AntagonistTransporterSelective serotoninReuptake inhibitorProtein-coupled receptorsAntagonismInhibits serotoninAgonistOrthostatic hypotensionBenzodiazepineAnticholinergic effects5HT2AAdrenergic receptorHeparinTransportersQuetiapineSynapticSymptomsNoradrenalineSSRIsMesolimbicAntagonistsPathwaysMechanismEpinephrineClinicalZiprasidoneCompoundHighStimulationDegranulationMast cellHormonePotentBrainActivityApparentlyRoleBlocksInteraction
Antagonist14
- It has been described as a serotonin antagonist and reuptake inhibitor (SARI) due to its combined actions as a potent antagonist of the serotonin 5-HT2A and 5-HT2C receptors and weak serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI). (wikipedia.org)
- Nefazodone acts primarily as a potent antagonist of the serotonin 5-HT2A receptor and to a lesser extent of the serotonin 5-HT2C receptor. (wikipedia.org)
- It has low but potentially significant affinity for the histamine H1 receptor, where it is an antagonist, and hence may have some antihistamine activity. (wikipedia.org)
- Ziprasidone is a selective monoaminergic antagonist with high affinity for the serotonin Type 2 (5HT2), dopamine Type 2 (D2), 1 and 2 adrenergic, and H1 histaminergic receptors. (lgmpharma.com)
- Ziprasidone acts as an antagonist at other receptors, but with lower potency. (lgmpharma.com)
- Ziprasidone functions as an antagonist at the Dopamine D2 , 5HT-2A , and 5HT-1D receptors, and as an agonist at the 5HT-1A receptor. (lgmpharma.com)
- Alfuzosin hydrochloride is an α1 adrenergic receptor antagonist. (targetmol.com)
- Rezatomidine is a selective antagonist of α2-adrenergic receptor and can be used in studies about chronic pain, including neuropathic pain. (targetmol.com)
- Perphenazine is a phenothiazine derivative and a dopamine antagonist with antiemetic and antipsychotic properties. (targetmol.com)
- Doxepin has a high affinity for the H1 receptor, making it a selective H1 antagonist at low dose and it has been shown to display sedating properties. (studylib.net)
- Doxepin HCl, a tricyclic antidepressant, is antagonist of histamine H1 Receptor (Kd = 310 pM) and histamine H4 receptor (pKi = 6.79). (csnpharm.cn)
- Quetiapine is an antagonist at serotonin 5-HT 1A and 5HT 2 , dopamine D1 and D2, histamine H1, and adrenergic alpha 1 and alpha 2 receptors. (illnesshacker.com)
- Quetiapine is an antagonist for 5-HT 2B , but only dexmethylphenidate is known to have any affect on 5-HT 2B , and even then it doesn't appear to have a particularly strong binding affinity. (stackexchange.com)
- Quetiapine is an α 2A antagonist, so that's a secondary mechanism by which quetiapine would affect norepinephrine levels. (stackexchange.com)
Transporter4
- Centanafadine hydrochloride is a dual inhibitor of norepinephrine (NE)/dopamine (DA) transporter, also inhibits serotonin transporter (IC50s: 6 nM, 38 nM, and 83. (targetmol.com)
- Fluoxetine HCl, an antidepressant, is an inhibitor of the selective serotonin reuptake with Kd of 0.81 nM against serotonin transporter. (csnpharm.cn)
- Desvenlafaxine succinate is a serotonin (5-HT) transporter and norepinephrine (NE) transporter reuptake inhibitor with Ki of 40.2 nM and 558.4 nM respectively. (csnpharm.cn)
- This left me with the most likely interaction: methylphenidate is an NDRI, so it fairly strongly blocks the norepinephrine transporter (NET), and norquetiapine also has a strong blocking effect on NET. (stackexchange.com)
Selective serotonin9
- Lexapro (escitalopram) is type of antidepressant called a selective serotonin reuptake inhibitor ( SSRI ) used to treat anxiety in adults and major depressive disorder in adults and adolescents who are at least 12 years old. (rxlist.com)
- DESCRIPTIONCitalopram hydrobromide is an orally administered selective serotonin reuptake inhibitor (SSRI) with a chemical structure unrelated to that of other SSRIs or of tricyclic, tetracyclic, or other available antidepressant agents. (medlibrary.org)
- In vitro and in vivo studies in animals suggest that citalopram is a highly selective serotonin reuptake inhibitor (SSRI) with minimal effects on norepinephrine (NE) and dopamine (DA) neuronal reuptake. (medlibrary.org)
- Sertraline HCl is a selective serotonin reuptake inhibitor (SSRI) class and inhibits 5-HT with Ki of 13 nM. (csnpharm.cn)
- Paroxetine HCl is a selective serotonin-reuptake inhibitor (SSRI) with antidepressant activity. (csnpharm.cn)
- Fluvoxketone is an antidepressant of the selective serotonin reuptake inhibitor (SSRI) class. (csnpharm.cn)
- Fluvoxamine maleate is a selective serotonin reuptake inhibitor and can be used as an antidepressant. (csnpharm.cn)
- Fluvoxamine is an antidepressant which functions pharmacologically as a selective serotonin reuptake inhibitor. (csnpharm.cn)
- Escitalopram is a selective serotonin reuptake inhibitor (SSRI) with Ki of 0.89 nM. (csnpharm.cn)
Reuptake inhibitor5
- Nefazodone has low but significant affinity for the serotonin, norepinephrine, and dopamine transporters as well, and therefore acts as a weak serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI). (wikipedia.org)
- Vilazodone is a combined serotonin specific reuptake inhibitor (SSRI) and 5-HT1A receptor partial agonist currently under clinical evaluation for the treatment of major depression. (csnpharm.cn)
- Venlafaxine is an antidepressant of the serotonin-norepinephrine reuptake inhibitor (SNRI) class. (csnpharm.cn)
- Reboxetine Mesylate is a norepinephrine reuptake inhibitor (NRI) used in the treatment of unipolar depression. (csnpharm.cn)
- Milnacipran is a serotonin-norepinephrine reuptake inhibitor (SNRI) used in the clinical treatment of fibromyalgia. (csnpharm.cn)
Protein-coupled receptors2
- The adrenergic receptors or adrenoceptors are a class of G protein-coupled receptors that are targets of many catecholamines like norepinephrine (noradrenaline) and epinephrine (adrenaline) produced by the body, but also many medications like beta blockers, β2 agonists and α2 agonists, which are used to treat high blood pressure and asthma, for example. (targetmol.com)
- G Protein Coupled Receptors (GPCR), nuclear hormone receptors, ion channels, and transporters are all important drug targets. (chempartner.com)
Antagonism9
- Alleviation of positive symptoms is due to antagonism at D2 receptors while relief of negative symptoms are due to 5HT2A antagonism. (lgmpharma.com)
- Antagonism at receptors other than dopamine and 5HT2 with similar receptor affinities may explain some of the other therapeutic and side effects of Ziprasidone. (lgmpharma.com)
- Ziprasidone's antagonism of muscarinic M1-5 receptors may explain its anticholinergic effects. (lgmpharma.com)
- Ziprasidone's antagonism of histamine H1 receptors may explain the somnolence observed with this drug. (lgmpharma.com)
- Ziprasidone's antagonism of adrenergic a1 receptors may explain the orthostatic hypotension observed with this drug. (lgmpharma.com)
- Antagonism of muscarinic, histaminergic, and adrenergic receptors has been hypothesized to be associated with various anticholinergic, sedative, and cardiovascular effects of other psychotropic drugs. (medlibrary.org)
- Antagonism at D2 receptors relieves positive symptoms while antagonism at 5HT2A receptors relieves negative symptoms of schizophrenia. (illnesshacker.com)
- Drowsiness and orthostatic hypotension associated with the use of quetiapine may be explained by its antagonism of histamine H1 and adrenergic alpha 1 receptors, respectively. (illnesshacker.com)
- However, quetiapine does not appear to have any particular binding affinity for β 1 or β 2 , and the description above says antagonism rather than agonism. (stackexchange.com)
Inhibits serotonin1
- 1S-cis)-Milnacipran HCl inhibits serotonin-norepinephrine reuptake and is used for the treatment of fibromyalgia. (csnpharm.cn)
Agonist3
- SynephrineHCl (Oxedrine, p-Synephrine) is an agonist that acts on sympathomimetic α-adrenergic receptor (AR). (targetmol.com)
- ST-91 is an agonist of α2-adrenoceptor with a mixed α-adrenergic receptor type/subtype selection profile. (targetmol.com)
- Rotigotine Hydrochloride, a dopamine receptor agonist prefering for D3 receptors over D1 and D2, has effective activity of anti-Parkinsonian. (targetmol.com)
Orthostatic hypotension1
- Droxidopa is an orally available prodrug of norepinephrine that is used in the treatment of symptomatic orthostatic hypotension due to neurogenic causes of auton. (targetmol.com)
Benzodiazepine2
- MDMA exhibited negligible affinities (greater than 500 microM) at opioid (mu, delta and kappa), central-type benzodiazepine, and corticotropin-releasing factor receptors, and at choline uptake sites and calcium channels. (erowid.org)
- Quetiapine has no significant affinity for cholinergic muscarinic or benzodiazepine receptors. (illnesshacker.com)
Anticholinergic effects1
- Nefazodone has negligible activity at muscarinic acetylcholine receptors, and accordingly, has no anticholinergic effects. (wikipedia.org)
5HT2A1
- Ziprasidone's antipsychotic activity is likely due to a combination of its antagonistic function at D2 receptors in the mesolimbic pathways and at 5HT2A receptors in the frontal cortex. (lgmpharma.com)
Adrenergic receptor4
- It also has high affinity for the α1-adrenergic receptor and serotonin 5-HT1A receptor, and relatively lower affinity for the α2-adrenergic receptor and dopamine D2 receptor. (wikipedia.org)
- Bucindolol Formatel is a blocker of β1-adrenergic receptor. (targetmol.com)
- 5-HT1A modulator 1 displays very high affinities for the 5-HT1A, α1-adrenergic receptor, and D2 receptor (IC50s = 2 nM, 10 nM, and 40 nM). (targetmol.com)
- When norepinephrine acts as a drug it increases blood pressure by increasing vascular tone through α-adrenergic receptor activation. (wikidoc.org)
Heparin1
- These mast cells contain many granules, themselves containing histamine, serotonin and heparin, a naturally occurring anticoagulant. (epiphanyasd.com)
Transporters1
- ChemPartner's in vitro biology team utilizes FLIPR calcium flux, cAMP, reporter genes, and radiometric assays to provide customized assay development and high-throughput screening services to support our clients' drug discovery for receptors, ion channels, and transporters. (chempartner.com)
Quetiapine5
- Quetiapine fumarate antagonizes serotonin activity mediated by 5-HT 1A and 5-HT2 receptors. (illnesshacker.com)
- In addition, quetiapine also binds to other alpha-1, alpha-2 adrenergic and histamine H1 receptors. (illnesshacker.com)
- Quetiapine also has an antagonistic effect on the histamine H1 receptor.It is an atypical antipsychotic used for the treatment of schizophrenia, bipolar disorder, and major depressive disorder. (illnesshacker.com)
- 5-HT 1A seems unlikely to be involved, since methylphenidate has a fairly low binding affinity for it, and quetiapine / norquetiapine are agonists. (stackexchange.com)
- The symptoms of excess norepinephrine mimic that of stress, which can lead to increased blood pressure, but it seems odd to refer to that as '[increasing the] toxicity of methylphenidate' - that phrasing implies that some aspect of methylphenidate is already inherently toxic, and that quetiapine somehow specifically amplifies that. (stackexchange.com)
Synaptic3
- Ziprasidone also inhibits synaptic reuptake of serotonin and norepinephrine. (lgmpharma.com)
- Norepinephrine is synthesized from tyrosine as a precursor, and packed into synaptic vesicles. (wikidoc.org)
- It performs its action by being released into the synaptic cleft, where it acts on adrenergic receptors, followed by the signal termination, either by degradation of norepinephrine, or by uptake by surrounding cells. (wikidoc.org)
Symptoms1
- Histamine, however, is not the only agent to cause symptoms in anaphylaxis. (medscape.com)
Noradrenaline1
- Norepinephrine ( INN ) (abbreviated norepi or NE ) or noradrenaline ( BAN ) (abbreviated NA or NAd ) is a catecholamine with multiple roles including as a hormone and a neurotransmitter . (wikidoc.org)
SSRIs2
- Selective serotonin reuptake inhibitors (SSRIs) are greatly preferred to the other classes of antidepressants in this setting. (medscape.com)
- Paroxetine HCl is an antidepressant agents known as selective serotonin-reuptake inhibitors (SSRIs). (csnpharm.cn)
Mesolimbic1
- With a lower affinity, this agent also reversibly binds to dopamine D1 and D2 receptors in the mesolimbic and mesocortical areas of the brain leading to decreased psychotic effects, such as hallucinations and delusions. (illnesshacker.com)
Antagonists2
- I'm coming at this without a whole lot of background in the topic, but I do understand the basics of binding profiles, dissociation constants, agonists/antagonists, binding affinity, etc., which has at least allowed me to do a bit of preliminary digging. (stackexchange.com)
- This seems like a strong candidate for being the source of concern - they're both antagonists on the same receptor. (stackexchange.com)
Pathways1
- This nucleus is the origin of most norepinephrine pathways in the brain. (wikidoc.org)
Mechanism2
- The mechanism of action of citalopram hydrobromide as an antidepressant 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). (medlibrary.org)
- It has been shown that the mechanism of development of histamine dysphalgia is more sudden than in migraine, since the release of endogenous histamine is present. (geneceutica.ro)
Epinephrine3
- Along with epinephrine , norepinephrine also underlies the fight-or-flight response , directly increasing heart rate , triggering the release of glucose from energy stores, and increasing blood flow to skeletal muscle . (wikidoc.org)
- The term "norepinephrine" is derived from the chemical prefix nor- , which indicates that norepinephrine is the next lower homolog of epinephrine . (wikidoc.org)
- The two structures differ only in that epinephrine has a methyl group attached to its nitrogen, while the methyl group is replaced by a hydrogen atom in norepinephrine. (wikidoc.org)
Clinical2
- Many of the clinical presentations seen in anaphylaxis are due to activation of multiple histamine receptors. (medscape.com)
- This structure explains some of the clinical uses of norepinephrine, since a modification of the system affects large areas of the brain. (wikidoc.org)
Ziprasidone1
- Stahl SM, Shayegan DK: The psychopharmacology of ziprasidone: receptor-binding properties and real-world psychiatric practice. (lgmpharma.com)
Compound1
- This compound also possesses minor anticholinergic activity, through its affinity to muscarinic receptors. (drugcentral.org)
High2
- When the specific antigen, or one similar to it, binds to the high affinity FcεRI-α receptor of the immunoglobulin, mast cell and basophil degranulation occurs. (medscape.com)
- thus you could get low brain serotonin but high blood serotonin. (epiphanyasd.com)
Stimulation2
- The stimulation of the H1 receptor is thought to play an important role in mediating arousal. (studylib.net)
- The combination of H 1 and H 2 receptor stimulation results in increased vascular permeability, flushing, hypotension, tachycardia, and headache. (medscape.com)
Degranulation1
- perhaps a contributing factor is serotonin released by the degranulation of mast cells. (epiphanyasd.com)
Mast cell1
- The most effective therapy is to use mast cell stabilizers , but even a standard OTC H1 antihistamine will provide some relief within 20 minutes. (epiphanyasd.com)
Hormone2
- Besides functioning as an antioxidant and anthelmintic , many isoflavones have been shown to interact with animal and human estrogen receptors , causing effects in the body similar to those caused by the hormone estrogen . (wikipedia.org)
- As a stress hormone , norepinephrine affects parts of the brain where attention and responding actions are controlled. (wikidoc.org)
Potent1
- Pipofezine is a potent inhibitor of the reuptake of serotonin. (csnpharm.cn)
Brain5
- The rank order of affinities of MDMA at various brain receptors and uptake sites are as follows: 5-HT uptake greater than alpha 2-adrenoceptors = 5-HT2 serotonin = M-1 muscarinic = H-1 histamine greater than norepinephrine uptake = M-2 muscarinic = alpha 1-adrenoceptors = beta-adrenoceptors greater than or equal to dopamine uptake = 5-HT1 serotonin much greater than D-2 dopamine greater than D-1 dopamine. (erowid.org)
- If inhibited, it may increase the amount of norepinephrine in the brain. (stackexchange.com)
- We have already seen that there often appears to be central hypo-function of serotonin in autism (i.e. low brain serotonin). (epiphanyasd.com)
- Remember that serotonin does not cross the blood brain barrier. (epiphanyasd.com)
- Norepinephrine can also suppress neuroinflammation when released diffusely in the brain from the locus ceruleus . (wikidoc.org)
Activity1
- bronchial smooth muscle constriction and increased mucus viscosity from H 1 receptor activity and H 2 activity causes increased mucus production. (medscape.com)
Apparently1
- it apparently blocks alpha-adrenergic, histamine H1, and some types of serotonin r. (targetmol.com)
Role2
- The nuclear receptor superfamily is ligand-activated transcription factor, which plays an essential role in cell differentiation, proliferation, and metabolism, and is related to many diseases, such as cardiovascular disease, inflammation, and cancer. (chempartner.com)
- Some of the most popular posts on my blog refer to my investigation into the role of histamine in autism. (epiphanyasd.com)
Blocks1
- Desipramine selectively blocks reuptake of norepinephrine from the neural synapse, and also appears to impair serotonin transport. (drugcentral.org)
Interaction1
- What I suspect the interaction is referring to is that both drugs increase norepinephrine through one or more mechanisms (e.g. by inhibiting reuptake and/or increasing production) leading to a potential scenario where a person who takes both drugs may end up having far too much norepinephrine. (stackexchange.com)