Adrenergic uptake inhibitors. Medical search

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.

Drugs that inhibit the transport of neurotransmitters into axon terminals or into storage vesicles within terminals. For many transmitters, uptake determines the time course of transmitter action so inhibiting uptake prolongs the activity of the transmitter. Blocking uptake may also deplete available transmitter stores. Many clinically important drugs are uptake inhibitors although the indirect reactions of the brain rather than the acute block of uptake itself is often responsible for the therapeutic effects.

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.

A centrally active muscarinic antagonist that has been used in the symptomatic treatment of PARKINSON DISEASE. Benztropine also inhibits the uptake of dopamine.

Compounds that suppress or block the plasma membrane transport of GAMMA-AMINOBUTYRIC ACID by GABA PLASMA MEMBRANE TRANSPORT PROTEINS.

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 It was withdrawn worldwide in 1986 due to the risk of acute hemolytic anemia with intravascular hemolysis resulting from its use.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)

One of the SEROTONIN UPTAKE INHIBITORS formerly used for depression but was withdrawn worldwide in September 1983 because of the risk of GUILLAIN-BARRE SYNDROME associated with its use. (From Martindale, The Extra Pharmacopoeia, 29th ed, p385)

Compounds that specifically inhibit the reuptake of serotonin in the brain.

A tricyclic dibenzazepine compound that potentiates neurotransmission. Desipramine selectively blocks reuptake of norepinephrine from the neural synapse, and also appears to impair serotonin transport. This compound also possesses minor anticholinergic activity, through its affinity to muscarinic receptors.

A biochemical messenger and regulator, synthesized from the essential amino acid L-TRYPTOPHAN. In humans it is found primarily in the central nervous system, gastrointestinal tract, and blood platelets. Serotonin mediates several important physiological functions including neurotransmission, gastrointestinal motility, hemostasis, and cardiovascular integrity. Multiple receptor families (RECEPTORS, SEROTONIN) explain the broad physiological actions and distribution of this biochemical mediator.

An 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.

A tricyclic antidepressant similar to IMIPRAMINE that selectively inhibits the uptake of serotonin in the brain. It is readily absorbed from the gastrointestinal tract and demethylated in the liver to form its primary active metabolite, desmethylclomipramine.

Sodium chloride-dependent neurotransmitter symporters located primarily on the PLASMA MEMBRANE of dopaminergic neurons. They remove DOPAMINE from the EXTRACELLULAR SPACE by high affinity reuptake into PRESYNAPTIC TERMINALS and are the target of DOPAMINE UPTAKE INHIBITORS.

Drugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or SEROTONIN RECEPTOR AGONISTS.

N-methyl-8-azabicyclo[3.2.1]octanes best known for the ones found in PLANTS.

Tricyclic anorexigenic agent unrelated to and less toxic than AMPHETAMINE, but with some similar side effects. It inhibits uptake of catecholamines and blocks the binding of cocaine to the dopamine uptake transporter.

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.

Tricyclic antidepressant similar in action and side effects to IMIPRAMINE. It may produce excitation.

A dopamine agonist and serotonin antagonist. It has been used similarly to BROMOCRIPTINE as a dopamine agonist and also for MIGRAINE DISORDERS therapy.

A monoamine oxidase inhibitor with antihypertensive properties.

A centrally active drug that apparently both blocks serotonin uptake and provokes transport-mediated serotonin release.

A pharmacologic congener of serotonin that contracts smooth muscle and has actions similar to those of tricyclic antidepressants. It has been proposed as an oxytocic.

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.

Biogenic amines having only one amine moiety. Included in this group are all natural monoamines formed by the enzymatic decarboxylation of natural amino acids.

A selective serotonin reuptake inhibitor that is used in the treatment of DEPRESSION and a variety of ANXIETY DISORDERS.

A serotonin uptake inhibitor that is effective in the treatment of depression.

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.

The relationship between the dose of an administered drug and the response of the organism to the drug.

The prototypical tricyclic antidepressant. It has been used in major depression, dysthymia, bipolar depression, attention-deficit disorders, agoraphobia, and panic disorders. It has less sedative effect than some other members of this therapeutic group.

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.

Membrane proteins whose primary function is to facilitate the transport of molecules across a biological membrane. Included in this broad category are proteins involved in active transport (BIOLOGICAL TRANSPORT, ACTIVE), facilitated transport and ION CHANNELS.

Precursor of epinephrine that is secreted by the adrenal medulla and is a widespread central and autonomic neurotransmitter. Norepinephrine is the principal transmitter of most postganglionic sympathetic fibers and of the diffuse projection system in the brain arising from the locus ceruleus. It is also found in plants and is used pharmacologically as a sympathomimetic.

A 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.

The movement of materials (including biochemical substances and drugs) through a biological system at the cellular level. The transport can be across cell membranes and epithelial layers. It also can occur within intracellular compartments and extracellular compartments.

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.

Sodium chloride-dependent neurotransmitter symporters located primarily on the PLASMA MEMBRANE of serotonergic neurons. They are different than SEROTONIN RECEPTORS, which signal cellular responses to SEROTONIN. They remove SEROTONIN from the EXTRACELLULAR SPACE by high affinity reuptake into PRESYNAPTIC TERMINALS. Regulates signal amplitude and duration at serotonergic synapses and is the site of action of the SEROTONIN UPTAKE INHIBITORS.

A phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells. Dipyridamole also potentiates the antiaggregating action of prostacyclin. (From AMA Drug Evaluations Annual, 1994, p752)

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.

A nucleoside that is composed of ADENINE and D-RIBOSE. Adenosine or adenosine derivatives play many important biological roles in addition to being components of DNA and RNA. Adenosine itself is a neurotransmitter.

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.

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.

2-Chloroadenosine. A metabolically stable analog of adenosine which acts as an adenosine receptor agonist. The compound has a potent effect on the peripheral and central nervous system.

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)

An indirect sympathomimetic. Tyramine does not directly activate adrenergic receptors, but it can serve as a substrate for adrenergic uptake systems and monoamine oxidase so it prolongs the actions of adrenergic transmitters. It also provokes transmitter release from adrenergic terminals. Tyramine may be a neurotransmitter in some invertebrate nervous systems.

The action of a drug that may affect the activity, metabolism, or toxicity of another drug.

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.

Fatty acid derivatives that have specificity for CANNABINOID RECEPTORS. They are structurally distinct from CANNABINOIDS and were originally discovered as a group of endogenous CANNABINOID RECEPTOR AGONISTS.

Compounds that interact with and modulate the activity of CANNABINOID RECEPTORS.

The observable response an animal makes to any situation.

Amides composed of unsaturated aliphatic FATTY ACIDS linked with AMINES by an amide bond. They are most prominent in ASTERACEAE; PIPERACEAE; and RUTACEAE; and also found in ARISTOLOCHIACEAE; BRASSICACEAE; CONVOLVULACEAE; EUPHORBIACEAE; MENISPERMACEAE; POACEAE; and SOLANACEAE. They are recognized by their pungent taste and for causing numbing and salivation.

The most common inhibitory neurotransmitter in the central nervous system.

Purine bases found in body tissues and fluids and in some plants.

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.

Fas/CD95/Apo-I activates the acidic sphingomyelinase via caspases. (1/489)

Fas/CD95/Apo-I has been shown to stimulate a variety of molecules including several members of the caspase family and the acidic sphingomyelinase (Martin and Green 1995; Gulbins et al, 1995). Here, we demonstrate that Fas receptor-triggered activation of the acidic sphingomyelinase, consumption of sphingomyelin, release of ceramide, and subsequent activation of JNK and p38-K are regulated by caspases. Inhibition of caspases by Ac-YVAD-chloromethylketone or transient CrmA transfection prevented stimulation of acidic sphingomyelinase, release of ceramide and activation of JNK and p38-K upon Fas-receptor crosslinking. Likewise, Fas triggered apoptosis was almost completely blocked by Ac-YVAD-chloromethylketone or CrmA mediated inhibition of caspases. The results suggest a new signalling cascade from the Fas receptor via caspases to acidic sphingomyelinase, ceramide and JNK/p38-K. (+info)

Effects of imipramine, an uptake inhibitor, on double-peaked constrictor responses to periarterial nerve stimulation in isolated, perfused canine splenic arteries. (2/489)

Using a cannula insertion method, periarterial nerve electrical stimulations were performed at 1 and 10 Hz in the isolated, perfused canine splenic artery. Electrical nerve stimulation readily caused double-peaked vasoconstrictions. The 1st-peak response at 1 Hz was not influenced by treatment with imipramine but the 2nd one was significantly enhanced by it. The 2nd-peak response was markedly blocked by prazosin. An additional treatment with alpha,beta-methylene ATP, a P2X-purinoceptor desensitizer, abolished electrical stimulation-induced vascular responses that remained. At 10 Hz, the responses to electrical stimulation were not significantly influenced by imipramine. On the other hand, the imipramine treatment inhibited the tyramine-induced vasoconstriction but potentiated the noradrenaline-induced one. ATP-induced responses were not modified by imipramine. From these results, it is concluded that 1) the 1st-peaked constriction is mainly due to a P2X-purinoceptor-dependent mechanism, 2) the 2nd one is mainly due to an alpha1-adrenoceptor-dependent mechanism, and 3) presynaptic uptake mechanisms may perform an important role in the regulation of vascular reactivity, especially at a low frequency. (+info)

Transmembrane domain I contributes to the permeation pathway for serotonin and ions in the serotonin transporter. (3/489)

Mutation of a conserved Asp (D98) in the rat serotonin (5HT) transporter (rSERT) to Glu (D98E) led to decreased 5HT transport capacity, diminished coupling to extracellular Na+ and Cl-, and a selective loss of antagonist potencies (cocaine, imipramine, and citalopram but not paroxetine or mazindol) with no change in 5HT Km value. D98E, which extends the acidic side chain by one carbon, affected the rank-order potency of substrate analogs for inhibition of 5HT transport, selectively increasing the potency of two analogs with shorter alkylamine side chains, gramine, and dihydroxybenzylamine. D98E also increased the efficacy of gramine relative to 5HT for inducing substrate-activated currents in Xenopus laevis oocytes, but these currents were noticeably dependent on extracellular medium acidification. I-V profiles for substrate-independent and -dependent currents indicated that the mutation selectively impacts ion permeation coupled to 5HT occupancy. The ability of the D98E mutant to modulate selective aspects of substrate recognition, to perturb ion dependence as well as modify substrate-induced currents, suggests that transmembrane domain I plays a critical role in defining the permeation pathway of biogenic amine transporters. (+info)

Diurnal variation in 5-HT1B autoreceptor function in the anterior hypothalamus in vivo: effect of chronic antidepressant drug treatment. (4/489)

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

Endothelium is required in the vascular spasm induced by tetraethylammonium and endothelin-1 in guinea-pig aorta. (5/489)

1. To investigate the role of endothelium in vascular spasm, we studied the influence of endothelin-1 (ET-1) on the contracting and spasmogenic effect of the K+-channel blocker, tetraethylammonium (TEA), in aorta rings of reserpine-treated guinea-pigs, perfused with either control (5.5 mM) or elevated (50 mM) glucose concentration. 2. Endothelium-dependent relaxation induced by acetylcholine was lost in rings contracted by noradrenaline in the presence of elevated glucose. In control medium, TEA (1-20 mM) induced a sustained tonic contraction, followed by a phasic spasm, characterized by rhythmic contractions. Elevated glucose, ET-1 (3 nM), or both, reduced the EC50 of TEA-induced tonic contraction, without modifying the maximum contractile effect. 3. In control medium, ET-1 reduced the time before TEA-induced spasm and increased the rate of rhythmic contractions. TEA-induced spasm was abolished by elevated glucose, and restored by ET-1. The spasm induced by TEA and ET-1 was amplified by the ETA antagonist, EMD94246, and suppressed by the ET(A)-ET(B) antagonist, bosentan. In endothelium-denuded vessels incubated with high glucose and ET-1, TEA evoked only a tonic contraction. 4. In control medium, L-NAME (N(G)-nitro-L-arginine methyl ester) abolished TEA-induced rhythmic contractions. L-arginine, but not D-arginine, prevented the effect of L-NAME. In the presence of elevated glucose and ET-1, TEA-induced spasm was not affected by L-NAME, whereas verapamil, indomethacin, metyrapone, glybenclamide or apamin abolished the phasic spasm, unmasking the tonic contracture. 5. In conclusion, endothelium plays a regulatory role in the genesis and maintenance of TEA-induced rhythmic contractions, through the release endothelium derived relaxing factor and vasodilating eicosanoids. (+info)

Neuronal uptake affects dynamic characteristics of heart rate response to sympathetic stimulation. (6/489)

Recently, studies in our laboratory involving the use of a Gaussian white noise technique demonstrated that the transfer function from sympathetic stimulation frequency to heart rate (HR) response showed dynamic characteristics of a second-order low-pass filter. However, determinants for the characteristics remain to be established. We examined the effect of an increase in mean sympathetic stimulation frequency and that of a blockade of the neuronal uptake mechanism on the transfer function in anesthetized rabbits. We found that increasing mean sympathetic stimulation frequency from 1 to 4 Hz significantly (P < 0.01) decreased the dynamic gain of the transfer function without affecting other parameters, such as the natural frequency, lag time, or damping coefficient. In contrast, the administration of desipramine (0.3 mg/kg iv), a neuronal uptake blocking agent, significantly (P < 0.01) decreased both the dynamic gain and the natural frequency and prolonged the lag time. These results suggest that the removal rate of norepinephrine at the neuroeffector junction, rather than the amount of available norepinephrine, plays an important role in determining the low-pass filter characteristics of the HR response to sympathetic stimulation. (+info)

Decrease in hepatic CYP2C11 mRNA and increase in heme oxygenase activity after intracerebroventricular injection of bacterial endotoxin. (7/489)

We previously reported (Arch. Toxcol. 1998, 72, 492-498) that the differential decrease in the levels of hepatic cytochrome P450 (CYP) isozymes in rats was observed 24 hr after intracerebroventricular (i.c.v.) injection of bacterial lipopolysaccharide (LPS) at the dose ineffective (0.1 microgram) when injected intraperitoneally (i.p.). Among CYP isozymes we examined, the male specific CYP isozyme, CYP2C11 was most severely affected by i.c.v. injection of LPS. In this study, we examined the gene expression of CYP2C11, the total P450 contents, the CYP2C11-dependent activity of imipramine N-demethylase (IMND) and protein of CYP2C11 10 hr after i.c.v. or i.p. injections of LPS. Intracerebroventricular injection of LPS significantly decreased the level of CYP2C11 mRNA (to 63% of saline i.c.v. control), the total P450 contents (to 70% of saline i.c.v. control), the IMND activity (to 74% of saline i.c.v. control), but not protein of CYP2C11 in rat liver. In contrast, i.p. injection of LPS at the same dose as i.c.v. did not significantly affect these parameters. Since CYP is a heme protein, we also measured the activity of heme oxygenase (HO) using the same rat liver microsomes. The HO activity was increased to 166% by i.c.v. injection of LPS and 135% by i.p. injection of LPS compared to corresponding saline control. It is suggested that i.c.v. injection of LPS down-regulates the expression of CYP2C11 at transcriptional level and that both the decrease in CYP2C11 mRNA and the increase in heme degradation may be involved in the decreased level of protein and activity of CYP2C11 by i.c.v. injection of LPS in rat liver. (+info)

Activities of trovafloxacin compared with those of other fluoroquinolones against purified topoisomerases and gyrA and grlA mutants of Staphylococcus aureus. (8/489)

Frequencies of mutation to resistance with trovafloxacin and four other quinolones were determined with quinolone-susceptible Staphylococcus aureus RN4220 by a direct plating method. First-step mutants were selected less frequently with trovafloxacin (1.1 x 10(-10) at 2 to 4x the MIC) than with levofloxacin or ciprofloxacin (3.0 x 10(-7) to 3.0 x 10(-8) at 2 to 4x the MIC). Mutants with a change in GrlA (Ser80-->Phe or Tyr) were most commonly selected with trovafloxacin, ciprofloxacin, levofloxacin, or pefloxacin. First-step mutants were difficult to select with sparfloxacin; however, second-step mutants with mutations in gyrA were easily selected when a preexisting mutation in grlA was present. Against 29 S. aureus clinical isolates with known mutations in gyrA and/or grlA, trovafloxacin was the most active quinolone tested (MIC at which 50% of isolates are inhibited [MIC(50)] and MIC(90), 1 and 4 microg/ml, respectively); in comparison, MIC(50)s and MIC(90)s were 32 and 128, 16 and 32, 8 and 32, and 128 and 256 microg/ml for ciprofloxacin, sparfloxacin, levofloxacin, and pefloxacin, respectively. Strains with a mutation in grlA only were generally susceptible to all of the quinolones tested. For mutants with changes in both grlA and gyrA MICs were higher and were generally above the susceptibility breakpoint for ciprofloxacin, sparfloxacin, levofloxacin, and pefloxacin. Addition of reserpine (20 microg/ml) lowered the MICs only of ciprofloxacin fourfold or more for 18 of 29 clinical strains. Topoisomerase IV and DNA gyrase genes were cloned from S. aureus RN4220 and from two mutants with changes in GrlA (Ser80-->Phe and Glu84-->Lys). The enzymes were overexpressed in Escherichia coli GI724, purified, and used in DNA catalytic and cleavage assays that measured the relative potency of each quinolone. Trovafloxacin was at least five times more potent than ciprofloxacin, sparfloxacin, levofloxacin, or pefloxacin in stimulating topoisomerase IV-mediated DNA cleavage. While all of the quinolones were less potent in cleavage assays with the altered topoisomerase IV, trovafloxacin retained its greater potency relative to those of the other quinolones tested. The greater intrinsic potency of trovafloxacin against the lethal topoisomerase IV target in S. aureus contributes to its improved potency against clinical strains of S. aureus that are resistant to other quinolones. (+info)

Dopamine reuptake inhibitor (en) , monoamine oxidase inhibitor (en) , adrenergic uptake inhibitors (en) , adrenergic agent (en) ...

https://eu.wikipedia.org/wiki/Anfetamina

Adrenergic uptake inhibitor. *Bietaserpine. *Deserpidine. *Methoserpidine. *Rescinnamine. *Reserpine. *Syrosingopine. Tyrosine ...

https://en.wikipedia.org/wiki/Fenoldopam

Adrenergic uptake inhibitor. *Bietaserpine. *Deserpidine. *Methoserpidine. *Rescinnamine. *Reserpine. *Syrosingopine. Tyrosine ...

https://en.wikipedia.org/wiki/Trimetaphan_camsilate

Adrenergic uptake inhibitor. *Bietaserpine. *Deserpidine. *Methoserpidine. *Rescinnamine. *Reserpine. *Syrosingopine. Tyrosine ... Guanfacine is a highly selective agonist of the α2A adrenergic receptor, with negligible affinity for any other receptor.[11] ... Arnsten AF (October 2010), "The use of α2A adrenergic agonists for the treatment of attention-deficit/hyperactivity disorder", ... Serotonin antagonists and reuptake inhibitors (e.g., etoperidone, hydroxynefazodone, lubazodone, mepiprazole, nefazodone, ...

https://en.wikipedia.org/wiki/Guanfacine

Adrenergic uptake inhibitor. *Bietaserpine. *Deserpidine. *Methoserpidine. *Rescinnamine. *Reserpine. *Syrosingopine. Tyrosine ... beta-blockers, β-blockers, beta-adrenergic blocking agents, beta antagonists, beta-adrenergic antagonists, beta-adrenoreceptor ... β1-adrenergic receptors are located mainly in the heart and in the kidneys.[4] β2-adrenergic receptors are located mainly in ... "Beta-Adrenergic Blocker Poisoning" (PDF). Courses.ahc.umn.edu. Archived from the original (PDF) on March 3, 2016. Retrieved ...

https://en.wikipedia.org/wiki/Beta_blocker

Two uptake mechanisms exist for terminating the action of adrenergic catecholamines - uptake 1 and uptake 2. Uptake 1 occurs at ... Inhibitors of these enzymes act as indirect agonists of adrenergic receptors as they prolong the action of catecholamines at ... the adrenergic receptors). Directly acting adrenergic agonists act on adrenergic receptors. All adrenergic receptors are G- ... Indirectly acting adrenergic agonists affect the uptake and storage mechanisms involved in adrenergic signalling. ...

https://en.wikipedia.org/wiki/Adrenergic_agonist

Assays have shown that SNRIs have insignificant penchant for mACh, α1 and α2 adrenergic, or H1 receptors. Agents with dual ... Active transport system regulates the uptake of tryptophan across the blood-brain barrier. Serotonergic pathways are classified ... Monoamine reuptake inhibitor List of antidepressants Serotonin releasing agent Selective serotonin reuptake inhibitor (SSRI) ... Selective serotonin reuptake inhibitors (SSRIs) selectively inhibit the reuptake of serotonin and are a widely used group of ...

https://en.wikipedia.org/wiki/Serotonin–norepinephrine_reuptake_inhibitor

... is a potent α2 adrenergic agonist. When xylazine and other α2 adrenergic receptor agonists are administered, they ... Xylazine appears to reduce sensitivity to insulin and glucose uptake in humans. Yohimbine has been used to decrease glucose ... Xylazine also serves as a transport inhibitor by suppressing norepinephrine transport function through competitive inhibition ... Xylazine is an analogue of clonidine and an agonist at the α2 class of adrenergic receptor. It is used for sedation, anesthesia ...

https://en.wikipedia.org/wiki/Xylazine

2008). "In-vitro and in-vivo characterization of JNJ-7925476, a novel triple monoamine uptake inhibitor". European Journal of ... at functionally important adrenergic receptor sites in the brain. However, elation may be associated with an excess of such ... Wong, DT; Bymaster, FP (1978). "An inhibitor of dopamine uptake, LR5182, cis-3-(3,4-dichlorophenyl)-2-n,n-dimethylaminomethyl- ... Wong DT, Bymaster FP, Engleman EA (1995). "Prozac (fluoxetine, Lilly 110140), the first selective serotonin uptake inhibitor ...

https://en.wikipedia.org/wiki/Serotonin–norepinephrine–dopamine_reuptake_inhibitor

Plasminogen activator inhibitor is also increased following cocaine use, thereby promoting thrombosis. Similar to local ... Fareed, Fareed N.; Chan, Gar; Hoffman, Robert S. (2007-12-01). "Death temporally related to the use of a Beta adrenergic ... re-uptake transporters with equal affinity. Monoamines accumulate in the synaptic cleft resulting in enhanced and prolonged ... Cocaine-induced platelet activation and thrombus formation is another deleterious effect, caused by alpha-adrenergic- and ...

https://en.wikipedia.org/wiki/Cocaine_intoxication

... adrenergic uptake inhibitors MeSH D27.505.519.625.600.220 - dopamine uptake inhibitors MeSH D27.505.519.625.600.850 - serotonin ... adrenergic uptake inhibitors MeSH D27.505.696.577.600.220 - dopamine uptake inhibitors MeSH D27.505.696.577.600.850 - serotonin ... adrenergic beta-antagonists MeSH D27.505.519.625.050.601 - adrenergic uptake inhibitors MeSH D27.505.519.625.120 - cholinergic ... adrenergic beta-antagonists MeSH D27.505.696.577.050.601 - adrenergic uptake inhibitors MeSH D27.505.696.577.120 - cholinergic ...

https://en.wikipedia.org/wiki/List_of_MeSH_codes_(D27)

Nakachi N, Kiuchi Y, Inagaki M, Inazu M, Yamazaki Y, Oguchi K (August 1995). "Effects of various dopamine uptake inhibitors on ... Gasić S, Korn A, Eichler HG (May 1986). "Effect of diclofensine, a novel antidepressant, on peripheral adrenergic function". ... 1982). "Diclofensine (Ro 8-4650)--a potent inhibitor of monoamine uptake: biochemical and behavioural effects in comparison ... Di Renzo G, Amoroso S, Taglialatela M, Canzoniero LM, Maida P, Lombardi G, Annunziato L (1988). "Pure uptake blockers of ...

https://en.wikipedia.org/wiki/Diclofensine

Binding studies indicate that it has no effect on monoamine uptake and no affinity for adrenergic, histamine, cholinergic, ... Inhibitors of these enzymes, e.g. the SSRI antidepressant fluvoxamine, reduce its clearance and can therefore lead to an ... blockade of which enhances the activity of frontocortical dopaminergic and adrenergic pathways". The Journal of Pharmacology ... blockade of which enhances the activity of frontocortical dopaminergic and adrenergic pathways". The Journal of Pharmacology ...

https://en.wikipedia.org/wiki/Agomelatine

Nicotinic, imidazoline I1 and I2, α2-adrenergic, glutamate NMDAr, and serotonin 5-HT2A and 5HT-3 receptors. Ion channels. ... Agmatine specific-selective uptake sites, organic cation transporters (mostly OCT2 subtype), extraneuronal monoamine ... Agmatine is a precursor for polyamine synthesis, competitive inhibitor of polyamine transport, inducer of spermidine/spermine ... It is synthesized in the brain, stored in synaptic vesicles, accumulated by uptake, released by membrane depolarization, and ...

https://en.wikipedia.org/wiki/Agmatine

Assays have shown that selective NRIs have insignificant penchant for mACh, α1 and α2 adrenergic, or H1 receptors.[22] ... Active transport system regulates the uptake of tryptophan across the blood-brain barrier. Serotonergic pathways are classified ... Selective serotonin reuptake inhibitors[edit]. Selective serotonin reuptake inhibitors (SSRIs) selectively inhibit the reuptake ... Monoamine reuptake inhibitor. References[edit]. *^ Cashman JR, Ghirmai S (October 2009). "Inhibition of serotonin and ...

https://en.wikipedia.org/wiki/Serotonin-norepinephrine_reuptake_inhibitor

It acts as a 5-HT2A and α1-adrenergic receptor antagonist and inhibits the reuptake and induces the release of serotonin, ... effects on uptake and retention of monoamines in rat brain synaptosomes". Psychopharmacology. 48 (3): 295-301. doi:10.1007/ ... dopamine, and norepinephrine to varying extents, and has been described as a serotonin antagonist and reuptake inhibitor (SARI ...

https://en.wikipedia.org/wiki/Mepiprazole

Schmidt AW, Hurt SD, Peroutka SJ (1989). "'[3H]quipazine' degradation products label 5-HT uptake sites". Eur. J. Pharmacol. 171 ... Bylund DB, Snyder SH (1976). "Beta adrenergic receptor binding in membrane preparations from mammalian brain". Mol. Pharmacol. ... 1996). "Interactions of selective serotonin reuptake inhibitors with the serotonin 5-HT2c receptor". Psychopharmacology. 126 (3 ... inhibitor, linezolid, and IV methylene blue are contraindicated as it can cause an increased risk of developing serotonin ...

https://en.wikipedia.org/wiki/Nortriptyline

When phosphorylated (by PKA) - disinhibition of Ca2+-ATPase of SR leads to faster Ca2+ uptake into the sarcoplasmic reticulum, ... Thus, activators of PKA, such as the beta-adrenergic agonist epinephrine (released by sympathetic stimulation), may enhance the ... In the unphosphorylated state, phospholamban is an inhibitor of cardiac muscle sarcoplasmic reticulum Ca2+-ATPase (SERCA2) ...

https://en.wikipedia.org/wiki/Phospholamban

... these are called selective serotonin re-uptake inhibitors. They are dependent on serotonin availability in the synapse. The 5- ... Additionally, it inhibits the release of norepinephrine from adrenergic nerves. Serotonin is also a growth factor for some ... Some drugs inhibit the re-uptake of serotonin, making it stay in the synaptic cleft longer. The tricyclic antidepressants (TCAs ... Popa D, Léna C, Alexandre C, Adrien J (April 2008). "Lasting syndrome of depression produced by reduction in serotonin uptake ...

https://en.wikipedia.org/wiki/Serotonin

Assays have shown that selective NRIs have insignificant penchant for mACh, α1 and α2 adrenergic, or H1 receptors.[22] ... Active transport system regulates the uptake of tryptophan across the blood-brain barrier. Serotonergic pathways are classified ... Redirected from Serotonin norepinephrine reuptake inhibitor). Serotonin-norepinephrine reuptake inhibitors (SNRIs) are a class ... Selective serotonin reuptake inhibitorsEdit. Selective serotonin reuptake inhibitors (SSRIs) selectively inhibit the reuptake ...

https://en.m.wikipedia.org/wiki/Serotonin_norepinephrine_reuptake_inhibitor

Waldmeier PC, Baumann PA, Hauser K, Maitre L, Storni A (June 1982). "Oxaprotiline, a noradrenaline uptake inhibitor with an ... It has negligible affinity for the serotonin transporter, dopamine transporter, α2-adrenergic receptor, and muscarinic ... Dextroprotiline acts as a potent norepinephrine reuptake inhibitor and H1 receptor antagonist, as well as a very weak α1- ... Oxaprotiline (developmental code name C 49-802 BDA), also known as hydroxymaprotiline, is a norepinephrine reuptake inhibitor ...

https://en.wikipedia.org/wiki/Oxaprotiline

Assays have shown that SNRIs have insignificant penchant for mACh, α1 and α2 adrenergic, or H1 receptors.[26] ... Active transport system regulates the uptake of tryptophan across the blood-brain barrier. Serotonergic pathways are classified ... Selective serotonin reuptake inhibitorsEdit. Selective serotonin reuptake inhibitors (SSRIs) selectively inhibit the reuptake ... Serotonin-norepinephrine reuptake inhibitors (SNRIs) are a class of antidepressant drugs that treat major depressive disorder ( ...

https://en.m.wikipedia.org/wiki/Serotonin-norepinephrine_reuptake_inhibitors

... 's status as a serotonin transporter (SERT) inhibitor at clinical doses in humans is uncertain. A PET imaging study ... Supporting atomoxetine's selectivity, a human study found no effects on platelet serotonin uptake (a marker of SERT inhibition ... but could be potentiated by NMDA or an α1-adrenergic receptor antagonist, suggesting a glutaminergic mechanism. In Sprague ... Kasi PM, Mounzer R, Gleeson GH (2011). "Cardiovascular side effects of atomoxetine and its interactions with inhibitors of the ...

https://en.wikipedia.org/wiki/Atomoxetine

Examples of medications are: ACE inhibitors, angiotensin receptor blockers,[11] and calcineurin inhibitor immunosuppressants ... Beta2-adrenergic agonist acts on beta-2 receptor to drive potassium into the cells. Therefore, beta blockers can cause the rise ... Insulin increases the uptake of potassium into the cells. Therefore, insulin deficiency can cause hyperkalemia. In addition to ... Calcineurin inhibitors such as cyclosporine, tacrolimus, diazoxide, and minoxidil can cause hyperkalemia.[12] Box jellyfish ...

https://en.m.wikipedia.org/wiki/Hyperkalemia

It also inhibits of neuronal re-uptake of norepinephrine (Uptake-1). These activities increase cardiac output and increase ... It is not an α-adrenergic agonist, does not cause vasoconstriction, and is not a pressor agent. As of 2004 there was some ... It should not be used in people taking monoamine oxidase inhibitors, nor in people who have certain adrenal cancers, low ... It also inhibits the neuronal re-uptake of norepinephrine. The most common adverse effects include fast heart beats and nausea ...

https://en.wikipedia.org/wiki/Dopexamine

Another active metabolite is (E)-10-hydroxynortiptyline, which is a norepinephrine uptake inhibitor four times weaker than ... Amitriptyline additionally acts as a potent inhibitor of the serotonin 5-HT2A, 5-HT2C, the α1A-adrenergic, the histamine H1 and ... A case of clinically significant interaction with potent CYP2D6 inhibitor terbinafine has been reported. A potent inhibitor of ... Schmidt AW, Hurt SD, Peroutka SJ (1989). "'[3H]quipazine' degradation products label 5-HT uptake sites". Eur. J. Pharmacol. 171 ...

https://en.wikipedia.org/wiki/Amitriptyline

Andersen PH (1989). "The dopamine inhibitor GBR 12909: selectivity and molecular mechanism of action". Eur J Pharmacol. 166 (3 ... Richelson E, Pfenning M (1984). "Blockade by antidepressants and related compounds of biogenic amine uptake into rat brain ... hypothalamus and striatum and into adrenergic nerves of rabbit aorta". J Pharmacol Exp Ther. 181 (3): 407-16. PMID 5033010.. ... deoxypipradrol and methylphenidate to inhibit the uptake of tritiated catecholamines into rat cerebral cortex slices, ...

https://da.wikipedia.org/wiki/Methylphenidat

It acts as a norepinephrine reuptake inhibitor, and to a lesser extent as a dopamine reuptake inhibitor. Ciclazindol has no ... Oh VM, Ehsanullah RS, Leighton M, Kirby MJ (January 1979). "Influence of ciclazindol on monoamine uptake and CNS function in ... effects on the SERT, 5-HT receptors, mACh receptors, or α-adrenergic receptors, and has only weak affinity for the H1 receptor ...

https://en.wikipedia.org/wiki/Ciclazindol

A double-blind comparative study of diazepam and clovoxamine, a novel inhibitor of noradrenaline and serotonin reuptake". ... Saletu B, Grünberger J, Rajna P, Karobath M (1980). "Clovoxamine and fluvoxamine-2 biogenic amine re-uptake inhibiting ... adrenergic, and serotonin receptors. The compound is structurally related to fluvoxamine. Freeman HL, Wakelin JS, Calanca A, ... It acts as a serotonin-norepinephrine reuptake inhibitor (SNRI), with little affinity for the muscarinic acetylcholine, ...

https://en.wikipedia.org/wiki/Clovoxamine

5-HT-uptake IC50(μM) DA-uptake IC50(μM) NA-uptake IC50(μM) ... an increase in adrenergic and dopaminergic neurotransmission.[1 ... 5-HT-uptake IC50(μM) DA-uptake IC50(μM) NA-uptake IC50(μM) ... A norepinephrine-dopamine reuptake inhibitor (NDRI) is a drug ... Norepinephrine-dopamine reuptake inhibitors are used for clinical depression, attention deficit hyperactivity disorder (ADHD), ... Amphetamine and many of the other substituted amphetamines are inhibitors of VMAT2 and potent agonists of the trace amine- ...

https://en.m.wikipedia.org/wiki/Norepinephrine-dopamine_reuptake_inhibitor

A Promising Class of Monoamine Uptake Inhibitors". Journal of Medicinal Chemistry. 49 (4): 1420-32. doi:10.1021/jm050797a. PMC ... that the use of any beta blockers to treat hypertension in these patients can cause an unopposed peripheral alpha-adrenergic ... is a stimulant of the cathinone class which acts as a norepinephrine-dopamine reuptake inhibitor (NDRI). It was first developed ...

https://en.wikipedia.org/wiki/Methylenedioxypyrovalerone

"Lamotrigine inhibits monoamine uptake in vitro and modulates 5-hydroxytryptamine uptake in rats". European Journal of ... adrenergic, dopamine D1 and D2, muscarinic, GABA, histaminergic H1, serotonin 5-HT2, and N-methyl-D-aspartate). Inhibitory ... It is known that lamotrigine is a weak inhibitor of human dihydrofolate reductase (DHFR) and other, more powerful, human DHFR ... inhibitors like methotrexate are known to be teratogenic.[47] Lamotrigine is expressed in breast milk; the manufacturer does ...

https://en.wikipedia.org/wiki/Lamotrigine

... has been shown to reduce iodine uptake and thus is classified as a goitrogen. Perchlorate ions are a competitive inhibitor of ... Meta-[I-131]iodobenzylguanidine is a radio-labeled analog of the adrenergic blocking agent guanethidine.[37] Radioactivity is ... Uptake of iodine-131[edit]. To completely block the uptake of iodine-131 by the purposeful addition of perchlorate ions to a ... The image of the thyroid in the neck is due to unwanted uptake of radioiodine (as iodide) by the thyroid, after breakdown of ...

https://en.wikipedia.org/wiki/Iodine-131

Inhibitors of eryptosis include erythropoietin, nitric oxide, catecholamines and high concentrations of urea. ... Iron Transport and Cellular Uptake by Kenneth R. Bridges, Information Center for Sickle Cell and Thalassemic Disorders. ... β-adrenergic receptors. Lipid rafts that have been implicated in cell signaling events in nonerythroid cells have been shown in ...

https://en.m.wikipedia.org/wiki/Red_blood_cells

COX-2 inhibitors[edit]. Main article: COX-2 inhibitor. These drugs have been derived from NSAIDs. The cyclooxygenase enzyme ... efflux and uptake in the rat dorsal raphe nucleus". British Journal of Anaesthesia. 79 (3): 352-6. doi:10.1093/bja/79.3.352. ... "Combining opioid and adrenergic mechanisms for chronic pain". Postgraduate Medicine. 126 (4): 98-114. doi:10.3810/pgm.2014.07. ... COX-2 selective inhibitors Celecoxib. Comes in free form; practically insoluble in water, fairly soluble in organic solvents. ...

https://en.wikipedia.org/wiki/Algesic

... is controlled through the balanced control of lipolytic B-adrenergic receptors and a2A-adrenergic receptor-mediated ... has garnered a great deal of interest after being identified as a potent stimulator of glucose uptake and a browning regulator ... β-adrenergic receptor activation.[46] UCP1 is proposed to function as a fatty acid proton symporter, although the exact ... Plasminogen activator inhibitor-1 (PAI-1). *TNFα. *IL-6. *Leptin. *Estradiol (E2) ...

https://en.wikipedia.org/wiki/Adipose

"A new selective inhibitor for uptake of serotonin into synaptosomes of rat brain: 3-(p-trifluoromethylphenoxy). N-methyl-3- ... "Interaction between the antidepressant-like behavioral effects of beta adrenergic agonists and the cyclic AMP PDE inhibitor ... Part I: monoamine oxidase inhibitors". J Clin Psychopharmacol. 27 (6): 555-9. doi:10.1097/jcp.0b013e3181bb617. PMID 18004120.. ... Anderson IM (2000). "Selective serotonin reuptake inhibitors versus tricyclic antidepressants: a meta-analysis of efficacy and ...

https://kn.wikipedia.org/wiki/ಖಿನ್ನತೆ-ಶಮನಕಾರಿ

Absorption follows the same process as that of lipids; the uptake mechanism appears to be similar to that of vitamin E, another ... Mellors, A.; Tappel, A. (Jul 1966). "Quinones and Quinols as Inhibitors of Lipid Peroxidation". Lipids. 1 (4): 282-284. doi: ... Inhibition of coenzyme Q10-enzymes by clinically used adrenergic blockers of beta-receptors". Research Communications in ... Bhagavan, Hemmi N.; Chopra, Raj K. (2006). "Coenzyme Q10: Absorption, tissue uptake, metabolism and pharmacokinetics". Free ...

https://en.wikipedia.org/wiki/Ubidecarenone

COX-2 inhibitorsEdit. Main article: COX-2 inhibitor. These drugs have been derived from NSAIDs. The cyclooxygenase enzyme ... Smith HS, Raffa RB, Pergolizzi JV, Taylor R, Tallarida RJ (July 2014). "Combining opioid and adrenergic mechanisms for chronic ... efflux and uptake in the rat dorsal raphe nucleus". British Journal of Anaesthesia. 79 (3): 352-6. doi:10.1093/bja/79.3.352. ... COX-2 selective inhibitors Celecoxib. Comes in free form; practically insoluble in water, fairly soluble in organic solvents. ...

https://en.m.wikipedia.org/wiki/Painkiller

Many amphetamines and adrenergic compounds raise body temperatures; whereas some tend to produce more euphoric activity, or ... Green AL, El Hait MA (April 1980). "p-Methoxyamphetamine, a potent reversible inhibitor of type-A monoamine oxidase in vitro ... Tseng LF, Menon MK, Loh HH (May 1976). "Comparative actions of monomethoxyamphetamines on the release and uptake of biogenic ... Differences in the in vivo dynamics of neurotransmitter release and serotonin uptake after acute para-methoxyamphetamine and 3, ...

https://en.wikipedia.org/wiki/Para-Methoxyamphetamine

The altanserin uptake decreases with age reflecting a loss of specific 5-HT2A receptors with age.[101][102][103] A study has ... but through its high affinity for alpha1 adrenergic receptors. It also has high affinity for H1 histaminergic receptors equal ... 5-HT2A receptor is an adaptive process provoked by chronic administration of selective serotonin reuptake inhibitors (SSRIs) ... related to ketanserin such as ritanserin are more selective 5-HT2A receptor antagonists with low affinity for alpha-adrenergic ...

https://en.m.wikipedia.org/wiki/5-HT2A_receptor

Sympathetic (adrenergic). α2: decreases secretion from beta cells, increases secretion from alpha cells, β2: increases ... It also decreases the uptake of glucose in fat and muscle. Glucagon release is stimulated by low blood glucose or insulin ... These include the secretion of inactive enzymes (zymogens), the secretion of the protective enzyme trypsin inhibitor, which ... levels, and during exercise.[16] Insulin acts to decrease blood glucose levels by facilitating uptake by cells (particularly ...

https://en.m.wikipedia.org/wiki/Pancreas

... was a relatively weak inhibitor (IC50 = 0.12 μM) of the uptake.[67] ... An adrenergic antagonist selective for α1 receptors. *^ Reversal of reserpine-induced hypothermia by a drug is a classical test ... a b B. Avula, S. K. Upparapalli, and I. A. Khan (2007). "Simultaneous analysis of adrenergic amines and flavonoids in citrus ... a b F. Pellati, S. Benvenuti, M. Melegari, and F. Firenzuoli (2002). "Determination of adrenergic agonists from extracts and ...

https://en.m.wikipedia.org/wiki/Synephrine

Iodine uptake against a concentration gradient is mediated by a sodium-iodine symporter and is linked to a sodium-potassium ... the contribution of adrenergic activity to hypermetabolism and protein breakdown". Metabolism: Clinical and Experimental. 36 (6 ... perchlorates are used as ionic inhibitors in anti thyroid compounds ... A related parameter is the free thyroxine index, which is total thyroxine multiplied by thyroid hormone uptake, which, in turn ...

https://en.wikipedia.org/wiki/Thyroid_hormone

positive regulation of dopamine uptake involved in synaptic transmission. • signal transduction. • fear response. • dopamine ... Roxindole - D4 selective but also D2 and D3 autoreceptor agonist, 5HT1A receptor agonist, serotonin reuptake inhibitor) ... Apomorphine - D4 selective but also D2 and D3 agonist, α-adrenergic and serotonergic weak antagonist ...

https://en.wikipedia.org/wiki/Dopamine_D4_receptor

... an inhibitor of anandamide uptake, prevents pain behaviour and modulates cytokine and apoptotic pathways in a rat model of ... Adrenergic. *Adrenergic receptor agonist (α. *β (1. *2)). *Adrenergic receptor antagonist (α (1 ... Amino acid reuptake inhibitor *Excitatory amino acid reuptake inhibitor (or glutamate-aspartate reuptake inhibitor) ... In contrast to plasmalemmal reuptake inhibitors, vesicular reuptake inhibitors do not increase the synaptic concentrations of a ...

https://en.wikipedia.org/wiki/Non-selective_monoamine_reuptake_inhibitors

Cheng J, Zhang W, Zhang X, Han F, Li X, He X, Li Q, Chen J (May 2014). "Effect of angiotensin-converting enzyme inhibitors and ... Insulin is the principal hormone that regulates the uptake of glucose from the blood into most cells of the body, especially ... angiotensin converting enzyme inhibitors (ACEIs) improve outcomes in those with DM while the similar medications angiotensin ...

https://en.wikipedia.org/wiki/Diabetic

For similar term named Cholinesterase-blocking drug, see Cholinesterase inhibitor.. Neuromuscular-blocking drugs block ... This also affects pipecuroniums metabolism by resisting hepatic uptake, metabolism, and biliary excretion. The length of the ... Adrenergic. *Adrenergic receptor agonist (α. *β (1. *2)). *Adrenergic receptor antagonist (α (1 ... It is generally accepted that non-depolarizing agents block by acting as reversible competitive inhibitors. That is, they bind ...

https://en.wikipedia.org/wiki/Neuromuscular-blocking_drug

See also: Receptor/signaling modulators • Monoamine reuptake inhibitors • Adrenergics • Dopaminergics • Serotonergics • ... Johnson MP, Conarty PF, Nichols DE (July 1991). "[3H]monoamine releasing and uptake inhibition properties of 3,4- ... and related amphetamine derivatives on inhibition of uptake of [3H]monoamines into synaptosomes from different regions of rat ...

https://en.wikipedia.org/wiki/MDAI

a b Bhagavan, Hemmi N.; Chopra, Raj K. (2006). "Coenzyme Q10: Absorption, tissue uptake, metabolism and pharmacokinetics". Free ... Mellors A, Tappel A, (July 1966). "Quinones and Quinols as Inhibitors of Lipid Peroxidation". Lipids 1 (4): 282-284. PMID ... Inhibition of coenzyme Q10-enzymes by clinically used adrenergic blockers of beta-receptors". Research communications in ... 1996). "Phase I study of lovastatin, an inhibitor of the mevalonate pathway, in patients with cancer". Clinical cancer research ...

https://da.wikipedia.org/wiki/Coenzym_Q10

Free fatty acids released into the blood are then available for cellular uptake.[11] Free fatty acids not immediately taken up ... Epinephrine binds to beta-adrenergic receptors on the cell membrane of the adipocyte, which causes cAMP to be generated inside ... G0S2 acts as a competitive inhibitor in the binding of CGI-58.[6] Fat-specific protein 27 (FSP-27) (a.k.a. CIDEC) is also a ...

https://en.m.wikipedia.org/wiki/Lipolysis

Drugs that block the transport of adrenergic transmitters into axon terminals or into storage vesicles within terminals. The ... Levomilnacipran is a serotonin and norepinephrine reuptake inhibitor and is indicated for the treatment of major depressive ... and amphetamines are among the therapeutically important drugs that may act via inhibition of adrenergic transport. Many of ...

https://www.drugbank.ca/categories/DBCAT000439

Adrenergic agonist (Alpha, Beta2) • Adrenergic antagonist (Alpha, Beta) • Adrenergic uptake inhibitor ... A adrenergic uptake inhibitor is a drug which blocks the reuptake of adrenergic neurotransmitters. ... Serotonin receptor agonist • Serotonin antagonist (5-HT3) • Serotonin uptake inhibitor (SSRI) ... Retrieved from "https://www.wikidoc.org/index.php?title=Adrenergic_uptake_inhibitor&oldid=158678" ...

http://www.wikidoc.org/index.php/Adrenergic_uptake_inhibitor

Maprotiline is a strong inhibitor of noradrenaline re-uptake in the brain and peripheral tissues, however it is worthy to note ... that it is a weak inhibitor of serotonergic uptake. In addition, it displays strong antihistaminic action (which may explain ... Maprotiline also has lower alpha adrenergic blocking activity than amitriptyline. Maprotylina Absorption Completely absorbed ...

http://pharmacycode.com/Maprotylina.html

Amitriptyline, a tertiary amine tricyclic antidepressant, is structurally related to both the skeletal muscle relaxant cyclobenzaprine and the thioxanthene antipsychotics such as thiothixene. It is extremely sedating, and thus improvement of sleep patterns can be the first benefit of treatment. Amitriptyline exhibits strong anticholinergic activity, cardiovascular effects including orthostatic hypotension, changes in heart rhythm and conduction, and a lowering of the seizure threshold. As with other antidepressants, several weeks of therapy may be required in order to realize the full clinical benefit of amitriptyline. Although not a labelled indication, amitriptyline is widely used in the management of chronic nonmalignant pain (e.g., post-herpetic neuralgia, fibromyalgia ...

http://pharmacycode.com/Amitriprolidine.html

Adrenergic Uptake Inhibitors. Neurotransmitter Uptake Inhibitors. Membrane Transport Modulators. Dopamine Uptake Inhibitors. ...

https://clinicaltrials.gov/show/NCT01237366?order=141

Adrenergic Uptake Inhibitors. Neurotransmitter Uptake Inhibitors. Membrane Transport Modulators. Dopamine Uptake Inhibitors. ...

https://clinicaltrials.gov/show/NCT01317277?order=278

Adrenergic Uptake Inhibitors. Neurotransmitter Uptake Inhibitors. Membrane Transport Modulators. Molecular Mechanisms of ... Adrenergic Agents. Neurotransmitter Agents. Antipsychotic Agents. Tranquilizing Agents. Central Nervous System Depressants. ...

https://www.clinicaltrials.gov/ct2/show/NCT01367080?term=AMITRIPTYLINE&rank=45

Adrenergic Uptake Inhibitors. Neurotransmitter Uptake Inhibitors. Membrane Transport Modulators. Molecular Mechanisms of ...

https://www.clinicaltrials.gov/ct2/show/NCT00033033?intr=Reserpine&rank=1

The objectives are as follows: The objective is to assess the efficacy and safety of specific serotonin re-uptake inhibitors ( ... Adrenergic Uptake Inhibitors. *Alternative Medicine/Therapies. *Analgesics. *Anti-Consultants. *Anti-Depressive Agents ... Riera, R.; & Rodriguez-Martin, J.L. Specific serotonin uptake inhibitors versus placebo or antidepressants for fibromyalgia. ( ... Currently available medication classes include the selective serotonin uptake inhibitors, the serotonin and norepinephrine ...

https://naric.com/?q=node/123

Adrenergic Uptake Inhibitors / therapeutic use* * Adult * Cognitive Behavioral Therapy / methods* * Colonic Diseases, ...

https://pubmed.ncbi.nlm.nih.gov/17509027/

Serotonin Uptake Inhibitors / therapeutic use* * Syndrome * Thiophenes / therapeutic use* Substances * Adrenergic Uptake ... Serotonin and noradrenaline reuptake inhibitors (SNRIs) for fibromyalgia syndrome Cochrane Database Syst Rev. 2013 Jan 31;(1): ... Objectives: To assess the benefits and harms of serotonin and noradrenaline reuptake inhibitors (SNRIs) compared with placebo ...

https://pubmed.ncbi.nlm.nih.gov/23440848/?dopt=Abstract

0 (Adrenergic Uptake Inhibitors); 0 (Anti-Dyskinesia Agents); 0 (Antipsychotic Agents); 0 (Dopamine Antagonists); 56LH93261Y ( ... 0 (Adrenergic beta-3 Receptor Agonists); 0 (Adrenergic beta-3 Receptor Antagonists); 0 (Enzyme Inhibitors); 0 (RNA, Messenger ... Pretreatment with itraconazole (ICZ, P-gp inhibitor, 50 mg/kg) for 30 min before oral administration of NDL (10 mg/kg) ... 0 (Adrenergic beta-1 Receptor Antagonists); 0 (Antihypertensive Agents); DRB57K47QC (Celiprolol); Y41JS2NL6U (Bisoprolol). ...

http://bases.bireme.br/cgi-bin/wxislind.exe/iah/online/?IsisScript=iah/iah.xis&nextAction=lnk&base=MEDLINE&lang=p&format=detailed.pft&indexSearch=EX&exprSearch=D02.033.100.624.698.268

Adrenergic uptake inhibitor Serotonin reuptake inhibitors Dopamine antagonist Histamine antagonist amitriptyline (& ... Chemistry of re-uptake inhibitors The chemical action of re-uptake inhibitors in general was unknown for a long time. In August ... Understanding of their mode of action as re-uptake inhibitors and development of the serotonin theory of depression came in the ... Note: Other sources suggest that most of the tricyclics combine adrenergic and serotonergic effects to some degree. This is ...

https://www.bionity.com/en/encyclopedia/Tricyclic_antidepressant.html

Dopamine reuptake inhibitor (en) , monoamine oxidase inhibitor (en) , adrenergic uptake inhibitors (en) , adrenergic agent (en) ...

https://eu.wikipedia.org/wiki/Anfetamina

Adrenergic Uptake Inhibitors (adverse effects, pharmacology, therapeutic use) *Atomoxetine Hydrochloride. *Attention Deficit ... Atomoxetine is a specific, noradrenergic reuptake inhibitor that provides an effective treatment option for patients with ADHD ...

http://www.curehunter.com/public/pubmed19689165.do

Adrenergic Uptake Inhibitors (adverse effects, therapeutic use) *Atomoxetine Hydrochloride. *Attention Deficit Disorder with ... clinical responses to the selective norepinephrine reuptake inhibitor atomoxetine (ATX) vary. We sought to determine in ...

http://www.curehunter.com/public/pubmed17588810.do

Many of the ADRENERGIC UPTAKE INHIBITORS also inhibit serotonin uptake; they are not included here. ... Serotonin Uptake Inhibitors. Compounds that specifically inhibit the reuptake of serotonin in the brain. This increases the ... An MAO inhibitor that is effective in the treatment of major depression, dysthymic disorder, and atypical depression. It also ... This monoamine oxidase inhibitor is effective in the treatment of major depression, dysthymic disorder, and atypical depression ...

https://www.bioportfolio.com/resources/trial/120246/Evaluation-of-Substance-P-Neurotransmission-in-Panic-Disorder-by-PET-Imaging-of.html

Final publication URL Indexing Status Subject indexing assigned by CRD MeSH Adrenergic Uptake Inhibitors; Adult; Attention ... The KCNH3 inhibitor ASP2905 shows potential in the treatment of attention deficit/hyperactivity disorder. N-(4-fluorophenyl)-N ... The KCNH3 inhibitor ASP2905 shows potential in the treatment of attention deficit/hyperactivity disorder. Full Text available ... phenyl-N"-(pyrimidin-2-ylmethyl)-1,3,5-triazine-2,4,6-triamine [ASP2905] is a potent and selective inhibitor of the potassium ...

https://www.tripdatabase.com/search?criteria=adhd+Methylphenidate&lang=en&page=5

Most of the ADRENERGIC UPTAKE INHIBITORS also inhibit dopamine uptake. MeSH. Drug Carriers (4) • Forms to which substances are ... DNA Gyrase Inhibitors (0) see Topoisomerase II Inhibitors. DNA Polymerase Inhibitors (0) see Nucleic Acid Synthesis Inhibitors ... Dopamine Uptake Inhibitors (22) • Drugs that block the transport of DOPAMINE into axon terminals or into storage vesicles ... DOPA Decarboxylase Inhibitors (0) see Aromatic Amino Acid Decarboxylase Inhibitors. Dopamine Agents (151) • Any drugs that are ...

https://druginfo.nlm.nih.gov/drugportal/drug/categories/d

Napamezole, an alpha-2 adrenergic receptor antagonist and monoamine uptake inhibitor in vitro. M H Perrone, L T Hamel, R A ... In vivo assessment of napamezole, an alpha-2 adrenoceptor antagonist and monoamine re-uptake inhibitor. M H Perrone, D ... Prostaglandin synthesis elicited by adrenergic stimuli in rabbit aorta is mediated via alpha-1 and alpha-2 adrenergic receptors ... Effect of a new Ca2(+)-calmodulin-dependent protein kinase II inhibitor on GABA release in cerebrospinal fluid of the rat. N ...

http://jpet.aspetjournals.org/content/254/2

Adolescent, Adrenergic Uptake Inhibitors/*therapeutic use, Child, Child; Preschool, Drug Resistance, Enuresis/*drug therapy, ...

http://uu.diva-portal.org/smash/record.jsf?pid=diva2:94769

Norepinephrine-Reuptake Inhibitors, Antidepressants, Adrenergic Uptake Inhibitors, Antidepressive Agents, Tricyclic. CAS number ... Alpha-1A adrenergic receptor. This alpha-adrenergic receptor mediates its action by association with G proteins that activate a ... inhibitor. References:. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M ... inhibitor. References:. Roubert C, Cox PJ, Bruss M, Hamon M, Bonisch H, Giros B: Determination of residues in the ...

http://www.nextbio.com/b/search/details/Nortriptyline?type=compound

A propylamine derivative and selective ADRENERGIC UPTAKE INHIBITOR that is used in the treatment of ATTENTION DEFICIT ... A methylphenidate derivative, DOPAMINE UPTAKE INHIBITOR and CENTRAL NERVOUS SYSTEM STIMULANT that is used in the treatment of ... A dextroamphetamine drug precursor that also functions as a CENTRAL NERVOUS SYSTEM STIMULANT and DOPAMINE UPTAKE INHIBITOR and ...

https://www.bioportfolio.com/resources/trial/68365/OROS-Methylphenidate-Concerta-Adolescents-Study-in-Korea.html

A adrenergic uptake inhibitor is a drug which blocks the reuptake of adrenergic neurotransmitters. ... Rescinnamine is an ... centrally acting/antiadrenergics: Clonidine • Guanfacine • Methyldopa • Moxonidine • Rilmenidine • adrenergic uptake inhibitor ... Alpha blockers (also called alpha-adrenergic blocking agents) constitute a variety of drugs which block Î±1-adrenergic ... An adrenergic is a drug, or other substance, which has effects similar to, or the same as, epinephrine (adrenaline). ... ...

http://www.statemaster.com/encyclopedia/Furosemide

Norepinephrine reuptake inhibitor,N RI]] / [[adrenergic uptake inhibitor,A RI]] , list2 = [[Atomoxetine]] • [[Maprotiline ... Neurotransmitter uptake inhibitor,RI]]s , list2 = {{Navbox subgroup , group1 = [[Serotonin uptake inhibitor,S RI]] , list1 = [[ ... Adrenergic antagonist,AA]]s , list4 = [[Tetracyclic antidepressant,Tetra]]s ([[Mianserin]], [[Mirtazapine]]) }} Templates ... Reversible inhibitor of monoamine oxidase A,RIMAs]]: Befloxatone • [[Brofaromine]] • Cimoxatone • [[Beta-carboline]]s ([[ ...

https://www.wikidoc.org/index.php?title=Template:Antidepressants&action=edit

... evidence using monoamine selective uptake inhibitors and release enhancers. Psychopharmacology (Berl), 1993. 113(1): p. 76-82. ... Mignot, E., et al., Canine cataplexy is preferentially controlled by adrenergic mechanisms: ... Cataplexy is treated with antidepressants such as tricyclics and serotonin reuptake inhibitors that enhance monoaminergic ... Serotonin reuptake inhibitors (SSRIs) have fewer side effects compared to the tricyclics and can be used in adults and children ...

http://www.scholarpedia.org/article/Cataplexy

However, with the addition of alpha-adrenergic receptor inhibitors, oxygen uptake decreased to values similar to those values ... metabolism and to compare these effects with the effects of other adrenergic agents in the presence of adrenergic inhibitors. ... diphosphate-induced mitochondrial oxygen uptake and in vitro myocardial tissue oxygen uptake, probably by modifying the ... The oxygen uptake was determined polarographically with a Clark-type electrode and enzymatic activities were assayed by ...

https://www.conicet.gov.ar/new_scp/detalle.php?keywords=&id=20966%E2%88%A9itulosyes%E2%88%A9itulosyes&articulos=yes&detalles=yes&art_id=2648435

Adrenergic Uptake Inhibitors; Androstadienes; Atropine; Cell Line, Tumor; Enzyme Inhibitors; Estrenes; Fluoxetine; Humans; ... phospholipase C inhibitor; serotonin receptor; serotonin uptake inhibitor; tritium; wortmannin; 1 (6 ((3 methoxyestra 1,3,5(10 ... adrenergic receptor affecting agent; androstane derivative; diagnostic agent; enzyme inhibitor; estrane derivative; ... Total [3H]-mI uptake into cells was measured, as well as specific receptor binding to determine receptor binding after the ...

https://scholar.sun.ac.za/handle/10019.1/11468?show=full

Adrenergic Uptake Inhibitors. dc.subject. Animals. dc.subject. Anti-Anxiety Agents. dc.subject. Anticonvulsants. ...

http://scholar.sun.ac.za/handle/10019.1/11460?show=full

... improvement in autistic behaviors provides a basis for the use of α-adrenergic agonists and α-adrenergic re-uptake inhibitors ...

https://scienceblogs.com/comment/1351454

It is believed that nortriptyline either inhibits the reuptake of the neurotransmitter serotonin at the neuronal membrane or acts at beta-adrenergic receptors. (nextbio.com)
myo-Inositol (mI) is a key metabolic precursor to the phospoinositide (PI) metabolic pathway as a key component of central G-protein coupled receptor signaling systems, including several subtypes of adrenergic, cholinergic, serotonergic and metabotropic glutamatergic receptors. (sun.ac.za)
In considering the cellular or organ-level responses to endogenous or exogenous adrenergic agents, both the number of adrenergic receptors present and the particular receptor subtype are important factors. (pharmacology2000.com)
For example, the adrenergic receptor subtype associated with bronchiolar smooth muscle is principally β 2 and, in accord with the activity of isoproterenol (Isuprel) at β 2 receptors bronchodilation is the likely consequence of isoproterenol administration. (pharmacology2000.com)
The net effect may be vasodilation (β 2 -receptor-mediated) since the β 2 adrenergic receptors are activated at lower catecholamine concentrations. (pharmacology2000.com)
Terbutaline (Brethine™) is an example among beta-receptors as this agent shows relatively high specificity for the β 2 -adrenergic receptor. (pharmacology2000.com)
An agent that binds to but does not activate alpha -adrenergic receptors thereby blocking the actions of endogenous or exogenous alpha -adrenergic agonists. (ebi.ac.uk)
Methylphenidate and atomoxetine enhance prefrontal function through α2-adrenergic and dopamine D1 receptors. (nih.gov)
We investigated norepinephrine (NE), dopamine (DA), and serotonin (5-HT) uptake inhibition using human embryonic kidney 293 (HEK 293) cells that express the respective human monoamine transporter, the drug-induced efflux of NE, DA, and 5-HT from monoamine-preloaded cells, and binding affinity to monoamine transporters and receptors. (nih.gov)
Mechanistically, we provide evidence that β 3 -adrenergic receptors, which are preferentially expressed on a Hes5-expressing precursor population in the subgranular zone (SGZ), mediate this norepinephrine-dependent activation. (jneurosci.org)
Finally, using a novel ex vivo "slice-sphere" assay that maintains an intact neurogenic niche, we demonstrate that antidepressants that selectively block the reuptake of norepinephrine, but not serotonin, robustly increase hippocampal precursor activity via β-adrenergic receptors. (jneurosci.org)
These findings suggest that the activation of neurogenic precursors and stem cells via β 3 -adrenergic receptors could be a potent mechanism to increase neuronal production, providing a putative target for the development of novel antidepressants. (jneurosci.org)
Adrenergic responses were mediated by alpha 1- receptors localized to astrocytes because PE and NE increased [Ca2+]i of acutely isolated hippocampal astrocytes. (jneurosci.org)
Levomilnacipran does not bind to any other receptors, ion channels, or transporters, including serotonergic (5HT1-7), α- and β adrenergic, muscarinic, or histaminergic receptors and Ca2+, Na+, K+ or Cl- channels to a significant degree. (drugbank.ca)
Like corynanthine , it acts as a α 1 -adrenergic receptor antagonist with preferential actions over α 2 -adrenergic receptors , underlying its hypotensive rather than hypertensive effects. (thefullwiki.org)
Note that many TCAs , TeCAs , antipsychotics , and ergolines , and some piperazines like buspirone , trazodone , nefazodone and etoperidone all antagonize α 1 -adrenergic receptors as well, which contributes to their side effects such as orthostatic hypotension . (thefullwiki.org)
Note that many atypical antipsychotics and azapirones like buspirone and gepirone (via metabolite 1-PP ) antagonize α 2 -adrenergic receptors as well. (thefullwiki.org)
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)
Alternative methods have been considered (MAO activity of platelets, platelet density of a2-adrenergic receptors, growth hormone release in response to clonidine), but results are still contaminated by noradrenergic activity at the periphery. (barnardhealth.us)
Indeed, in animal studies, down-regulation of bl-adrenergic receptors only appears following 10-20 days of chronic treatment, a delay that corresponds to clinical observations. (barnardhealth.us)
Not all antidepressants, however, induce desensitization of b-adrenergic receptors. (barnardhealth.us)
Beta blockers block the action of endogenous catecholamines epinephrine (adrenaline) and norepinephrine (noradrenaline) on adrenergic beta receptors , of the sympathetic nervous system , which mediates the fight-or-flight response . (netlibrary.net)
[4] [5] Some block all activation of β-adrenergic receptors and others are selective. (netlibrary.net)
[6] β 1 -adrenergic receptors are located mainly in the heart and in the kidneys. (netlibrary.net)
[5] β 2 -adrenergic receptors are located mainly in the lungs, gastrointestinal tract, liver, uterus, vascular smooth muscle, and skeletal muscle. (netlibrary.net)
[5] β 3 -adrenergic receptors are located in fat cells. (netlibrary.net)
These agents also commonly have action at α- adrenergic receptors and/or 5-HT receptors . (wikidoc.org)
Adrenergic receptors (ARs) particularly 1AR and 2AR will be the prominent receptor subtypes from GPCR family members and have supplied first convincing proof to get GPCRs dimerization [7-13]. (saracatinib.info)
These research additional support our idea and are persuasive evidences to forecast the functional connection between adrenergic and somatostatin receptors inside a receptor particular manner. (saracatinib.info)
An adrenergic agonist is a drug that stimulates a response from the adrenergic receptors. (wikipedia.org)
The five main categories of adrenergic receptors are: α1, α2, β1, β2, and β3, although there are more subtypes, and agonists vary in specificity between these receptors, and may be classified respectively. (wikipedia.org)
Alternatively, it may refer to something which is susceptible to epinephrine, or similar substances, such as a biological receptor (specifically, the adrenergic receptors). (wikipedia.org)
Directly acting adrenergic agonists act on adrenergic receptors. (wikipedia.org)
All adrenergic receptors are G-protein coupled, activating signal transduction pathways. (wikipedia.org)
The receptors are classed physiologically, though pharmacological selectivity for receptor subtypes exists and is important in the clinical application of adrenergic agonists (and, indeed, antagonists). (wikipedia.org)
Inhibitors of these enzymes act as indirect agonists of adrenergic receptors as they prolong the action of catecholamines at the receptors. (wikipedia.org)
A great number of drugs are available which can affect adrenergic receptors. (wikipedia.org)
The following headings provide some useful examples to illustrate the various ways in which drugs can enhance the effects of adrenergic receptors. (wikipedia.org)
These drugs act directly on one or more adrenergic receptors. (wikipedia.org)
these are: Adrenaline (almost all adrenergic receptors). (wikipedia.org)

Napamezole, an alpha-2 adrenergic receptor antagonist and monoamine uptake inhibitor in vitro. (aspetjournals.org)
However, with the addition of alpha-adrenergic receptor inhibitors, oxygen uptake decreased to values similar to those values obtained with isoproterenol. (conicet.gov.ar)
Total [3H]-mI uptake into cells was measured, as well as specific receptor binding to determine receptor binding after the pretreatments. (sun.ac.za)
Some agents exhibit much higher affinities for particular receptor subtype, so much so that they are defined as almost exclusively associated with that adrenergic subtype. (pharmacology2000.com)
Moreover, intrahippocampal injection of a selective β 3 -adrenergic receptor agonist in vivo increases the number of proliferating cells in the SGZ. (jneurosci.org)
Similarly, systemic injection of the β-adrenergic receptor agonist isoproterenol not only results in enhancement of proliferation in the SGZ but also leads to an increase in the percentage of nestin/glial fibrillary acidic protein double-positive neural precursors in vivo . (jneurosci.org)
Among the most important and most widely used medications are thiazide diuretics , calcium channel blockers , ACE inhibitors , angiotensin II receptor antagonists (ARBs), and beta blockers . (rug.nl)
In the United States, the JNC8 (Eighth Joint National Committee on the Prevention, Detection, Evaluation, and Treatment of High Blood Pressure) recommends thiazide-type diuretics to be one of the first-line drug treatments for hypertension, either as monotherapy or in combination with calcium channel blockers , ACE inhibitors , or angiotensin II receptor antagonists . (rug.nl)
The 8th Joint National Committee (JNC-8) recommends calcium channel blockers to be a first-line treatment either as monotherapy or in combination with thiazide -type diuretics, ACE inhibitors , or angiotensin II receptor antagonists for all patients regardless of age or race. (rug.nl)
However, ACE inhibitors (and angiotensin II receptor antagonists) should not be a first-line treatment for black hypertensives without chronic kidney disease . (rug.nl)
clonidine is an adrenergic agonist on the α2 receptor , since this receptor is located presynaptically to inhibit further release of adrenaline and noradrenaline. (wikidoc.org)
Since the demonstration that most antidepressants decrease b1-adrenergic receptor transduction in the cerebral cortex of the rat, this parameter has generally been considered as a biochemical correlate of therapeutic activity. (barnardhealth.us)
A reactivation of serotonin transmission, which can be obtained by some antidepressants such as SSRIs (specific serotonin re-uptake inhibitors), can hamper the development of b-adrenergic receptor desensitization even when noradrenergic transmission is also reactivated. (barnardhealth.us)
Beta blockers (β-blockers, beta-adrenergic blocking agents, beta antagonists, beta-adrenergic antagonists, beta-adrenoreceptor antagonists, or beta adrenergic receptor antagonists ) are a class of drugs that are particularly used for the management of cardiac arrhythmias , protecting the heart from a second heart attack ( myocardial infarction ) after a first heart attack (secondary prevention), [1] and, in certain cases, hypertension . (netlibrary.net)
Background In today's research, we describe heterodimerization between human-Somatostatin Receptor 5 (hSSTR5) and 2-Adrenergic Receptor (2AR) and its own effect on the receptor trafficking, coupling to adenylyl cyclase and signaling including mitogen activated protein kinases and calcineurin-NFAT pathways. (saracatinib.info)

There has been success when tic symptoms are co-morbid with ADHD, and as such, guanfacine and other alpha-2-adrenergic agonists ( clonidine ) are commonly the first choice for treatment. (thefullwiki.org)
In rats, McN-5652 did not induce the stereotyped behavior often caused by dopamine agonists and inhibitors of dopamine uptake. (aspetjournals.org)
Indirectly acting adrenergic agonists affect the uptake and storage mechanisms involved in adrenergic signalling. (wikipedia.org)

Maprotiline is a strong inhibitor of noradrenaline re-uptake in the brain and peripheral tissues, however it is worthy to note that it is a weak inhibitor of serotonergic uptake. (pharmacycode.com)
To assess the benefits and harms of serotonin and noradrenaline reuptake inhibitors (SNRIs) compared with placebo for treating FMS symptoms in adults. (nih.gov)
Drug therapy, for example, with serotonin and noradrenaline reuptake inhibitors (SNRIs), focuses on reducing key symptoms and improving quality of life. (unboundmedicine.com)
To assess the efficacy, tolerability and safety of serotonin and noradrenaline reuptake inhibitors (SNRIs) compared with placebo or other active drug(s) in the treatment of fibromyalgia in adults. (unboundmedicine.com)
The present study investigates the effect of combination of the antidepressant venlafaxine (serotonin/noradrenaline reuptake inhibitor, SNRI) with the angiotensin converting enzyme inhibitor perindopril on the immobility time in the forced swimming test (FST) as well as on systolic blood pressure (SBP) in uninephroctemized DOCA salt-treated rats as a model of experimental hypertension. (ispub.com)
Additionally, development of hypertension is one of the known complications of venlafaxine which is a serotonin/noradrenaline reuptake inhibitor, SNRI. (ispub.com)
In the present study, we manipulate noradrenergic activity during sleep in humans with either the α2-autoreceptor agonist clonidine or the noradrenaline reuptake inhibitor reboxetine. (ox.ac.uk)
viagra reflux Serotonin Noradrenaline Reuptake Inhibitors SNRIs Ipek Komsuoglu Celikyurt. (viagrarx.fr)

alpha -Adrenergic antagonists are used in the treatment of hypertension, vasospasm, peripheral vascular disease, shock, and pheochromocytoma. (ebi.ac.uk)

Levomilnacipran is a serotonin and norepinephrine reuptake inhibitor and is indicated for the treatment of major depressive disorder (MDD). (drugbank.ca)
Levomilnacipran is a selective serotonin and norepinephrine reuptake inhibitor. (drugbank.ca)
It belongs to a class of drugs a selective norepinephrine reuptake inhibitor. (globalgenericpharmacy.com)
MECHANISM OF ACTION - Duloxetine is a selective serotonin and norepinephrine reuptake inhibitor SNRI. (viagrarx.fr)
a serotonin norepinephrine reuptake inhibitor (SNRI), is the first drug that is widely approved in Europe for treatment of stress urinary incontinence (SUI) in women. (viagrarx.fr)
In 1993, a new drug was introduced to the US market called venlafaxine, a serotonin-norepinephrine reuptake inhibitor. (wikipedia.org)

This action could be counteracted by alpha-adrenergic agonist effects. (conicet.gov.ar)

The tricyclic antidepressants (ANTIDEPRESSIVE AGENTS, TRICYCLIC) and amphetamines are among the therapeutically important drugs that may act via inhibition of adrenergic transport. (drugbank.ca)

Finally, the therapeutic efficacy of tricyclic drugs or monoamine oxidase inhibitors, usually considered as antidepressants , may result from their actions on the noradrenergic system. (barnardhealth.us)

Most of the ADRENERGIC UPTAKE INHIBITORS also inhibit dopamine uptake. (nih.gov)
ACE inhibitors inhibit the activity of angiotensin-converting enzyme (ACE), an enzyme responsible for the conversion of angiotensin I into angiotensin II, a potent vasoconstrictor . (rug.nl)
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)

RG 12915: a potent 5-hydroxytryptamine-3 antagonist that is an orally effective inhibitor of cytotoxic drug-induced emesis in the ferret and dog. (aspetjournals.org)
Panic attacks are induced by yohimbine, an a2-adrenergic antagonist that increases LC firing, in approximately 60-70% of patients with panic disorders. (barnardhealth.us)

The exact mechanism of action is not well understood, however it is generally thought that tricyclic antidepressants work by inhibiting the re-uptake of the neurotransmitters norepinephrine , dopamine , or serotonin by nerve cells . (bionity.com)
SNRIs, along with SSRIs and norepinephrine reuptake inhibitors (NRIs), are second-generation antidepressants. (wikipedia.org)
Over the past two decades, second-generation antidepressants have simply replaced first-generation antidepressants, such as tricyclic antidepressants (TCAs) and monoamine oxidase inhibitors (MAOIs), as the drugs of choice for the treatment of MDD due to their improved tolerability and safety profile. (wikipedia.org)

Atomoxetine is a specific, noradrenergic reuptake inhibitor that provides an effective treatment option for patients with ADHD and co -morbid conditions. (curehunter.com)
While fluoxetine also reduced 5HT2A-R function, but to a lesser degree, imipramine increased 5HT2A-R function, which may explain why mI seems to be effective exclusively in selective serotonin reuptake inhibitor-sensitive disorders. (sun.ac.za)
A new drug, solriamfetol, a selective norepinephrine-dopamine reuptake inhibitor, is the first drug of its class that is being considered by the US Food and Drug Administration (FDA) to treat excessive sleepiness in OSA and narcolepsy patients. (stanford.edu)
The unique mechanism of action of venlafaxine is to be a selective reuptake inhibitor of norepinephrine besides blockade of serotonin uptake ( Szot et al . (ispub.com)

Atomoxetine acts as norepinephrine Uptake Inhibitor. (globalgenericpharmacy.com)

[9] Low-dose thiazides are more effective at treating hypertension than beta blockers and are similar to angiotensin-converting enzyme (ACE) inhibitors . (bingj.com)
A review of literature demonstrated important data concerning psychotropic effects of angiotensin converting enzyme inhibitors [ACEIs]. (ispub.com)
Patients develop unsteady gait, which may lead to hypotension, angiotensin converting enzyme ace inhibitor, and immunosuppressive condition predisposes to the right ventricle is the most frequently arising from repetitive motion. (medpsychmd.com)

Other sources suggest that most of the tricyclics combine adrenergic and serotonergic effects to some degree. (bionity.com)

All of the cathinones were potent NE uptake inhibitors but differed in their DA vs. 5-HT transporter inhibition profiles and monoamine release effects. (nih.gov)
the mechanism of its reinforcing effects is thought to involve inhibition of dopamine uptake. (bireme.br)

Serotonin-norepinephrine reuptake inhibitors (SNRIs) are a class of antidepressant drugs that treat major depressive disorder (MDD), anxiety disorders, obsessive-compulsive disorder (OCD), social phobia, attention-deficit hyperactivity disorder (ADHD), chronic neuropathic pain, fibromyalgia syndrome (FMS), and menopausal symptoms. (wikipedia.org)
SNRIs can be contrasted with the more widely used selective serotonin reuptake inhibitors (SSRIs), which act upon serotonin only. (wikipedia.org)

Hepatic portal venous delivery of a nitric oxide synthase inhibitor enhances net hepatic glucose uptake. (semanticscholar.org)
1999). On the other hand, the vasoprotective effect of perindopril might be explained on the basis that the RAS plays an important role in the elevation of asymmetric dimethylarginine (ADMA), an endogenous inhibitor of nitric oxide synthase and this can be effectively reversed upon perindopril treatment ( Ito et al . (ispub.com)

To investigate the possible role of altered autonomic nervous activity in the effect of portal glucose delivery, the effects of adrenergic blockade and acetylcholine (ACh) on hepatic glucose metabolism were examined in 42-h-fasted conscious dogs. (semanticscholar.org)

Drugs that block the transport of adrenergic transmitters into axon terminals or into storage vesicles within terminals. (drugbank.ca)
[7] There are fixed-dose combination drugs , such as ACE inhibitor and thiazide combinations . (rug.nl)
A systematic review of 63 trials with over 35,000 participants indicated ACE inhibitors significantly reduced doubling of serum creatinine levels compared to other drugs (ARBs, α blockers, β blockers, etc.), and the authors suggested this as a first line of defense. (rug.nl)
On the basis of encouraging clinical as well as experimental data, the development of highly selective COX-2 inhibitors appears to be a sound strategy to develop a new generation of anti-inflammatory drugs. (justia.com)
Other drugs affect the uptake and storage mechanisms of adrenergic catecholamines, prolonging their action. (wikipedia.org)
For this reason, this class of drugs became known as monoamine oxidase inhibitors, or MAOIs. (wikipedia.org)

Two uptake mechanisms exist for terminating the action of adrenergic catecholamines - uptake 1 and uptake 2. (wikipedia.org)

It also plays a role of an adrenergic uptake inhibitor, an antidepressant, a xenobiotic, and an environmental contaminant. (globalgenericpharmacy.com)

CONCLUSIONS: The data suggest that while isoproterenol increases "in vivo" oxygen uptake by the working rat heart, isoproterenol can simultaneously decrease maximal adenosine 5'-diphosphate-induced mitochondrial oxygen uptake and in vitro myocardial tissue oxygen uptake, probably by modifying the mitochondrial respiratory enzymes. (conicet.gov.ar)
The regulation of net hepatic glucose uptake in vivo. (semanticscholar.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)
The high potency of McN-5652 as a serotonin uptake inhibitor in vivo is indicated further by the low doses required to potentiate L-5-hydroxytryptophan-induced head twitches in mice (ED50 = 0.4 mg/kg 2 hr after p.o. dosing) and the serotonin syndrome in rats (ED50 = 1.5 mg/kg 2 hr after p.o. dosing). (aspetjournals.org)

Methedrone was a more potent 5-HT than DA transporter inhibitor and released NE and 5-HT similar to para-methoxymethamphetamine (PMMA), para-methoxyamphetamine (PMA), 4-methylthioamphetamine (4-MTA), and 3,4-methylenedioxymethamphetamine (MDMA). (nih.gov)
McN-5652: a highly potent inhibitor of serotonin uptake. (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)
Duloxetine is also considered a less potent inhibitor of dopamine re-uptake. (viagrarx.fr)

[11] The AASK trial showed that ACE inhibitors are more effective at slowing down the decline of kidney function compared to calcium channel blockers and beta blockers . (rug.nl)
[10] Low-dose thiazides are tolerated as well as the other classes of diuretics, including ACE inhibitors , beta blockers and calcium channel blockers . (bingj.com)

Our objective was to test an additional primary action of isoproterenol on tissue and mitochondrial oxidative metabolism and to compare these effects with the effects of other adrenergic agents in the presence of adrenergic inhibitors. (conicet.gov.ar)
Isoproterenol (0.01 to 100 nM) decreased the oxygen uptake by the heart slices in a dose-dependent manner. (conicet.gov.ar)

[5] Although clinical evidence shows calcium channel blockers and thiazide-type diuretics are preferred first-line treatments for most people (from both efficacy and cost points of view), an ACE inhibitor is recommended by NICE in the UK for those under 55 years old. (rug.nl)
[7] Results from the ALLHAT trial showed that thiazide -type diuretics and calcium channel blockers were both more effective as monotherapy in improving cardiovascular outcomes compared to ACE inhibitors for this subgroup. (rug.nl)

Duloxetine has no significant affinity for adrenergic, cholinergic, histaminergic. (viagrarx.fr)

Amphetamine has multiple mechanisms of action including blocking uptake of adrenergics and dopamine, stimulation of release of monamines, and inhibiting monoamine oxidase. (nih.gov)
Monoamine oxidase inhibitors allopurinola mg po daily, days carboplatin auc = iv infused over minutes plus administration o ampule o d. (medpsychmd.com)

[13] However, the UK National Institute for Health and Clinical Excellence recommends ACE inhibitor and calcium channel blockers for first-line treatment of hypertension in adults (CG127). (bingj.com)

Anatomy1

Organisms1

Chemicals and Drugs50

Analytical, Diagnostic and Therapeutic Techniques and Equipment1

Psychiatry and Psychology1

Phenomena and Processes3

Fas/CD95/Apo-I activates the acidic sphingomyelinase via caspases. (1/489)

Effects of imipramine, an uptake inhibitor, on double-peaked constrictor responses to periarterial nerve stimulation in isolated, perfused canine splenic arteries. (2/489)

Transmembrane domain I contributes to the permeation pathway for serotonin and ions in the serotonin transporter. (3/489)

Diurnal variation in 5-HT1B autoreceptor function in the anterior hypothalamus in vivo: effect of chronic antidepressant drug treatment. (4/489)

Endothelium is required in the vascular spasm induced by tetraethylammonium and endothelin-1 in guinea-pig aorta. (5/489)

Neuronal uptake affects dynamic characteristics of heart rate response to sympathetic stimulation. (6/489)

Decrease in hepatic CYP2C11 mRNA and increase in heme oxygenase activity after intracerebroventricular injection of bacterial endotoxin. (7/489)

Activities of trovafloxacin compared with those of other fluoroquinolones against purified topoisomerases and gyrA and grlA mutants of Staphylococcus aureus. (8/489)

Adrenergic Uptake Inhibitors

Neurotransmitter Uptake Inhibitors

Dopamine Uptake Inhibitors

Benztropine

GABA Uptake Inhibitors

Nomifensine

Zimeldine

Nipecotic Acids

Serotonin Uptake Inhibitors

Desipramine

Serotonin

Cocaine

Clomipramine

Dopamine Plasma Membrane Transport Proteins

Serotonin Antagonists

Tropanes

Mazindol

Dopamine

Protriptyline

Metergoline

Pargyline

Fenfluramine

Quipazine

Amphetamines

Biogenic Monoamines

Fluvoxamine

Paroxetine

Dicarboxylic Acids

Fluoxetine

Dose-Response Relationship, Drug

Imipramine

Norepinephrine Plasma Membrane Transport Proteins

Membrane Transport Proteins

Norepinephrine

Rats, Sprague-Dawley

Biological Transport

Citalopram

Piperazines

Serotonin Plasma Membrane Transport Proteins

Dipyridamole

N-Methyl-3,4-methylenedioxyamphetamine

Adenosine

Microdialysis

Receptors, Serotonin

2-Chloroadenosine

Monoamine Oxidase Inhibitors

Tyramine

Drug Interactions

Synaptosomes

Endocannabinoids

Cannabinoid Receptor Modulators

Behavior, Animal

Polyunsaturated Alkamides

Pyrrolidines

gamma-Aminobutyric Acid

Xanthines

Methamphetamine

Fas/CD95/Apo-I activates the acidic sphingomyelinase via caspases. (1/489)

Effects of imipramine, an uptake inhibitor, on double-peaked constrictor responses to periarterial nerve stimulation in isolated, perfused canine splenic arteries. (2/489)

Transmembrane domain I contributes to the permeation pathway for serotonin and ions in the serotonin transporter. (3/489)

Diurnal variation in 5-HT1B autoreceptor function in the anterior hypothalamus in vivo: effect of chronic antidepressant drug treatment. (4/489)

Endothelium is required in the vascular spasm induced by tetraethylammonium and endothelin-1 in guinea-pig aorta. (5/489)

Neuronal uptake affects dynamic characteristics of heart rate response to sympathetic stimulation. (6/489)

Decrease in hepatic CYP2C11 mRNA and increase in heme oxygenase activity after intracerebroventricular injection of bacterial endotoxin. (7/489)

Activities of trovafloxacin compared with those of other fluoroquinolones against purified topoisomerases and gyrA and grlA mutants of Staphylococcus aureus. (8/489)

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