Receptors, Dopamine: Cell-surface proteins that bind dopamine with high affinity and trigger intracellular changes influencing the behavior of cells.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.Receptors, Dopamine D2: 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.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.Receptors, Dopamine D1: A subfamily of G-PROTEIN-COUPLED RECEPTORS that bind the neurotransmitter DOPAMINE and modulate its effects. D1-class receptor genes lack INTRONS, and the receptors stimulate ADENYLYL CYCLASES.Dopamine Agonists: Drugs that bind to and activate dopamine receptors.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.Receptors, Dopamine D3: A subtype of dopamine D2 receptors that are highly expressed in the LIMBIC SYSTEM of the brain.Receptor, Serotonin, 5-HT2A: A serotonin receptor subtype found widely distributed in peripheral tissues where it mediates the contractile responses of variety of tissues that contain SMOOTH MUSCLE. Selective 5-HT2A receptor antagonists include KETANSERIN. The 5-HT2A subtype is also located in BASAL GANGLIA and CEREBRAL CORTEX of the BRAIN where it mediates the effects of HALLUCINOGENS such as LSD.Receptors, Dopamine D5: A subtype of dopamine D1 receptors that has higher affinity for DOPAMINE and differentially couples to GTP-BINDING PROTEINS.Receptor, Serotonin, 5-HT1A: 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.Quinpirole: A dopamine D2/D3 receptor agonist.Dopamine Agents: Any drugs that are used for their effects on dopamine receptors, on the life cycle of dopamine, or on the survival of dopaminergic neurons.Spiperone: A spiro butyrophenone analog similar to HALOPERIDOL and other related compounds. It has been recommended in the treatment of SCHIZOPHRENIA.Benzazepines: Compounds with BENZENE fused to AZEPINES.Receptors, Serotonin: 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.Dopamine Plasma Membrane Transport Proteins: 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.Receptor, Serotonin, 5-HT1B: 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.Apomorphine: 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.Receptor, Serotonin, 5-HT2C: A serotonin receptor subtype found primarily in the CENTRAL NERVOUS SYSTEM and the CHOROID PLEXUS. This receptor subtype is believed to mediate the anorectic action of SEROTONIN, while selective antagonists of the 5-HT2C receptor appear to induce ANXIETY. Several isoforms of this receptor subtype exist, due to adenine deaminase editing of the receptor mRNA.Serotonin Antagonists: Drugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or SEROTONIN RECEPTOR AGONISTS.Receptors, Serotonin, 5-HT1: A subclass of G-protein coupled SEROTONIN receptors that couple preferentially to GI-GO G-PROTEINS resulting in decreased intracellular CYCLIC AMP levels.Receptors, Dopamine D4: A subtype of dopamine D2 receptors that has high affinity for the antipsychotic CLOZAPINE.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.Serotonin Plasma Membrane Transport Proteins: 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.Salicylamides: Amides of salicylic acid.2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine: A selective D1 dopamine receptor agonist used primarily as a research tool.Receptors, Serotonin, 5-HT3: A subclass of serotonin receptors that form cation channels and mediate signal transduction by depolarizing the cell membrane. The cation channels are formed from 5 receptor subunits. When stimulated the receptors allow the selective passage of SODIUM; POTASSIUM; and CALCIUM.Sulpiride: A dopamine D2-receptor antagonist. It has been used therapeutically as an antidepressant, antipsychotic, and as a digestive aid. (From Merck Index, 11th ed)Serotonin Uptake Inhibitors: Compounds that specifically inhibit the reuptake of serotonin in the brain.Ergolines: A series of structurally-related alkaloids that contain the ergoline backbone structure.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)Serotonin Receptor Agonists: 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.Serotonin 5-HT2 Receptor Antagonists: Drugs that bind to but do not activate SEROTONIN 5-HT2 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN 5-HT2 RECEPTOR AGONISTS. Included under this heading are antagonists for one or more specific 5-HT2 receptor subtypes.Dopamine Uptake Inhibitors: 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.Raclopride: A substituted benzamide that has antipsychotic properties. It is a dopamine D2 receptor (see RECEPTORS, DOPAMINE D2) antagonist.Serotonin Agents: Drugs used for their effects on serotonergic systems. Among these are drugs that affect serotonin receptors, the life cycle of serotonin, and the survival of serotonergic neurons.Flupenthixol: A thioxanthene neuroleptic that, unlike CHLORPROMAZINE, is claimed to have CNS-activating properties. It is used in the treatment of psychoses although not in excited or manic patients. (From Martindale, The Extra Pharmacopoeia, 30th ed, p595)Butaclamol: A benzocycloheptapyridoisoquinolinol that has been used as an antipsychotic, especially in schizophrenia.Serotonin 5-HT2 Receptor Agonists: Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT2 RECEPTORS. Included under this heading are agonists for one or more of the specific 5-HT2 receptor subtypes.Serotonin 5-HT1 Receptor Agonists: 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.Neostriatum: The phylogenetically newer part of the CORPUS STRIATUM consisting of the CAUDATE NUCLEUS and PUTAMEN. It is often called simply the striatum.Receptors, Serotonin, 5-HT2: A subclass of G-protein coupled SEROTONIN receptors that couple preferentially to the GQ-G11 G-PROTEINS resulting in increased intracellular levels of INOSITOL PHOSPHATES and free CALCIUM.Receptor, Serotonin, 5-HT2B: 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.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.Serotonin 5-HT1 Receptor Antagonists: 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.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.Rats, Sprague-Dawley: 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.Behavior, Animal: The observable response an animal makes to any situation.Dopamine beta-HydroxylaseDomperidone: A specific blocker of dopamine receptors. It speeds gastrointestinal peristalsis, causes prolactin release, and is used as antiemetic and tool in the study of dopaminergic mechanisms.Bromocriptine: A semisynthetic ergotamine alkaloid that is a dopamine D2 agonist. It suppresses prolactin secretion.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.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.MSH Release-Inhibiting Hormone: A hypothalamic tripeptide, enzymatic degradation product of OXYTOCIN, that inhibits the release of MELANOCYTE-STIMULATING HORMONES.Serotonin Syndrome: An adverse drug interaction characterized by altered mental status, autonomic dysfunction, and neuromuscular abnormalities. It is most frequently caused by use of both serotonin reuptake inhibitors and monoamine oxidase inhibitors, leading to excess serotonin availability in the CNS at the serotonin 1A receptor.Caudate Nucleus: Elongated gray mass of the neostriatum located adjacent to the lateral ventricle of the brain.Oxidopamine: A neurotransmitter analogue that depletes noradrenergic stores in nerve endings and induces a reduction of dopamine levels in the brain. Its mechanism of action is related to the production of cytolytic free-radicals.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.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.Motor Activity: The physical activity of a human or an animal as a behavioral phenomenon.Neurons: 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.Dose-Response Relationship, Drug: The relationship between the dose of an administered drug and the response of the organism to the drug.Receptor, Serotonin, 5-HT1D: A serotonin receptor subtype that is localized to the CAUDATE NUCLEUS; PUTAMEN; the NUCLEUS ACCUMBENS; the HIPPOCAMPUS, and the RAPHE NUCLEI. 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-HT1B RECEPTOR, but is expressed at low levels. It is particularly sensitive to the agonist SUMATRIPTAN and may be involved in mediating the drug's antimigrane effect.Homovanillic AcidPergolide: A long-acting dopamine agonist which has been used to treat PARKINSON DISEASE and HYPERPROLACTINEMIA but withdrawn from some markets due to potential for HEART VALVE DISEASES.Tryptophan Hydroxylase: An enzyme that catalyzes the hydroxylation of TRYPTOPHAN to 5-HYDROXYTRYPTOPHAN in the presence of NADPH and molecular oxygen. It is important in the biosynthesis of SEROTONIN.Ketanserin: A selective serotonin receptor antagonist with weak adrenergic receptor blocking properties. The drug is effective in lowering blood pressure in essential hypertension. It also inhibits platelet aggregation. It is well tolerated and is particularly effective in older patients.8-Hydroxy-2-(di-n-propylamino)tetralin: A serotonin 1A-receptor agonist that is used experimentally to test the effects of serotonin.Radioligand Assay: Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).Substantia Nigra: 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.Serotonin 5-HT3 Receptor Antagonists: Drugs that bind to but do not activate SEROTONIN 5-HT3 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN 5-HT3 RECEPTOR AGONISTS.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.Hydroxyindoleacetic AcidCatalepsy: 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.Microdialysis: 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.Dyskinesia, Drug-Induced: Abnormal movements, including HYPERKINESIS; HYPOKINESIA; TREMOR; and DYSTONIA, associated with the use of certain medications or drugs. Muscles of the face, trunk, neck, and extremities are most commonly affected. Tardive dyskinesia refers to abnormal hyperkinetic movements of the muscles of the face, tongue, and neck associated with the use of neuroleptic agents (see ANTIPSYCHOTIC AGENTS). (Adams et al., Principles of Neurology, 6th ed, p1199)Putamen: The largest and most lateral of the BASAL GANGLIA lying between the lateral medullary lamina of the GLOBUS PALLIDUS and the EXTERNAL CAPSULE. It is part of the neostriatum and forms part of the LENTIFORM NUCLEUS along with the GLOBUS PALLIDUS.Fenoldopam: A dopamine D1 receptor agonist that is used as an antihypertensive agent. It lowers blood pressure through arteriolar vasodilation.Stereotyped Behavior: Relatively invariant mode of behavior elicited or determined by a particular situation; may be verbal, postural, or expressive.Receptors, Serotonin, 5-HT4: A subtype of G-protein-coupled SEROTONIN receptors that preferentially couple to GS STIMULATORY G-PROTEINS resulting in increased intracellular CYCLIC AMP. Several isoforms of the receptor exist due to ALTERNATIVE SPLICING of its mRNA.Tetrahydronaphthalenes: Partially saturated 1,2,3,4-tetrahydronaphthalene compounds.Tyrosine 3-Monooxygenase: An enzyme that catalyzes the conversion of L-tyrosine, tetrahydrobiopterin, and oxygen to 3,4-dihydroxy-L-phenylalanine, dihydrobiopterin, and water. EC 1.14.16.2.Dopaminergic Neurons: Neurons whose primary neurotransmitter is DOPAMINE.Hydroxydopamines: Dopamines with a hydroxy group substituted in one or more positions.PyrrolidinesBrain Chemistry: 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.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.Biogenic Monoamines: Biogenic amines having only one amine moiety. Included in this group are all natural monoamines formed by the enzymatic decarboxylation of natural amino acids.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.Fluoxetine: 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.HT29 Cells: Human colonic ADENOCARCINOMA cells that are able to express differentiation features characteristic of mature intestinal cells such as the GOBLET CELLS.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.PiperazinesAntiparkinson Agents: Agents used in the treatment of Parkinson's disease. The most commonly used drugs act on the dopaminergic system in the striatum and basal ganglia or are centrally acting muscarinic antagonists.Methamphetamine: A central nervous system stimulant and sympathomimetic with actions and uses similar to DEXTROAMPHETAMINE. The smokable form is a drug of abuse and is referred to as crank, crystal, crystal meth, ice, and speed.Raphe Nuclei: 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.5-Hydroxytryptophan: The immediate precursor in the biosynthesis of SEROTONIN from tryptophan. It is used as an antiepileptic and antidepressant.Yawning: An involuntary deep INHALATION with the MOUTH open, often accompanied by the act of stretching.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.Methysergide: An ergot derivative that is a congener of LYSERGIC ACID DIETHYLAMIDE. It antagonizes the effects of serotonin in blood vessels and gastrointestinal smooth muscle, but has few of the properties of other ergot alkaloids. Methysergide is used prophylactically in migraine and other vascular headaches and to antagonize serotonin in the carcinoid syndrome.Basal Ganglia: Large subcortical nuclear masses derived from the telencephalon and located in the basal regions of the cerebral hemispheres.alpha-Methyltyrosine: An inhibitor of the enzyme TYROSINE 3-MONOOXYGENASE, and consequently of the synthesis of catecholamines. It is used to control the symptoms of excessive sympathetic stimulation in patients with PHEOCHROMOCYTOMA. (Martindale, The Extra Pharmacopoeia, 30th ed)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)Reward: An object or a situation that can serve to reinforce a response, to satisfy a motive, or to afford pleasure.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.Drug Partial Agonism: Drug agonism involving selective binding but reduced effect. This can result in some degree of DRUG ANTAGONISM.Lisuride: An ergot derivative that acts as an agonist at dopamine D2 receptors (DOPAMINE AGONISTS). It may also act as an antagonist at dopamine D1 receptors, and as an agonist at some serotonin receptors (SEROTONIN RECEPTOR AGONISTS).Drug Interactions: The action of a drug that may affect the activity, metabolism, or toxicity of another drug.Fluphenazine: A phenothiazine used in the treatment of PSYCHOSES. Its properties and uses are generally similar to those of CHLORPROMAZINE.Serotonergic Neurons: Neurons whose primary neurotransmitter is SEROTONIN.Vesicular Monoamine Transport Proteins: A family of vesicular amine transporter proteins that catalyze the transport and storage of CATECHOLAMINES and indolamines into SECRETORY VESICLES.Rats, Wistar: A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.Cyclic AMP: An adenine nucleotide containing one phosphate group which is esterified to both the 3'- and 5'-positions of the sugar moiety. It is a second messenger and a key intracellular regulator, functioning as a mediator of activity for a number of hormones, including epinephrine, glucagon, and ACTH.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.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.Citalopram: 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.Dihydroxyphenylalanine: 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.PhenanthridinesNerve Tissue ProteinsAnalysis of Variance: A statistical technique that isolates and assesses the contributions of categorical independent variables to variation in the mean of a continuous dependent variable.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)Grooming: An animal's cleaning and caring for the body surface. This includes preening, the cleaning and oiling of feathers with the bill or of hair with the tongue.Central Nervous System Stimulants: A loosely defined group of drugs that tend to increase behavioral alertness, agitation, or excitation. They work by a variety of mechanisms, but usually not by direct excitation of neurons. The many drugs that have such actions as side effects to their main therapeutic use are not included here.Serotonin 5-HT3 Receptor Agonists: Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT3 RECEPTORS.Autoradiography: 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)Binding, Competitive: The interaction of two or more substrates or ligands with the same binding site. The displacement of one by the other is used in quantitative and selective affinity measurements.Self Administration: Administration of a drug or chemical by the individual under the direction of a physician. It includes administration clinically or experimentally, by human or animal.Conditioning, Operant: Learning situations in which the sequence responses of the subject are instrumental in producing reinforcement. When the correct response occurs, which involves the selection from among a repertoire of responses, the subject is immediately reinforced.Monoamine Oxidase: An enzyme that catalyzes the oxidative deamination of naturally occurring monoamines. It is a flavin-containing enzyme that is localized in mitochondrial membranes, whether in nerve terminals, the liver, or other organs. Monoamine oxidase is important in regulating the metabolic degradation of catecholamines and serotonin in neural or target tissues. Hepatic monoamine oxidase has a crucial defensive role in inactivating circulating monoamines or those, such as tyramine, that originate in the gut and are absorbed into the portal circulation. (From Goodman and Gilman's, The Pharmacological Basis of Therapeutics, 8th ed, p415) EC 1.4.3.4.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.Dextroamphetamine: The d-form of AMPHETAMINE. It is a central nervous system stimulant and a sympathomimetic. It has also been used in the treatment of narcolepsy and of attention deficit disorders and hyperactivity in children. Dextroamphetamine has multiple mechanisms of action including blocking uptake of adrenergics and dopamine, stimulating release of monamines, and inhibiting monoamine oxidase. It is also a drug of abuse and a psychotomimetic.Time Factors: Elements of limited time intervals, contributing to particular results or situations.Tropanes: N-methyl-8-azabicyclo[3.2.1]octanes best known for the ones found in PLANTS.Serotonin 5-HT4 Receptor Agonists: Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT4 RECEPTORS.Fenclonine: A selective and irreversible inhibitor of tryptophan hydroxylase, a rate-limiting enzyme in the biosynthesis of serotonin (5-HYDROXYTRYPTAMINE). Fenclonine acts pharmacologically to deplete endogenous levels of serotonin.Benzamides: BENZOIC ACID amides.Octopamine: An alpha-adrenergic sympathomimetic amine, biosynthesized from tyramine in the CNS and platelets and also in invertebrate nervous systems. It is used to treat hypotension and as a cardiotonic. The natural D(-) form is more potent than the L(+) form in producing cardiovascular adrenergic responses. It is also a neurotransmitter in some invertebrates.Paroxetine: A serotonin uptake inhibitor that is effective in the treatment of depression.Adenylate Cyclase: An enzyme of the lyase class that catalyzes the formation of CYCLIC AMP and pyrophosphate from ATP. EC 4.6.1.1.Serotonin 5-HT4 Receptor Antagonists: Drugs that bind to but do not activate SEROTONIN 5-HT4 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN RECEPTOR AGONISTS.Amphetamines: Analogs or derivatives of AMPHETAMINE. Many are sympathomimetics and central nervous system stimulators causing excitation, vasopressin, bronchodilation, and to varying degrees, anorexia, analepsis, nasal decongestion, and some smooth muscle relaxation.Tranquilizing Agents: A traditional grouping of drugs said to have a soothing or calming effect on mood, thought, or behavior. Included here are the ANTI-ANXIETY AGENTS (minor tranquilizers), ANTIMANIC AGENTS, and the ANTIPSYCHOTIC AGENTS (major tranquilizers). These drugs act by different mechanisms and are used for different therapeutic purposes.Locomotion: Movement or the ability to move from one place or another. It can refer to humans, vertebrate or invertebrate animals, and microorganisms.Neurotransmitter Agents: Substances used for their pharmacological actions on any aspect of neurotransmitter systems. Neurotransmitter agents include agonists, antagonists, degradation inhibitors, uptake inhibitors, depleters, precursors, and modulators of receptor function.Benzothiazoles: Compounds with a benzene ring fused to a thiazole ring.Microinjections: The injection of very small amounts of fluid, often with the aid of a microscope and microsyringes.Hyperkinesis: Excessive movement of muscles of the body as a whole, which may be associated with organic or psychological disorders.3,4-Dihydroxyphenylacetic Acid: A deaminated metabolite of LEVODOPA.Exploratory Behavior: The tendency to explore or investigate a novel environment. It is considered a motivation not clearly distinguishable from curiosity.Ergotamines: A series of structurally-related alkaloids containing the ergotaman backbone structure.Cocaine-Related Disorders: Disorders related or resulting from use of cocaine.Mice, Knockout: Strains of mice in which certain GENES of their GENOMES have been disrupted, or "knocked-out". To produce knockouts, using RECOMBINANT DNA technology, the normal DNA sequence of the gene being studied is altered to prevent synthesis of a normal gene product. Cloned cells in which this DNA alteration is successful are then injected into mouse EMBRYOS to produce chimeric mice. The chimeric mice are then bred to yield a strain in which all the cells of the mouse contain the disrupted gene. Knockout mice are used as EXPERIMENTAL ANIMAL MODELS for diseases (DISEASE MODELS, ANIMAL) and to clarify the functions of the genes.1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine: A dopaminergic neurotoxic compound which produces irreversible clinical, chemical, and pathological alterations that mimic those found in Parkinson disease.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.RNA, Messenger: RNA sequences that serve as templates for protein synthesis. Bacterial mRNAs are generally primary transcripts in that they do not require post-transcriptional processing. Eukaryotic mRNA is synthesized in the nucleus and must be exported to the cytoplasm for translation. Most eukaryotic mRNAs have a sequence of polyadenylic acid at the 3' end, referred to as the poly(A) tail. The function of this tail is not known for certain, but it may play a role in the export of mature mRNA from the nucleus as well as in helping stabilize some mRNA molecules by retarding their degradation in the cytoplasm.Butyrophenones: Compounds containing phenyl-1-butanone.Rats, Inbred Strains: Genetically identical individuals developed from brother and sister matings which have been carried out for twenty or more generations or by parent x offspring matings carried out with certain restrictions. This also includes animals with a long history of closed colony breeding.Limbic System: A set of forebrain structures common to all mammals that is defined functionally and anatomically. It is implicated in the higher integration of visceral, olfactory, and somatic information as well as homeostatic responses including fundamental survival behaviors (feeding, mating, emotion). For most authors, it includes the AMYGDALA; EPITHALAMUS; GYRUS CINGULI; hippocampal formation (see HIPPOCAMPUS); HYPOTHALAMUS; PARAHIPPOCAMPAL GYRUS; SEPTAL NUCLEI; anterior nuclear group of thalamus, and portions of the basal ganglia. (Parent, Carpenter's Human Neuroanatomy, 9th ed, p744; NeuroNames, http://rprcsgi.rprc.washington.edu/neuronames/index.html (September 2, 1998)).Piribedil: A dopamine D2 agonist. It is used in the treatment of parkinson disease, particularly for alleviation of tremor. It has also been used for circulatory disorders and in other applications as a D2 agonist.Oxazines: Six-membered heterocycles containing an oxygen and a nitrogen.Catecholamines: A general class of ortho-dihydroxyphenylalkylamines derived from tyrosine.Metoclopramide: A dopamine D2 antagonist that is used as an antiemetic.Piperidines: A family of hexahydropyridines.Tiapamil Hydrochloride: A phenylethylamine derivative that acts as a calcium antagonist showing hemodynamic effects in patients with acute myocardial infarction.Biogenic Amines: A group of naturally occurring amines derived by enzymatic decarboxylation of the natural amino acids. Many have powerful physiological effects (e.g., histamine, serotonin, epinephrine, tyramine). Those derived from aromatic amino acids, and also their synthetic analogs (e.g., amphetamine), are of use in pharmacology.Adrenergic Uptake Inhibitors: Drugs that block the transport of adrenergic transmitters into axon terminals or into storage vesicles within terminals. The tricyclic antidepressants (ANTIDEPRESSIVE AGENTS, TRICYCLIC) and amphetamines are among the therapeutically important drugs that may act via inhibition of adrenergic transport. Many of these drugs also block transport of serotonin.Synaptosomes: 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.Mice, Inbred C57BLElectric Stimulation: Use of electric potential or currents to elicit biological responses.Adrenergic Agents: Drugs that act on adrenergic receptors or affect the life cycle of adrenergic transmitters. Included here are adrenergic agonists and antagonists and agents that affect the synthesis, storage, uptake, metabolism, or release of adrenergic transmitters.Parkinson Disease, Secondary: Conditions which feature clinical manifestations resembling primary Parkinson disease that are caused by a known or suspected condition. Examples include parkinsonism caused by vascular injury, drugs, trauma, toxin exposure, neoplasms, infections and degenerative or hereditary conditions. Clinical features may include bradykinesia, rigidity, parkinsonian gait, and masked facies. In general, tremor is less prominent in secondary parkinsonism than in the primary form. (From Joynt, Clinical Neurology, 1998, Ch38, pp39-42)5,7-Dihydroxytryptamine: 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.Medial Forebrain Bundle: 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.Positron-Emission Tomography: An imaging technique using compounds labelled with short-lived positron-emitting radionuclides (such as carbon-11, nitrogen-13, oxygen-15 and fluorine-18) to measure cell metabolism. It has been useful in study of soft tissues such as CANCER; CARDIOVASCULAR SYSTEM; and brain. SINGLE-PHOTON EMISSION-COMPUTED TOMOGRAPHY is closely related to positron emission tomography, but uses isotopes with longer half-lives and resolution is lower.Carbon Radioisotopes: Unstable isotopes of carbon that decay or disintegrate emitting radiation. C atoms with atomic weights 10, 11, and 14-16 are radioactive carbon isotopes.N-Methyl-3,4-methylenedioxyamphetamine: An N-substituted amphetamine analog. It is a widely abused drug classified as a hallucinogen and causes marked, long-lasting changes in brain serotonergic systems. It is commonly referred to as MDMA or ecstasy.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.Aromatic-L-Amino-Acid Decarboxylases: An enzyme group with broad specificity. The enzymes decarboxylate a range of aromatic amino acids including dihydroxyphenylalanine (DOPA DECARBOXYLASE); TRYPTOPHAN; and HYDROXYTRYPTOPHAN.Sympatholytics: Drugs that inhibit the actions of the sympathetic nervous system by any mechanism. The most common of these are the ADRENERGIC ANTAGONISTS and drugs that deplete norepinephrine or reduce the release of transmitters from adrenergic postganglionic terminals (see ADRENERGIC AGENTS). Drugs that act in the central nervous system to reduce sympathetic activity (e.g., centrally acting alpha-2 adrenergic agonists, see ADRENERGIC ALPHA-AGONISTS) are included here.Rats, Long-Evans: An outbred strain of rats developed in 1915 by crossing several Wistar Institute white females with a wild gray male. Inbred strains have been derived from this original outbred strain, including Long-Evans cinnamon rats (RATS, INBRED LEC) and Otsuka-Long-Evans-Tokushima Fatty rats (RATS, INBRED OLETF), which are models for Wilson's disease and non-insulin dependent diabetes mellitus, respectively.GTP-Binding Proteins: Regulatory proteins that act as molecular switches. They control a wide range of biological processes including: receptor signaling, intracellular signal transduction pathways, and protein synthesis. Their activity is regulated by factors that control their ability to bind to and hydrolyze GTP to GDP. EC 3.6.1.-.Schizophrenia: A severe emotional disorder of psychotic depth characteristically marked by a retreat from reality with delusion formation, HALLUCINATIONS, emotional disharmony, and regressive behavior.Patch-Clamp Techniques: 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.Colforsin: Potent activator of the adenylate cyclase system and the biosynthesis of cyclic AMP. From the plant COLEUS FORSKOHLII. Has antihypertensive, positive inotropic, platelet aggregation inhibitory, and smooth muscle relaxant activities; also lowers intraocular pressure and promotes release of hormones from the pituitary gland.Fenfluramine: A centrally active drug that apparently both blocks serotonin uptake and provokes transport-mediated serotonin release.Glutamic Acid: A non-essential amino acid naturally occurring in the L-form. Glutamic acid is the most common excitatory neurotransmitter in the CENTRAL NERVOUS SYSTEM.Neural Pathways: Neural tracts connecting one part of the nervous system with another.Monoamine Oxidase Inhibitors: A chemically heterogeneous group of drugs that have in common the ability to block oxidative deamination of naturally occurring monoamines. (From Gilman, et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 8th ed, p414)Kinetics: The rate dynamics in chemical or physical systems.Cerebral Cortex: 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.Catechol O-Methyltransferase: Enzyme that catalyzes the movement of a methyl group from S-adenosylmethionone to a catechol or a catecholamine.Tegmentum Mesencephali: Portion of midbrain situated under the dorsal TECTUM MESENCEPHALI. The two ventrolateral cylindrical masses or peduncles are large nerve fiber bundles providing a tract of passage between the FOREBRAIN with the HINDBRAIN. Ventral MIDBRAIN also contains three colorful structures: the GRAY MATTER (PERIAQUEDUCTAL GRAY), the black substance (SUBSTANTIA NIGRA), and the RED NUCLEUS.gamma-Aminobutyric Acid: The most common inhibitory neurotransmitter in the central nervous system.Norepinephrine Plasma Membrane Transport Proteins: 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.Extracellular Space: 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.Reinforcement (Psychology): The strengthening of a conditioned response.Animals, Newborn: Refers to animals in the period of time just after birth.Carbidopa: An inhibitor of DOPA DECARBOXYLASE, preventing conversion of LEVODOPA to dopamine. It is used in PARKINSON DISEASE to reduce peripheral adverse effects of LEVODOPA. It has no antiparkinson actions by itself.Tryptamines: Decarboxylated monoamine derivatives of TRYPTOPHAN.Startle Reaction: A complex involuntary response to an unexpected strong stimulus usually auditory in nature.
6-MeO-THH
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Neuroscience/Cellular Neurobiology/Neurotransmitters - Wikibooks, open books for an open world
Lexapro description as supplied by the FDA and Forrest Pharma.
Dopamine receptor - wikidocAgonistAntagonistsAntagonistInhibitorsInhibitionAcetylcholineProtein-coupledSerotonergicMuscarinicDopaminergicGABAInhibitoryNeurotransmittersAdrenergic receptorsAntagonismMediateInhibitorEndogenousLigandsBlockadeVitroAgonismRelease of dopamineNeuronsModulationAntidepressantsSynthesisSelectivityMetabolismMolecularModulateHigher affinityAffinity for D1 receptorsNeurologicalOrallyNMDAMonoamineRegulateHead twitches in miceGlutamateStriatalAdenylateRisk of Serotonin SyndromeSchizophreniaInteractionsCholinergicUptakeHighly selective
Agonist51
- Six healthy volunteers received two PET scans, one after placebo, the other after 1 mg flesinoxan, a selective 5-HT1A receptor agonist. (nih.gov)
- We did not find any difference in striatal [11C]raclopride binding between conditions, even though flesinoxan lead to typical 5-HT1A receptor agonist side effects and produced elevation of growth hormone in five of the six subjects. (nih.gov)
- Recent studies have suggested that aripiprazole , a partial dopamine agonist, reduces the prolactin response to antipsychotics. (clinicaltrials.gov)
- BRL 54443 is a 5-HT1E and 5-HT1F receptor agonist with pK i of 8.7 and 9.25, respectively, with a weak binding affinity for 5-HT1A, 5-HT1B, 5-HT1D receptors. (selleckchem.com)
- Eletriptan is a selective 5-HT1B and 5-HT1D receptor agonist with K i of 0.92 nM and 3.14 nM, respectively. (selleckchem.com)
- Aripiprazole is a human 5-HT 1A receptor partial agonist with a K i of 4.2 nM. (selleckchem.com)
- Urapidil HCl is a hydrochloride salt form of urapidil which is α1-adrenoceptor antagonist and 5-HT1A receptor agonist with pIC50 of 6.13 and 6.4 respectively. (selleckchem.com)
- Almotriptan Malate is a selective 5-hydroxytryptamine1B/1D (5-HT1B/1D) receptor agonist, used for the treatment of Migraine attacks in adults. (selleckchem.com)
- Rizatriptan Benzoate is a 5-HT1 agonist triptan drug for the treatment of migraine headaches. (selleckchem.com)
- Buspirone is a serotonergic ( 5HT(1A) receptor agonist ) anxiolytic drug with some D(2) dopaminergic effect, used for anxiety disorders. (selleckchem.com)
- BMY 7378 is a multi-targeted inhibitor of α2C-adrenoceptor and α1D-adrenoceptor with pK i of 6.54 and 8.2, respectively, and acts as a mixed agonist and antagonist for 5-HT1A receptor with pK i of 8.3. (selleckchem.com)
- Vilazodone HCl is a selective serotonin reuptake inhibitor ( SSRI ) and a partial agonist of 5-HT1A receptors , used for the treatment of major depressive disorder. (selleckchem.com)
- DOSTINEX Tablets contain cabergoline, a dopamine receptor agonist . (rxlist.com)
- Requip is a dopamine agonist commonly prescribed for treating Parkinson's disease and Restless Leg Syndrome . (progressivehealth.com)
- Since Requip contains a dopamine agonist, dopamine antagonists such as neuroleptics can reduce its efficacy. (progressivehealth.com)
- Ropinirole is a non-ergoline dopamine agonist initially intended for only treating Parkinson's disease. (progressivehealth.com)
- Ropinirole is a dopamine receptor agonist. (progressivehealth.com)
- It is a full agonist on dopamine, D2 receptors. (progressivehealth.com)
- It is a partial D 2 and 5-HT 1A receptor agonist and has been prescribed as an atypical antipsychotical drug. (utmb.edu)
- Here we examined the effects of the 5-HT 1B R agonist 5-propoxy-3-(1,2,3,6-tetrahydro-4-pyridinyl)-1H-pyrrolo[3,2-b]pyridine (CP94253) on spontaneous and cocaine-induced locomotion and on cocaine-primed reinstatement of conditioned place preference (CPP) in male mice given daily repeated injections of either saline or cocaine (15 mg/kg, IP) for 20 days. (frontiersin.org)
- These 5-HT 1B R agonist effects are reversed by a 5-HT 1B R antagonist, demonstrating that they are 5-HT 1B R-mediated. (frontiersin.org)
- The D 2 Lh form may function as a classical post-synaptic receptor, i.e., transmit information (in either an excitatory or an inhibitory fashion) unless blocked by a receptor antagonist or a synthetic partial agonist . (wikipedia.org)
- A semisynthetic ergotamine alkaloid that is a dopamine D2 agonist. (selfdecode.com)
- The D 2 Lh may have the classic function of a post-synaptic receptor, i.e., keep going on the neurotransmission (excitatory or inhibitory) once blocked by a receptor antagonist or stimulated by the endogenous neurotransmitter itself or a synthetic full or partial agonist . (wikidoc.org)
- Atropine (muscarinic cholinergic blocking agent), pyrilamine maleate (PM, histamine H 1 blocker), cimetidine (histamine H 2 blocker), 8-hydroxy-2-(di-n-propylamino)-tetralin (8-OHDPAT, specific 5-HT 1A receptor agonist) and SCH-23390 (selective dopamine D 1 receptor antagonist) were examined on the cough response to inhaled capsaicin in conscious guinea-pigs. (elsevier.com)
- Serotonin 5-HT1F receptor agonist indicated to treat acute migraine with or without aura. (medscape.com)
- 5-HT1B/1D receptor agonist. (medscape.com)
- A selective agonist for serotonin 5-HT1B/1D receptors, naratriptan has higher bioavailability and a longer half-life than sumatriptan, which may contribute to a lower rate of headache recurrences. (medscape.com)
- A selective agonist for serotonin 5-HT1B/1D receptors in cranial arteries, zolmitriptan suppresses the inflammation associated with migraine headaches. (medscape.com)
- A selective agonist for serotonin 5-HT1B/1D receptors in cranial arteries, rizatriptan suppresses the inflammation associated with migraine headaches. (medscape.com)
- A selective 5-HT1B/1D receptor agonist, almotriptan results in cranial vessel constriction, inhibition of neuropeptide release, and reduced pain transmission in trigeminal pathways. (medscape.com)
- Which antidepressants with 5-HT1 receptor agonist activity are available for the treatment of fibromyalgia? (medscape.com)
- Currently available drugs with 5-HT1a receptor agonist activity include buspirone (Buspar), vilazodone (Viibryd), and vortioxetine (Brintellix). (medscape.com)
- Preliminary research suggests that metergoline is an agonist at the D2 receptor , which is not surprising given its similarity to lisuride, bromocriptine, etc. (raypeatforum.com)
- A dopamine agonist and serotonin antagonist. (raypeatforum.com)
- Metergoline is a potent serotonin antagonist and putative dopamine agonist. (raypeatforum.com)
- Dihydrexidine - full agonist with 10-fold selectivity for D 1 -like receptors over D 2 that has been in Phase IIa clinical trials as a cognitive enhancer. (worldheritage.org)
- CY-208,243 - high intrinsic activity partial agonist with moderate selectivity for D 1 -like over D 2 -like receptors, member of ergoline ligand family like pergolide and bromocriptine . (worldheritage.org)
- Subsequently we examined the ability of LSD, 5-HT and a number of tryptamine derivatives to stimulate cAMP accumulation in order to determine their agonist potency and efficacy. (meta.org)
- Serotonin hydrochloride is a monoamine neurotransmitter in the CNS and an endogenous 5-HT receptor agonist. (medchemexpress.com)
- Pimavanserin is a selective inverse agonist of the 5-HT2A receptor with pIC 50 and pK d of 8.73 and 9.3, respectively. (medchemexpress.com)
- 2-Methyl-5-HT (2-Methyl-5-hydroxytryptamine) is a potent and selective 5-HT 3 receptor agonist. (medchemexpress.com)
- Sumatriptan succinate (GR 43175) is a serotonin1 (5-HT1) receptor agonist, which is effective in the acute treatment of migraine headache. (medchemexpress.com)
- PF-04995274 is a potent, high-affinity, orally active and partial serotonin 4 receptor (5-HT 4 R) agonist. (medchemexpress.com)
- Aripiprazole (OPC-14597) is a human 5-HT1A receptor partial agonist with a Ki of 4.2 nM. (medchemexpress.com)
- Pindolol (LB-46) is a nonselective β-blocker with partial beta-adrenergic receptor agonist activity, also functions as a 5-HT1A receptor weak partial agonist / antagonist (Ki=33nM). (medchemexpress.com)
- Lorcaserin is a serotonin 2C receptor agonist. (bvsalud.org)
- 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)
- A derivative of morphine that is a dopamine D2 agonist. (drugbank.ca)
- Taken together, our data suggested that THB, with D 2 receptor antagonist and 5-HT 1A receptor agonist properties, has significant potential as a therapeutic for treatment of FD. (aspetjournals.org)
- Ginkgo Biloba acts as an agonist / modulator of 5-HT1A receptor expression, whereas Berberine acts as a presynaptic only agonist of 5-HT1A's - while at the 5-HT1A postsynaptic (where it releases ACTH, cortisol, prolactin etc) it acts to inhibit. (longecity.org)
Antagonists3
- A variety of tryptamine derivatives were tested and showed a significantly higher affinity when the 5-HT6 receptor was labelled with [3H]-5-HT, whereas ergoline compounds and several antagonists had higher affinities when [3H]-LSD was used as radioligand. (meta.org)
- The Emergence of Selective 5-HT2B Antagonists Structures, Activities and Potential Therapeutic Applications [General Reviews]. (ebscohost.com)
- While selective 5-HT2A antagonists have been known for some time, knowledge of the precise role played by the 5-HT2B receptor was hampered by the. (ebscohost.com)
Antagonist18
- LY310762 is a 5-HT1D receptor antagonist with K i of 249 nM, having a weaker affinity for 5-HT1B receptor. (selleckchem.com)
- Asenapine is a high-affinity antagonist of serotonin , norepinephrine , dopamine and histamine receptors , used for the treatment of schizophrenia and acute mania associated with bipolar disorder. (selleckchem.com)
- BRL-15572 is a 5-HT1D receptor antagonist with pK i of 7.9, also shows a considerable affinity at 5-HT1A and 5-HT2B receptors, exhibiting 60-fold selectivity over 5-HT1B receptor. (selleckchem.com)
- Risperidone is a mutil-targeted antagonist for dopamine, serotonin, adrenergic and histamine receptors , used to treat schizophrenia and bipolar disorder. (selleckchem.com)
- Iloperidone is a dopamine (D2)/serotonin (5-HT2) receptor antagonist, used for the treatment of schizophrenia. (selleckchem.com)
- Sertraline HCl is a 5-HT antagonist with K i of 13 nM. (selleckchem.com)
- In vivo occupancy of the 5-HT1A receptor by a novel pan 5-HT1(A/B/D) receptor antagonist, GSK588045, using positron emission tomography. (semanticscholar.org)
- it is a potent antagonist on the serotonin receptors 5-HT1, 5-HT2, 5-HT6, and 5-HT7. (raypeatforum.com)
- More importantly, just like lisuride metergoline is a potent antagonist on the dreaded 5-HT2B receptor. (raypeatforum.com)
- In addition, unlike other serotonin antagonist that simply block serotonin receptors metergoline is actually capable of also reducing serotonin synthesis. (raypeatforum.com)
- As a serotonin antagonist it targets the 5-HT1, 5-HT2, 5-HT6, and 5-HT7 receptors but due to its general antiserotonin effects it is considered a non-specific serotonin antagonist just like cyproheptadine. (raypeatforum.com)
- As metergoline acts predominantly as a serotonin antagonist it might be expected to have additive or synergistic effects when combiend with bromocriptine. (raypeatforum.com)
- Chlorpromazine Hydrochloride is an antagonist of the dopamine D2 , 5HT2A , potassium channel and sodium channel . (medchemexpress.com)
- Risperidone is a serotonin 5-HT 2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D 2 receptor antagonist, with K i s of 4.8, 5.9 nM for 5-HT 2A and dopamine D 2 receptor, respectively. (medchemexpress.com)
- Olanzapine (LY170053) is 5-HT2 and D1/D2 antagonist. (medchemexpress.com)
- SB269970 hydrochloride (SB-269970A) is a hydrochloride salt form of SB-269970, which is a 5-HT7 receptor antagonist with the pK i of 8.3, exhibits >50-fold selectivity against other receptors. (medchemexpress.com)
- 0.05), which was inhibited by [ O -methyl-3 H ]- N -(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)- N -(2-pyridinyl)cyclohexanecarboxamide trihydrochloride (WAY-100635), a 5-HT 1A antagonist, and N ω -nitro- l -arginine methyl ester, a nitric-oxide synthase inhibitor but not a vasoactive intestinal peptide antagonist, was observed. (aspetjournals.org)
- Metergoline SHOULD also work as it is know to be 5-HT2B antagonist as well but I don't have much in vivo evidence to back it up with. (raypeatforum.com)
Inhibitors2
- Lexapro is in the drug class called selective withdrawal serotonin reuptake inhibitors (ssris). (lifeisnotbubblewrapped.com)
- Some of the most widely prescribed medications are selective serotonin reuptake inhibitors (SSRIs), based on the hypothesized role of serotonin in the production of PMS symptoms. (springer.com)
Inhibition10
- The invention relates to a group of novel phenylpiperazine derivatives with a dual mode of action: serotonin reuptake inhibition and partial agonism on dopamine-D 2 receptors. (google.com)
- Insulin indirectly relieves GS inhibition ( 4 , 5 ) through a signaling cascade beginning with phosphorylation of substrates, including insulin receptor substrate 1 (IRS-1), by the tyrosine kinase activity of activated insulin receptor ( 6 , 7 ). (diabetesjournals.org)
- The mechanism of antidepressant action of escitalopram, the S-enantiomer of racemic citalopram, is presumed to be linked to potentiation of serotonergic activity in the central nervous system (CNS) resulting from its inhibition of CNS neuronal reuptake of serotonin (5-HT). (theroadbackprogram.com)
- Escitalopram is at least 100-fold more potent than the R-enantiomer with respect to inhibition of 5-HT reuptake and inhibition of 5-HT neuronal firing rate. (theroadbackprogram.com)
- In vitro studies show that escitalopram is at least 7 and 27 times more potent than S - DCT and S-DDCT, respectively, in the inhibition of serotonin reuptake, suggesting that the metabolites of escitalopram do not contribute significantly to the antidepressant actions of escitalopram. (theroadbackprogram.com)
- Lamotrigine is a novel anticonvulsant drug for inhibition of 5-HT with IC50 of 240 μM and 474 μM in human platelets and rat brain synaptosomes, and also is a sodium channel blocker. (selleckchem.com)
- Isocorynoxeine, a major bioactive tetracyclic oxindole alkaloids found in Uncaria rhynchophylla , exhibits a dose-dependent inhibition of 5-HT2A receptor-mediated current response with an IC50 of 72.4 μM and shows various beneficial effects, including lowering blood pressure, vasodilatation, and protection against ischemia-induced neuronal damage. (selleckchem.com)
- Bupropion is structurally different from other antidepressants and its ability to reduce pain is due to its inhibition of the neuronal reuptake of norepinephrine and dopamine. (medscape.com)
- The efficacy of Paroxetine is presumed to be linked to potentiation of serotonergic activity in the central nervous system resulting from inhibition of neuronal reuptake of serotonin (5-hydroxy-tryptamine, 5 HT). (khidmatdrug.online)
- Berry-Kravis E, Freedman SB, Dawson G. Specific receptor-mediated inhibition of cyclic AMP synthesis by dopamine in a neuroblastoma X brain hybrid cell line NCB-20. (rush.edu)
Acetylcholine11
- With the awareness of selectivity challenge, ActiTarg-CNS, focuses on diverse structural variations and targets primarily three general receptor groups: serotonin, dopamine, and acetylcholine. (timtec.net)
- Using the longitudinal muscle of the guinea pig ilium, MDMA evoked dose-related, transient contractions, but failed to reduce contractions produced by serotonin, acetylcholine, or GABA. (ecstasy.org)
- We studied the roles for four major neurotransmitters [acetylcholine, histamine, serotonin (5-hydroxytryptamine, 5-HT) and dopamine] in the modulation of the cough reflex. (elsevier.com)
- Like other transmembrane receptors, acetylcholine receptors are classified according to their "pharmacology," or according to their relative affinities and sensitivities to different molecules. (meddic.jp)
- Although all acetylcholine receptors, by definition, respond to acetylcholine, they respond to other molecules as well. (meddic.jp)
- nicotinic acetylcholine receptors ( nAChR , also known as "ionotropic" acetylcholine receptors) are particularly responsive to nicotine. (meddic.jp)
- muscarinic acetylcholine receptors ( mAChR , also known as "metabotropic" acetylcholine receptors) are particularly responsive to muscarine. (meddic.jp)
- Nicotinic acetylcholine receptors can be blocked by curare, hexamethonium and toxins present in the venoms of snakes and shellfishes, like α-bungarotoxin. (meddic.jp)
- Muscarinic acetylcholine receptors can be blocked by the drugs atropine and scopolamine. (meddic.jp)
- Further, they demonstrate that Bacopa primarily either acts via antioxidant mechanism (i.e., neuroprotection) or alters different neurotransmitters (serotonin (5-hydroxytryptamine, 5-HT), dopamine (DA), acetylcholine (ACh), γ -aminobutyric acid (GABA)) to execute the pharmacological effect. (hindawi.com)
- HTR1B is a G-protein coupled receptor that activates a second messenger cascade to mediate inhibitory neurotransmission and regulate the release of serotonin, dopamine, and acetylcholine in the brain. (biomedcentral.com)
Protein-coupled11
- G protein-coupled receptors (GPCRs) are cell surface receptors that mediate physiological responses to a diverse array of stimuli. (aspetjournals.org)
- The largest class of cell surface receptors in mammalian genomes is the superfamily of G protein-coupled receptors (GPCRs 1 ). (aspetjournals.org)
- Dopamine receptors are a class of G protein-coupled receptors that are prominent in the vertebrate central nervous system (CNS). (wikipedia.org)
- Dopamine receptors have been shown to heterodimerize with a number of other G protein-coupled receptors . (wikipedia.org)
- While the rest are G protein-coupled receptors, 5-HT3 is a sodium/potassium ligand gated ion channel. (progressivehealth.com)
- In contrast, the mAChRs are not ion channels, but belong instead to the superfamily of G-protein-coupled receptors that activate other ionic channels via a second messenger cascade. (meddic.jp)
- The TSH receptor is a member of the G protein-coupled receptor superfamily of integral membrane proteins [ 1 ] and is coupled to the G s protein. (meddic.jp)
- The D 5 subtype is a G-protein coupled receptor , which promotes synthesis of cAMP by adenylyl cyclase via activation of Gα s/olf family of G proteins . (wikidoc.org)
- It is suggested that these G protein-coupled receptors redundantly activate phospholipase C in basolateral amygdala . (wikidoc.org)
- This G protein-coupled receptor stimulates adenylate cyclase and indirectly activates cyclic AMP-dependent protein kinases . (worldheritage.org)
- 5-HT receptors (Serotonin receptors) are a group of G protein-coupled receptors (GPCRs) and ligand-gated ion channels (LGICs) found in the central and peripheral nervous systems. (medchemexpress.com)
Serotonergic11
- Vortioxetine (Lu AA21004) is a multimodal serotonergic agent, inhibits 5-HT1A , 5-HT1B , 5-HT3A , 5-HT7 receptor and SERT with IC50 of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively. (selleckchem.com)
- Escitalopram has no or very low affinity for serotonergic (5-HT1-7) or other receptors including alpha- and beta-adrenergic, dopamine (D 1-5), histamine (H1-3), muscarinic (M1-5), and benzodiazepine receptors. (theroadbackprogram.com)
- Thus, one aim of this study was to localize, autoradiographically, the region-specific changes of dopaminergic, serotonergic, and GABAergic transmitter receptors in the hippocampus and the amygdala after a stressful and fear-inducing situation, i.e., separation from the family and exposure to a novel environment. (jneurosci.org)
- CONTEXT Serotonergic dysfunction is implicated in the pathogenesis of posttraumatic stress disorder (PTSD), and recent animal models suggest that disturbances in serotonin type 1B receptor function, in particular, may contribute to chronic anxiety. (semanticscholar.org)
- Serotonin and drugs that act on the serotonergic system produce their effects by binding to serotonin receptors. (progressivehealth.com)
- Serotonin syndrome refers to the set of adverse drug reactions caused by excessive serotonergic activity mostly in the central nervous system but also in the serotonin receptors located in the peripheral nervous system. (progressivehealth.com)
- This review focuses on the studies which trace the effect of Bacopa treatment on serotonergic system and 5-HT mediated key molecular changes that are associated with memory formation. (hindawi.com)
- OBJECTIVE: Activation of one or more serotonin (5-HT) receptors may play a role in mediating the antidepressant effects of serotonergic antidepressants. (bvsalud.org)
- Serotonergic Agents: Co-administration of linezolid and serotonergic agents was not associated with serotonin syndrome in Phase 1, 2 or 3 studies. (epharmapedia.com)
- Thus berberine may be a useful tool not for increasing serotonergic neurotransmission through that pathway in particular, but for inhibiting excess serotonin and for reducing some of the negative neuroendocrine effects of serotonin. (longecity.org)
- Berberine also inhibits PDE-5 mRNA - thus it may be the best natural tool for post and current SSRI-induced sexual dysfunction as well as in improving cognitive disturbances caused by serotonergic drugs. (longecity.org)
Muscarinic6
- Receptor binding experiments indicated that McN-5652 has a weak affinity for serotonin 5-HT2 and alpha-1 adrenergic receptors (apparent Ki approximately 200 nM) and a very low affinity for dopamine D1 and D2 receptors, serotonin 5-HT1, alpha-2 adrenergic, muscarinic and gamma-aminobutyric acid-A receptors. (aspetjournals.org)
- Antagonism of muscarinic, histaminergic, and adrenergic receptors has been hypothesized to be associated with various anticholinergic, sedative, and cardiovascular side effects of other psychotropic drugs. (theroadbackprogram.com)
- Nicotinic and muscarinic are two main kinds of "cholinergic" receptors. (meddic.jp)
- Molecular biology has shown that the nicotinic and muscarinic receptors belong to distinct protein superfamilies. (meddic.jp)
- It has been shown that M 1 -Muscarinic receptors cooperate with D 5 receptors and beta-2 adrenergic receptors to consolidate cued fear memory. (wikidoc.org)
- Takasu K, Honda M, Ono H, Tanabe M. Spinal alpha(2)-adrenergic and muscarinic receptors and the NO release cascade mediate supraspinally produced effectiveness of gabapentin at decreasing mechanical hypersensitivity in mice after partial nerve injury. (labome.org)
Dopaminergic3
- In addition to the cerebral dopaminergic (DA) system, the serotoninergic (5-HT) system also plays a crucial role in regulating psychoemotional, cognitive and motor functions in the central nervous system (CNS). (utmb.edu)
- Abnormal dopamine receptor signaling and dopaminergic nerve function is implicated in several neuropsychiatric disorders. (wikipedia.org)
- Gamma aminobutyric acid (GABA) hypoactivity induces dopamine hyperactivity because dopaminergic neurons are affected by the inhibitory influence. (ebscohost.com)
GABA9
- the first widely accepted demonstration of functional consequences for GPCR heterodimerization came from the GABA B receptors. (aspetjournals.org)
- It has no affinity for 5-HT1, alpha-1, beta adrenoreceptors and GABA receptors. (progressivehealth.com)
- GABA has an ionotropic receptor, GABAA, that directly gates Cl- channels, and it has a metabotropic receptor, GABAB, that gates K+ and Ca2+ channels indirectly. (wikibooks.org)
- GABA A receptor density in the hippocampus and amygdala was downregulated (nonsignificant trend) after parental separation. (jneurosci.org)
- no such suppressing influence was observed for the GABA A receptors. (jneurosci.org)
- FST and FO were tested for their binding activity of the GABA(A)-benzodiazepine and 5-HT(2C) receptors, which are well-known molecular targets for sleep aids. (bvsalud.org)
- In GABA(A) and 5-HT(2C) receptor binding assays, FST displayed an effective concentration-dependent binding affinity to GABA(A) receptor, similar to the binding affinity to 5-HT(2C) receptor. (bvsalud.org)
- FO exhibited higher affinity to 5-HT(2C) receptor, compared with the GABA(A) receptor. (bvsalud.org)
- The data demonstrate that FST and FO possess sedative-hypnotic activity possibly by modulating GABA(A) and 5-HT(2C) receptors. (bvsalud.org)
Inhibitory1
- At 5-HT1 and 5-HT5 receptors, serotonin produces inhibitory responses while at the other serotonin receptors, excitatory responses are produced. (progressivehealth.com)
Neurotransmitters3
- Drugs in this class prevent the breakdown of monoamine neurotransmitters such as serotonin. (progressivehealth.com)
- The serotonin receptors modulate the release of many neurotransmitters, as well as many hormones. (medchemexpress.com)
- Numerous studies have focused on the neurotransmitters related to the pathogenesis of schizophrenia, including serotonin. (biomedcentral.com)
Adrenergic receptors2
- What are the three types of adrenergic receptors and what G proteins are they coupled to? (brainscape.com)
- It has only low to moderate affinity for cholinergic and alpha-adrenergic receptors. (drugbank.ca)
Antagonism3
- Thioridazine hydrochloride is an antipsychotic drug, used in the treatment of schizophrenia and psychosis, shows D4 selectivity or serotonin antagonism. (medchemexpress.com)
- When taking metergoline and lisuride simultaneaously isn't the 5-HT1A antagonism of metergoline cancelled out by the lisuride agonism of the 5-HT1A? (raypeatforum.com)
- Yes, you want 5-HT1 and 5-HT2B antagonism. (raypeatforum.com)
Mediate3
- Of the approximately 1000 genes thought to encode GPCRs in humans, about 300 to 400 mediate the effects of endogenous ligands, with the remainder being sensory receptors. (aspetjournals.org)
- D 1 receptors regulate neuronal growth and development, mediate some behavioral responses, and modulate dopamine receptor D 2 -mediated events. (worldheritage.org)
- However, the key signaling components that mediate specific function of serotonin neurotransmission have not been fully identified. (frontiersin.org)
Inhibitor20
- McN-5652: a highly potent inhibitor of serotonin uptake. (aspetjournals.org)
- McN-5652 is characterized by exceptionally high potency as an inhibitor of the uptake of serotonin by rat brain synaptosomes in vitro (Ki approximately 0.6 nM) and ex vivo (ED50 approximately 2 mg/kg p.o. (aspetjournals.org)
- McN-5652 also potently inhibited the synaptosomal uptake of norepinephrine (Ki approximately 3 nM) and was a moderately potent inhibitor of the synaptosomal uptake of dopamine (Ki approximately 40 nM). (aspetjournals.org)
- A serotonin transport inhibitor (Fluoxetine) reduced the amount released, whereas the addition of tryptophan increased the amount released. (ecstasy.org)
- LEXAPRO ™ (escitalopram oxalate) is an orally administered selective serotonin reuptake inhibitor (SSRI). (theroadbackprogram.com)
- In vitro and in vivo studies in animals suggest that escitalopram is a highly selective serotonin reuptake inhibitor (SSRI) with minimal effects on norepinephrine and dopamine neuronal reuptake. (theroadbackprogram.com)
- Fluoxetine is a selective serotonin -reuptake inhibitor (SSRI) at the neuronal membrane, used in the treatment of depression. (selleckchem.com)
- Sevoflurane is a noncompetitive inhibitor of 5-HT3 receptor . (selleckchem.com)
- Venlafaxine HCl is an arylalkanolamine serotonin-norepinephrine reuptake inhibitor (SNRI), used to treat major depressive disorder (MDD), generalised anxiety disorder (GAD), panic disorder and social phobia. (selleckchem.com)
- Dapoxetine HCl is a short-acting novel selective serotonin reuptake inhibitor, used for the treatment of premature ejaculation. (selleckchem.com)
- Fluvoxamine Maleate is a selective serotonin (5-HT) reuptake inhibitor (SSRI), used in the treatment of obsessive-compulsive disorder. (selleckchem.com)
- Desvenlafaxine is a serotonin (5-HT) and norepinephrine (NE) reuptake inhibitor with K i of 40.2 nM and 558.4 nM, respectively. (selleckchem.com)
- Escitalopram Oxalate is a selective serotonin (5-HT) reuptake inhibitor (SSRI) with K i of 0.89 nM. (selleckchem.com)
- Duloxetine HCl is a serotonin-norepinephrine reuptake inhibitor with K i of 4.6 nM, used for treatment of major depressive disorder and generalized anxiety disorder (GAD). (selleckchem.com)
- Paroxetine Mesylate is the mesylate salt form of paroxetine, a phenylpiperidine derivative and a selective serotonin reuptake inhibitor (SSRI) with antidepressant and anxiolytic properties. (selleckchem.com)
- Levomilnacipran Hydrochloride is a selective serotonin and norepinephrine reuptake inhibitor with antidepressant activity. (selleckchem.com)
- SSRI is also known as selective serotonin reuptake inhibitor. (progressivehealth.com)
- In vitro studies in animals also suggest that paroxetine is a potent and highly selective inhibitor of neuronal serotonin reuptake and has only very weak effects on norepinephrine and dopamine neuronal reuptake. (khidmatdrug.online)
- Serotonin hydrochloride is also a catechol O-methyltransferase ( COMT ) inhibitor with a K i of 44 μM. (medchemexpress.com)
- Selective serotonin reuptake inhibitor (SSRI) medications affect the levels of serotonin in the brain. (emedicinehealth.com)
Endogenous2
- Bradberry, C.W., Sprouse, J.S., Aghajanian, G.K. and Roth, R.H. 3,4-Methylenedioxymethamphetamine (MDMA)-Induced Release of Endogenous Serotonin from the Rat Dorsal Raphe Nucleus in vitro: Effects of Fluoxetine and Tryptophan. (ecstasy.org)
- The amines are of great interest, because both mood-altering drugs and addictive drugs show a very straightforward affinity for receptors sites designed for endogenous amines. (blogspot.com)
Ligands5
- Ye, N, Song, Z & Zhang, A 2014, ' Dual ligands targeting dopamine D 2 and serotonin 5-HT 1A receptors as new antipsychotical or anti-parkinsonian agents ', Current Medicinal Chemistry , vol. 21, no. 4, pp. 437-457. (utmb.edu)
- There are a number of ligands selective for the D 1 receptors. (worldheritage.org)
- None of the known ligands is selective for the D 1 vs. the D 5 receptor, but the benzazepines generally are more selective for the D 1 and D 5 receptors versus the D 2 -like family. (worldheritage.org)
- The recent molecular identification of 5-HT4 receptors and the development of selective 5-HT4 receptor ligands have led to many important new insights into the signalling pathways and the physiological roles of these G protein-coupledreceptors in neurones. (ebscohost.com)
- Recent Advances in the Discovery of Selective and Non-Selective 5-HT1D Receptor Ligands. (ebscohost.com)
Blockade1
- D1 receptor agonism and D2 receptor blockade also increases mRNA translation by phosphorylating ribosomal protein s6 , resulting in activation of mTOR. (wikipedia.org)
Vitro2
- An in vitro assay has been used to compare several drugs for their ability to induce synaptosomal serotonin release. (ecstasy.org)
- This mini-review will focus on recent in vitro and in vivo pharmacological and biochemical studies showing the involvement of 5-HT4 receptors in cognitive processes and the amyloid precursor protein processing. (ebscohost.com)
Agonism5
- The putative dopamine agonism is probably responsible at least partially for this effect. (raypeatforum.com)
- However, its exact dopamine receptor agonism profile is not well-known. (raypeatforum.com)
- So, it represents a viable alternative for experiments where lowering of prolactin is desirable but WITHOUT agonism (and potential downregulation) of dopamine receptors. (raypeatforum.com)
- The dopamine agonism profile of metergoline is not well-known except some evidence for D2 receptor agonism. (raypeatforum.com)
- So either metergoline or cyproheptadine would cancel out cabergoline's agonism of 5-HT2B? (raypeatforum.com)
Release of dopamine3
- It affects synthesis, storage, and release of dopamine into the synaptic cleft ). (wikipedia.org)
- This last compound was, however, some 10x more effective than MDMA in the release of dopamine. (ecstasy.org)
- The D 2 Sh are pre-synaptic situated, having modulatory functions (called autoreceptor , they regulate the neurotransmission by feed-back mechanisms, i.e., synthesis, storage and release of dopamine into the synaptic cleft ). (wikidoc.org)
Neurons3
- Serotonin gating of cortical and thalamic glutamate inputs onto principal neurons of the basolateral amygdala. (semanticscholar.org)
- The 5-HT2A receptor is mainly expressed in nociceptive sensory neurons in rat lumbar dorsal root ganglia. (semanticscholar.org)
- Dopamine receptor D 5 is exclusively expressed by large aspiny neurons in neostriatum of primates, which are typically cholinergic interneurons . (wikidoc.org)
Modulation3
- Dopamine receptors have key roles in many processes, including the control of motivation, learning, and fine motor movement, as well as modulation of neuroendocrine signaling. (wikidoc.org)
- Subtype-specific changes in 5-HT receptor-mediated modulation of C fibre-evoked spinal field potentials are triggered by peripheral nerve injury. (semanticscholar.org)
- Modulation of hyaluronan receptor (CD44) function in vivo in a murine model of rheumatoid arthritis. (rush.edu)
Antidepressants1
- The most important groups of drugs acting on serotonin receptors are the antidepressants, MAOI and SSRI. (progressivehealth.com)
Synthesis1
- The level of serotonin synthesis in the body is increased by foods that contain more tryptophan (the amino acid that serves as a precursor to serotonin) that competing amino acids such as leucine and phenylalanine. (progressivehealth.com)
Selectivity1
- Although dihydrexidine has significant D 2 properties, it is highly biased at D 2 receptors and was used for the first demonstration of functional selectivity with dopamine receptors. (worldheritage.org)
Metabolism1
- Therefore, they prevent the metabolism of serotonin and, therefore, increases its activity at serotonin receptors. (progressivehealth.com)
Molecular3
- Its empirical formula is C 26 H 37 N 5 O 2 and its molecular weight is 451.62. (rxlist.com)
- Another conclusion might be that we should wait until we have more information about the molecular and physiological basis for obesity before designing new medications to help the obese (5). (lowcarber.org)
- 1992). "Molecular cloning and sequencing of an alternatively spliced form of the human thyrotropin receptor transcript. (meddic.jp)
Higher affinity3
- Nortriptyline is a metabolite of Amitriptyline and nortriptyline has a higher affinity for noradrenaline than serotonin, which is why I think it can wire people more than Amitriptyline can. (ic-network.com)
- Amitriptyline has a higher affinity for serotonin. (ic-network.com)
- D 5 receptor is a subtype of the dopamine receptor that has a 10-fold higher affinity for dopamine than the D 1 subtype. (wikidoc.org)
Affinity for D1 receptors1
- Molindone has much lower affinity for D2 receptors than most antipsychotic agents and has a relatively low affinity for D1 receptors. (drugbank.ca)
Neurological1
- Each receptor family in its downstream signaling pathways commands broad spectrum of neurological processes. (timtec.net)
Orally1
- Usual Pediatric Dose for Migraine: Use only after a clear mail diagnosis of migraine mail has maxalt been established 6 years or older and weight less than 40 kg: -Initial dose: 5 mg orally once 6 years or older and. (partizipation.at)
NMDA2
- The postsynaptic receptors for glutamate include three types of ionotropic receptors, AMPA, kainate, and NMDA, and eight metabotropic receptors, mGluR1 through mGluR8. (wikibooks.org)
- At postsynaptic sites, it mediates the scaffolding of NMDA receptors, AMPA receptors, potassium channels, and other associated signaling protein clusters. (biolegend.com)
Monoamine1
Regulate2
- D 5 receptors are thought to positively regulate expression of renalase . (wikidoc.org)
- Do you think NAC (N-Acetyl Cysteine) could help regulate excessive dopamine as well? (raypeatforum.com)
Head twitches in mice1
- Results: FCS-304 significantly potentiated 5-HTP induced head twitches in mice, in a dose dependent manner. (bvsalud.org)
Glutamate1
- MAGUKs, such as PSD-95, SAP97, PSD-83, CASK, and MAGIs are involved in the synaptic development and function where they are important for the spatial organization of both pre- and postsynaptic proteins, including glutamate and other receptors. (biolegend.com)
Striatal2
- The release of tritiated serotonin and dopamine from superfused rat striatal slices was observed for three amphetamine derivatives. (ecstasy.org)
- D 5 receptor is also found in striatal astrocytes of the rat basal ganglia . (wikidoc.org)
Adenylate2
- The D 4 receptor is considered to be D 2 -like in which the activated receptor inhibits the enzyme adenylate cyclase , thereby reducing the intracellular concentration of the second messenger cyclic AMP . (wikipedia.org)
- Berry-Kravis E, Dawson G. Possible role of gangliosides in regulating an adenylate cyclase-linked 5-hydroxytryptamine (5-HT1) receptor. (rush.edu)
Risk of Serotonin Syndrome1
- Taking them within two weeks best of each other increases your risk of serotonin syndrome. (trans2000.com)
Schizophrenia2
- Among the large 5-HT receptor family, accumulating data have revealed new insights into the therapeutic benefit of the 5-HT 1A receptor in treating various CNS disorders, especially schizophrenia and Parkinson's disease. (utmb.edu)
- Prior studies addressing the association between schizophrenia and HTR1B polymorphisms in the Chinese Han population include only the 5′-untranslated (5'UTR) and coding regions, with little data concerning the 5′-promoter and 3′-regulatory regions. (biomedcentral.com)
Interactions2
- Such concerns are best addressed by considering the evidence that these receptor-receptor interactions are specific versus non-specific and that they are functionally important versus physiologically irrelevant. (aspetjournals.org)
- Long-term serotonin changes are blocked by 5-HT re-uptake blockers, and the interactions between MDMA and caffeine have been reported. (ecstasy.org)
Cholinergic1
- The muscarine cholinergic receptor activates a G protein when bound to extracellular ACh. (meddic.jp)
Uptake2
- McN-5652 is one of a series of substituted pyrrolo-isoquinolines that, as a group, potently inhibit the uptake of one or more of the monoamines, norepinephrine, serotonin and dopamine. (aspetjournals.org)
- Studies at clinically relevant doses in humans have demonstrated that paroxetine blocks the uptake of serotonin into human platelets. (khidmatdrug.online)
Highly selective1
- In return, GSK3 directly interacts with serotonin receptors in a highly selective manner, with a prominent effect on modulating serotonin 1B receptor activity. (frontiersin.org)
