmlive.com)
- Classic neuroleptic drugs, antagonists at dopamine D2 receptors, are generally the mainstay of tic treatment, but side effects often limit their usefulness. (hopkinsmedicine.org)
- Risperidone is a benzisoxazol derivative that at low doses acts on 5-HT2 receptors, while at higher doses it is a potent D2 antagonist. (hopkinsmedicine.org)
- Unlike other antipsychotics it demonstrates a mix of agonist and antagonistic effects at dopamine receptors, depending on testing conditions. (hopkinsmedicine.org)
- Furthermore, consistent with other partial agonists it shows agonistic effects most clearly when there is little dopamine with which to compete or when receptors are maximally responsive. (hopkinsmedicine.org)
- Fifteen established genetic variations (polymorphisms), including those from of metabolizing enzymes (CYP2D6), dopamine and serotonin transporters (DAT,5-HTT), dopamine receptors (D2, D3, D4) and serotonin receptors (5HT2A and 5HT2C), are being investigated in children with TS using DNA obtained from buccal swabs. (hopkinsmedicine.org)
- The most important transmitters and their receptors include serotonin and the 5-HT3 receptor, dopamine, dopamine receptor and substance P, and the neurokinin 1 (NK1) receptor. (medscape.com)
- Drugs that bind to but do not activate DOPAMINE RECEPTORS , thereby blocking the actions of dopamine or exogenous agonists. (bvsalud.org)
- 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. (bvsalud.org)
- Potential link between genetic polymorphisms of catechol-O-methyltransferase and dopamine receptors and treatment efficacy of risperidone on schizophrenia. (cdc.gov)
- Lack of association between polymorphisms of dopamine receptors, type D2, and bipolar affective illness in a Polish population. (cdc.gov)
Agonist3
- Semisynthetic ergot alkaloid derivative with strong dopamine D2-receptor agonist and partial dopamine D1-receptor effects. (medscape.com)
- The last post outlined the horrors of dopamine agonist withdrawal syndrome (DAWS) . (rxisk.org)
- Previous evidence indicates the utility of low-dose partial dopamine agonist (PDAs) add-ons to mitigate antipsychotic-induced metabolic adverse effects or hyperprolactinemia. (lww.com)
Agonists and antagonists1
- The cumulative body of empirical evidence shows that dopamine agonists and antagonists (e.g. (bvsalud.org)
Metoclopramide2
Called dopamine receptor1
- Amisulpride is in a class of medications called dopamine receptor antagonists. (medlineplus.gov)
Dopaminergic antagonist1
- Tardive dyskinesias (TDs) are involuntary movements of the tongue, lips, face, trunk, and extremities that occur in patients treated with long-term dopaminergic antagonist medications. (medscape.com)
NMDA2
- Auvelity is the first FDA-approved NMDA antagonist for depression that can be taken orally as opposed to intravenously (through an IV), intramuscularly (injected into the muscle), or intranasally (sprayed into the nose). (headinghealth.com)
- While ketamine, Spravato, and Auvelity are all NMDA antagonists, Auvelity is unique in ways that makes them difficult to compare. (headinghealth.com)
Receptor agonists1
- These agents are ergot derivatives and dopamine receptor agonists. (medscape.com)
Action of dopamine1
- It works by blocking the action of dopamine, a natural substance that may cause nausea and vomiting. (medlineplus.gov)
Muscarinic1
- Scopolamine, a muscarinic receptor antagonist is widely to induce cognitive / memory impairment in clinical research (human volunteers) and in experimental animals. (neurofit.com)
Neuroleptics2
- The acute movement disorders that occur as manifestations of effects of neuroleptics and other dopamine antagonists include akathisia, acute dystonia, and other hyperkinetic dyskinesias. (medscape.com)
- 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)
Release of dopamine1
- CBD, a nonpsychoactive cannabis extract, was discovered to stimulate the release of dopamine in mice. (dailysandiegonews.com)
Increase in dopamine2
- But if it is the case that cannabis does not cause a significant increase in dopamine levels, this will mean our ideas about cannabis and psychosis will need a rethink. (mindhacks.com)
- This is credited to an increase in dopamine. (news-medical.net)
Partial3
- It is considered a D2 receptor partial antagonist, exerting relatively weak agonism as compared to natural endogenous dopamine. (hopkinsmedicine.org)
- The dilemma of polypharmacy in psychosis: is it worth combining partial and full dopamine modulation? (lww.com)
- is it worth combining partial and full dopamine modulation? (lww.com)
Antipsychotics2
- Thus, dopamine antagonists (e.g. many antipsychotics) result in elevated prolactin levels. (radiopaedia.org)
- Association study between antipsychotics- induced restless legs syndrome and polymorphisms of dopamine D1, D2, D3, and D4 receptor genes in schizophrenia. (cdc.gov)
Schizophrenia2
- Despite some dissenting voices, disruption to the mesolimbic dopamine pathway is widely thought to be the key problem in the development of delusions, hallucinations and the other psychotic symptoms commonly diagnosed as schizophrenia. (mindhacks.com)
- Some of the antipsychotic medications used in conditions like schizophrenia act as dopamine antagonists. (news-medical.net)
Antipsychotic agents1
- Blonanserin is a dual-action serotonin 2 and dopamine D 2 receptor antagonist that is structurally unrelated to existing antipsychotic agents on the market and is expected to be effective in the treatment of both positive and negative symptoms. (pmlive.com)
Selective1
- this was confirmed by intra-NAc administration of Ro 15-4513 and furosemide, a selective α6-GABA A antagonist. (nih.gov)
Precursor2
Striatal2
- Increased striatal dopamine synthesis capacity in gambling addiction. (mpg.de)
- Moreoever, a D2 antagonist caused an increase in evoked spike firing of striatal neurons recorded intracellularly in vivo (West and Grace 2002). (scholarpedia.org)
Norepinephrine1
- The standard array of antidepressants works primarily on one or more of three of the brain's chemical messengers: serotonin, norepinephrine, and dopamine. (headinghealth.com)
Inhibitor1
- Dopamine is the main neuroendocrine inhibitor of the secretion of prolactin from the anterior pituitary gland. (news-medical.net)
19961
- My first brush with the fact that dopamine antagonists can cause withdrawal came when Carole came to see me in 1996. (rxisk.org)
Neurotransmitter3
- Traditionally, this was explained by the drug increasing dopamine levels in the brain but a new study shortly to be published in NeuroImage suggests that the active ingredient in cannabis doesn't effect this important neurotransmitter. (mindhacks.com)
- Dopamine is a neurotransmitter released by the brain that plays a number of roles in humans and other animals. (news-medical.net)
- Dopamine is a neurotransmitter and influences our perception of satisfaction and pleasure. (dailysandiegonews.com)
Modulation2
- Abnormal modulation of reward versus punishment learning by a dopamine D2-receptor antagonist in pathological gamblers. (mpg.de)
- This article will briefly cover: basic dopamine neuron physiology and electrophysiology of dopamine modulation of cortex. (scholarpedia.org)
Sulpiride1
- The D 1 antagonist SCH23390 [ R (+)-7-chloro-8-hydroxy-3-methyl-1-phenyl-2,3,4,5-tetrahydro-1 H -3-benzazepine hydrochloride] (15-30 μg/kg) and D 2 antagonist sulpiride (25-125 mg/kg) reduced activity nonspecifically. (jneurosci.org)
Potent1
- Use of potent dopamine antagonists, prolonged exposure to dopamine antagonists, and prior occurrence of acute movement disorders on exposure to dopamine antagonists are also associated with an increased risk for the occurrence of acute movement adverse effects. (medscape.com)
Transporter3
- Dysfunction of the dopamine transporter has been hypothesized to play a role in the development of TD. (medscape.com)
- [ 4 ] Thus, further research is needed to investigate the role of the dopamine transporter in the development and maintenance of TD. (medscape.com)
- Cocaine is a dopamine transporter blocker that competitively inhibits dopamine uptake to increase the presence of dopamine. (news-medical.net)
Domperidone1
- Domperidone belongs to the group of medications called dopamine antagonists . (medbroadcast.com)
Inhibition3
- Mimic dopamine action of inhibition of prolactin release. (medscape.com)
- Pirot et al (1992) showed that the GABA antagonist bicuculline blocked the iontophoretic DA and VTA-mediated inhibition of spontaneous firing in 57% and 51% of cells respectively. (scholarpedia.org)
- Moreover a D2 antagonist reduced the DA-mediated and VTA-stimulation induced inhibition of spontaneous firing in PFC in 89% and 54% of cells respectively. (scholarpedia.org)
Rats2
- DARPP-32, a dopamine- and adenosine 3',5'-monophosphate (cAMP)-regulated phosphoprotein (32 kilodaltons in size), is an obligate intermediate in progesterone (P)-facilitated sexual receptivity in female rats and mice. (cdc.gov)
- WIN blocked doPamine from being released by rats. (dailysandiegonews.com)
Hypothesis4
- The anhedonia hypothesis maintains that pleasure for food-reward is determined by dopamine activity in the brain. (bvsalud.org)
- the dopamine hypersensitivity hypothesis and the serotonin-dopamine antagonist hypothesis. (who.int)
- The neuroleptic-induced TD with those who did serotonin-dopamine antagonist hypothesis not develop it under comparatively similar maintains that drugs which have a high conditions. (who.int)
- The dopamine hypothesis of schizo-phrenia pathogenesis argues that the behavioural changes seen in patients are caused by excessive dopamine activity in certain regions of the brain, primarily the mesolimbic and mesocortical pathways. (pmlive.com)
Prolactin4
- These cells can produce prolactin in absence of dopamine. (news-medical.net)
- Dopamine is occasionally called prolactin-inhibiting factor (PIF), prolactin-inhibiting hormone(PIH), or prolactostatin. (news-medical.net)
- The exception is prolactin which, except during pregnancy when it too is stimulated by a releasing hormone, is tonically inhibited by prolactin inhibitory hormone (PIH) which is actually dopamine. (radiopaedia.org)
- Conversely, prolactin secreting adenomas (prolactinomas) can be treated medically with dopamine agonists (e.g. bromocriptine and cabergoline). (radiopaedia.org)
Synaptic2
- Nestler, 2001 ), psychostimulant-induced increases in synaptic dopamine may facilitate the formation of particularly strong conditioned associations between the reinforcer and the environment. (jneurosci.org)
- Amphetamine increases the concentration of dopamine in the synaptic gap, but by a different mechanism. (news-medical.net)
Risperidone1
- Dopamine D3 receptor Ser9Gly polymorphism and risperidone response. (cdc.gov)
Neurons3
- Dopamine is produced in the dopaminergic neurons in the ventral tegmental area (VTA) of the midbrain, the substantia nigra pars compacta, and the arcuate nucleus of the hypothalamus. (news-medical.net)
- Dopamine produced by neurons in the arcuate nucleus of the hypothalamus is released in the hypothalamo-hypophysial blood vessels of the median eminence, which supply the pituitary gland. (news-medical.net)
- Dopamine (DA) neurons show two predominant patterns of firing activity termed tonic and phasic (Grace 1991, 2000). (scholarpedia.org)
Effects5
- Acute effects of dopamine antagonists also include parkinsonian syndromes manifested by bradykinesia, rigidity, and pill rolling tremor. (medscape.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)
- The researchers found no difference in dopamine levels between the THC and the sugar pill, even though the participants clearly reported the effects of the drug. (mindhacks.com)
- 5-HT 2A receptor antagonists block acute psychedelic effects, but whether they also block therapeutic effects requires further investigation. (aboriginalhealth.net)
- Effects of polychlorinated biphenyls on dopamine release from PC12 cells. (cdc.gov)
Cocaine1
- Cocaine and amphetamines inhibit the re-uptake of dopamine. (news-medical.net)
Drugs8
- The dopamine antagonists include the antipsychotic, anti-nausea, anti-itch and other groups of drugs. (rxisk.org)
- In itself, this is partly based on another assumption - the virtual mantra of recreational drug research that 'all drugs of abuse increase dopamine levels in the reward system' of which the striatum is a part. (mindhacks.com)
- My suspicion is that drugs which humans find "pleasurable" probably do involve dopamine whereas ones which people find "interesting" don't. (mindhacks.com)
- This means food, sex, and several drugs of abuse are also stimulants of dopamine release in the brain, particularly in areas such as the nucleus accumbens and prefrontal cortex. (news-medical.net)
- These drugs are primarily dopamine receptor antagonists, effective in the treatment of positive symptoms. (pmlive.com)
- These drugs are generally dual-action serotonin and dopamine receptor antagonists and are more effective than the older typicals in addressing the positive symptoms as well as less likely to result in extrapyramidal adverse events. (pmlive.com)
- Concomitant dopamine-depleting agents (eg, reserpine, tetrabenazine) or other drugs known to deplete monoamine stores: not recommended. (empr.com)
- A dopamine antagonist wait and see and brandname drugs going to work. (mychicagoathlete.com)
Acute2
- The acute movement disorders resulting from exposure to dopamine antagonists are commonly termed extrapyramidal syndromes (EPSs). (medscape.com)
- The occurrence of acute movement disorders on exposure to dopamine antagonists is increased in female patients and older patients. (medscape.com)
Nucleus accumbens1
- The dopamine D 3 receptor (D 3 R), in the nucleus accumbens (NAc), plays an important role in alcohol reward mechanisms. (nih.gov)
Chemical3
- It acts by blocking the actions of certain chemical messengers (dopamine) in the brain that controls the movement of stomach muscles. (netmeds.com)
- Dopamine is the chemical that mediates pleasure in the brain. (news-medical.net)
- CBD is a chemical that has many benefits that include the capacity to increase the levels of dopamine in the brain. (dailysandiegonews.com)
Transporters1
- Amphetamines are similar in structure to dopamine, and so can enter the presynaptic neuron via its dopamine transporters. (news-medical.net)
Clinical2
- Dopamine antagonists have been used for several other clinical purposes including as ANTIEMETICS , in the treatment of Tourette syndrome, and for hiccup. (bvsalud.org)
- Association of dopamine-related genetic loci to dopamine D3 receptor antagonist ABT-925 clinical response. (cdc.gov)
Withdrawal2
- This week's features the equally grim horror of dopamine antagonist withdrawal syndrome (DAAWS). (rxisk.org)
- Withdrawal dyskinesias may also occur as treatment with dopamine antagonists is decreased or withdrawn. (medscape.com)
Vitro1
- In vitro affinity of piribedil for dopamine D3 receptor subtypes, an autoradiographic study. (axonmedchem.com)
Blockade2
- A number of studies have investigated the relationship between the time course of central nervous system dopamine and serotonin receptor blockade and plasma drug concentrations after the discontinuation of QTP treatment, and shown that the disappearance of QTP from plasma is much more rapid than the decrease in serotonin receptor occupancy [136,143, 145] . (researchgate.net)
- Dopamine receptor blockade is associated with NEUROLEPTIC MALIGNANT SYNDROME . (bvsalud.org)
Mice1
- Cannabinoid antagonists may enhance the duration of the pattern of the scallop in mice. (dailysandiegonews.com)
Pleasurable1
- By increasing presence of dopamine both these lead to increased pleasurable feelings and addiction. (news-medical.net)
Hydrochloride1
- Conditioned activity was selectively reduced by the opiate antagonist naltrexone (10-20 mg/kg) and by the noncompetitive AMPA receptor antagonist GYKI 52466 [1-(4-aminophenyl)-4-methyl-7,8-methylenedioxy-5 H -2,3-benzodiazepine hydrochloride] (5-10 mg/kg). (jneurosci.org)
Brain8
- This has led to the assumption that the small increased risk of psychosis reliably associated with cannabis use is due to the drug increasing dopamine levels in a deep brain structure called the striatum . (mindhacks.com)
- When there is a deficiency in dopamine in the brain, movements may become delayed and uncoordinated. (news-medical.net)
- On the flip side, if there is an excess of dopamine, the brain causes the body to make unnecessary movements, such as repetitive tics. (news-medical.net)
- Levels of dopamine in the brain, especially the prefrontal cortex, help in improved working memory. (news-medical.net)
- Vision helps a dopamine response in the brain and this in turn helps one to focus and direct their attention. (news-medical.net)
- Dopamine in the frontal lobes of the brain controls the flow of information from other areas of the brain. (news-medical.net)
- An update on diet, dopamine and the brain people. (mpg.de)
- This is the first research to demonstrate that synthetic cannabinoids could interfere with brain dopamine release. (dailysandiegonews.com)