70 Results for "

desensitization

" in MedChemExpress (MCE) Product Catalog:
Products (70)

70 Results for "desensitization" in MCE Product Catalog:

19
19 Publications Verification
Cat. No.: HY-122272
CAS No.: 61869-08-7
Purity:  99.92%
Synonyms: BRL29060
Paroxetine (BRL29060) is an orally active and selective serotonin reuptake inhibitor (SSRI) and apoptosis inducer with blood-brain barrier permeability. Paroxetine inhibits nitric oxide synthase and CYP2D6, induces desensitization of 5-HT1A/1B/1D autoreceptors, downregulates 5-HT2 receptors, and promotes the production of inflammatory cytokines. Paroxetine is a weak norepinephrine (NE) uptake inhibitor and possesses antitumor activity. Paroxetine is widely used in research concerning depression, obsessive-compulsive disorder, panic disorder, social phobia, generalized anxiety disorder, post-traumatic stress disorder, premenstrual dysphoric disorder, hot flashes, and related conditions .
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19
19 Publications Verification
Cat. No.: HY-B0492
CAS No.: 78246-49-8
Synonyms: BRL29060 hydrochloride; BRL29060A
Paroxetine (BRL29060) hydrochloride is an orally active and selective serotonin reuptake inhibitor (SSRI) and apoptosis inducer with blood-brain barrier permeability. Paroxetine hydrochloride inhibits nitric oxide synthase and CYP2D6, induces desensitization of 5-HT1A/1B/1D autoreceptors, downregulates 5-HT2 receptors, and promotes the production of inflammatory cytokines. Paroxetine hydrochloride is a weak norepinephrine (NE) uptake inhibitor and possesses antitumor activity. Paroxetine hydrochloride is widely used in research concerning depression, obsessive-compulsive disorder, panic disorder, social phobia, generalized anxiety disorder, post-traumatic stress disorder, premenstrual dysphoric disorder, hot flashes, and related conditions .
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8
8 Cited Publications
Cat. No.: HY-100903
CAS No.: 113158-34-2
Purity:  98.91%
Synonyms: nor-Binaltorphimine dihydrochloride; nor-BNI dihydrochloride
Target:  

Opioid Receptor

Research Areas:  

Neurological Disease

Norbinaltorphimine dihydrochloride (nor-Binaltorphimine dihydrochloride; nor-BNI dihydrochloride) is a selective, long-acting competitive antagonist of the κ-opioid receptor. Norbinaltorphimine dihydrochloride blocks κ-opioid receptor-mediated analgesic effects, and inhibits butorphanol-induced changes in κ-opioid receptor binding kinetics, desensitization and down-regulation. Norbinaltorphimine dihydrochloride suppresses specific opioid withdrawal symptoms, precipitates withdrawal behaviors in butorphanol-dependent rats, and serves as a molecular probe for studying κ-opioid receptor-agonist interactions. Norbinaltorphimine dihydrochloride is applicable to research related to neurological disorders such as pain .
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8
8 Cited Publications
Cat. No.: HY-117040
CAS No.: 105618-26-6
Purity:  98.70%
Synonyms: Norbinaltorphimine; NorBNI
Target:  

Opioid Receptor

Research Areas:  

Neurological Disease

nor-Binaltorphimine (Norbinaltorphimine; NorBNI) is a selective, long-acting competitive antagonist of the κ-opioid receptor. nor-Binaltorphimine blocks κ-opioid receptor-mediated analgesic effects, and inhibits butorphanol-induced changes in κ-opioid receptor binding kinetics, desensitization and down-regulation. nor-Binaltorphimine suppresses specific opioid withdrawal symptoms, precipitates withdrawal behaviors in butorphanol-dependent rats, and serves as a molecular probe for studying κ-opioid receptor-agonist interactions. nor-Binaltorphimine is applicable to research related to neurological disorders such as pain .
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4
4 Cited Publications
Cat. No.: HY-103045
CAS No.: 865608-11-3
Purity:  98.95%
CMPD101 is a potent, highly selective and membrane-permeable small-molecule inhibitor of GRK2/3 with IC50 of 18 nM and 5.4 nM, respectively. CMPD101 exhibits less selectively against GRK1, GRK5, ROCK-2 and PKCα with IC50s of 3.1 μM , 2.3 μM, 1.4 μM and 8.1 μM, respectively. CMPD101 can be used for the study of heart failure .
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2
2 Cited Publications
Cat. No.: HY-101165
CAS No.: 2259-96-3
Purity:  98.29%
Target:  

iGluR GABA Receptor

Research Areas:  

Neurological Disease

Cyclothiazide is a positive allosteric modulator of ionotropic AMPA-type glutamate receptors. Cyclothiazide inhibits GABAA receptors. Cyclothiazide is frequently used to produce a fast inhibition of AMPA receptor desensitization and a much slower potentiation of the AMPA current. Cyclothiazide can potentiate responses to kainate in hippocampal neurons. Cyclothiazide has effects on glutamatergic neurotransmission. Cyclothiazide also induces epileptiform EEG activity accompanying behavioral seizures .
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1
1 Cited Publications
Cat. No.: HY-N2071
CAS No.: 77-53-2
Synonyms: (+)-Cedrol; α-Cedrol
Cedrol is a potent competitive inhibitor of cytochrome P-450(CYP) enzyme. Cedrol plays an anticancer role by inducing cell cycle arrest and Caspase-dependent apoptosis. Cedrol acts as a neutrophil agonist that can desensitize cells to subsequent stimulation of N-formyl peptides. Cedrol prevents neuropathic pain caused by chronic contractile injury by inhibiting oxidative stress and inflammation. In addition, Cedrol has antibacterial, hair loss prevention and anti-anxiety properties .
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1
1 Cited Publications
Cat. No.: HY-N4323
CAS No.: 4176-97-0
14-Deoxyandrographolide is a diterpene with calcium channel blocking activity and acts as a uterine smooth muscle relaxant. 14-Deoxyandrographolide stimulates the release of nitric oxide (NO) in endothelial cells. 14-Deoxyandrographolide gradually desensitizes liver cells to TNF-α mediated apoptosis by inducing the release of TNFRSF1A .
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Cat. No.: HY-W004049
CAS No.: 99-06-9
3-Hydroxybenzoic acid is an orally active endogenous metabolite. 3-Hydroxybenzoic acid is an agonist for GPR81 and GPR109A. 3-Hydroxybenzoic acid acts as stress response desensitizers. 3-Hydroxybenzoic acid can be used for anti-inflammatory and analgesic study .
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Cat. No.: HY-W001160
CAS No.: 1953-54-4
5-Hydroxyindole is an orally active hydroxylated indole and tryptophan metabolite. 5-Hydroxyindole activates α7 nicotinic acetylcholine receptors and acts on intestinal L-type calcium channels. 5-Hydroxyindole slows down the desensitization of 5-HT3 receptor-mediated ion currents in cells. 5-Hydroxyindole causes convulsions and loss of consciousness. 5-Hydroxyindole is used in the study of neuroblastoma, schizophrenia, and diseases related to intestinal motility disorders .
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Cat. No.: HY-12509
CAS No.: 141286-78-4
Purity:  99.87%
Target:  

iGluR

Research Areas:  

Neurological Disease

PEPA is an AMPA receptor allosteric potentiator. PEPA shows preferential action of PEPA on the flop form of AMPA receptors. PEPA is a more potent suppressor of desensitization of receptors containing GluR3 and GluR4 as opposed to those containing GluR1. PEPA has antianxiety effects .
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Cat. No.: HY-121027
CAS No.: 486-89-5
Purity:  98.15%
Synonyms: (-)-Anagyrine; Monolupine; Rhombinine
Anagyrine ((-)-Anagyrine) is a quinolizidine alkaloid that has been found in Lupinus albus. Anagyrine binds to muscarinic and nicotinic acetylcholine receptors with IC50 values of 132 and 2096 µM respectively. Anagyrine is a potent and effective desensitizer of nAChR, and Anagyrine can directly, without metabolism, desensitize nAChR .
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Cat. No.: HY-110023
CAS No.: 60525-15-7
Purity:  98.27%
Target:  

Serotonin Transporter

Research Areas:  

Neurological Disease

Zimelidine dihydrochloride is an orally active selective serotonin reuptake inhibitor. Zimelidine dihydrochloride competitively inhibits central 5-HT uptake and desensitizes 5-HT autoreceptors in dorsal raphe nucleus. Zimelidine dihydrochloride time-dependently modulates 5-HT neuronal firing and hippocampal CA3 responses. Zimelidine dihydrochloride strengthens central serotonergic neurotransmission and produces related behavioral changes. Zimelidine dihydrochloride exerts anxiolytic, analgesic, feeding-suppressive and tolerance-attenuating effects. Zimelidine dihydrochloride is used for the study of depressive disorders and analgesic tolerance .
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Cat. No.: HY-106103
CAS No.: 81377-02-8
Purity:  99.30%
Synonyms: MK-678; L-363586
Seglitide (MK-678) is an orally active, selective SSTR2 agonist and somatostatin analog. Seglitide also acts as a competitive Somatostatin receptor antagonist, with pA2 values of 6.50, 6.24 and 6.09 against SS14, SS25 and SS28, respectively. Seglitide produces only weak, transient inhibition of myocardial contractility in isolated right atria of guinea pigs. Seglitide inhibits glucagon secretion and reduces circulating insulin levels. Seglitide causes a sustained, reversible reduction in elevated systolic blood pressure in streptozotocin (HY-13753)-induced diabetic rats, but exerts no effect on spontaneously hypertensive rats. Seglitide induces membrane hyperpolarization and inhibits electrical excitability. Seglitide induces concentration-dependent contraction and significant desensitization in isolated distal colon of rats. Seglitide can be used in research related to hypertension complicated with insulin-dependent diabetes mellitus .
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Cat. No.: HY-163671
CAS No.: 2767348-36-5
Target:  

GPR52 Arrestin

Research Areas:  

Neurological Disease

PW0729 is a selective GPR52 agonist. PW0729 activates G protein/cAMP signaling pathway, with bias toward this pathway over β-arrestin recruitment, and induces GPR52 desensitization. PW0729 can be used for the research of neuropsychiatric and neurological diseases .
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Cat. No.: HY-P1831
CAS No.: 150238-87-2
Synonyms: ProAM N20, Human; PAMP-20, human
Proadrenomedullin (1-20), human is a potent hypotensive and catecholamine release–inhibitory peptide released from chromaffin cells. Proadrenomedullin (1-20) inhibits catecholamine secretion in PC12 pheochromocytoma cells (IC50 ≈ 350 nM) by suppressing Na +/Ca 2+ influx and blocking desensitization. Proadrenomedullin (1-20), human specifically acts on nicotinic cholinergic receptors in a non competitive manner. Proadrenomedullin (1-20), human can be used for research on conditions such as hypertension .
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Cat. No.: HY-100939
CAS No.: 14279-91-5
Purity:  99.07%
Target:  

Sodium Channel

Research Areas:  

Neurological Disease

4-Chlorophenylguanidine hydrochloride is an urokinase-type plasminogen activator inhibitor. 4-Chlorophenylguanidine hydrochloride is a potent ASIC3 positive allosteric modulator and reverses the effects of ASIC3 desensitization. 4-Chlorophenylguanidine hydrochloride influences ASIC3 activity through directly activating the channel and increasing proton sensitivity. 4-Chlorophenylguanidine hydrochloride offers a chemical backbone for the design of new ASIC3 ligands to study ASIC3 in vivo .
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Cat. No.: HY-122272R
CAS No.: 61869-08-7
Synonyms: BRL29060 (Standard)
Paroxetine (BRL29060) (Standard) is the analytical standard of Paroxetine (HY-122272). This product is intended for research and analytical applications. Paroxetine (BRL29060) is an orally active and selective serotonin reuptake inhibitor (SSRI) and apoptosis inducer with blood-brain barrier permeability. Paroxetine inhibits nitric oxide synthase and CYP2D6, induces desensitization of 5-HT1A/1B/1D autoreceptors, downregulates 5-HT2 receptors, and promotes the production of inflammatory cytokines. Paroxetine is a weak norepinephrine (NE) uptake inhibitor and possesses antitumor activity. Paroxetine is widely used in research concerning depression, obsessive-compulsive disorder, panic disorder, social phobia, generalized anxiety disorder, post-traumatic stress disorder, premenstrual dysphoric disorder, hot flashes, and related conditions .
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Cat. No.: HY-103229
CAS No.: 909400-43-7
Purity:  ≥99.0%
Target:  

iGluR

Research Areas:  

Neurological Disease

Cl-HIBO is a highly subtype-selective GluR1/2 agonist (EC50=4.7 and 1.7 μM, respectively). Cl-HIBO is a potent AMPA receptor agonist (IC50=0.22 μM). Cl-HIBO has desensitizing properties .
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Cat. No.: HY-W004049R
CAS No.: 99-06-9
3-Hydroxybenzoic acid (Standard) is the analytical standard of 3-Hydroxybenzoic acid. This product is intended for research and analytical applications. 3-Hydroxybenzoic acid is an orally active endogenous metabolite. 3-Hydroxybenzoic acid is an agonist for GPR81 and GPR109A. 3-Hydroxybenzoic acid acts as stress response desensitizers. 3-Hydroxybenzoic acid can be used for anti-inflammatory and analgesic study.
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