Search Result
Results for "
α1-adrenergic receptor antagonist
" in MedChemExpress (MCE) Product Catalog:
5
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-101815
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- HY-121186
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- HY-B0781S
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Histamine Receptor
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Neurological Disease
Endocrinology
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Promethazine-d4 (hydrochloride) is the deuterium labeled Promethazine hydrochloride. Promethazine hydrochloride is the first-generation antihistamine; strong antagonist of the H1 receptor and moderate mACh receptor antagonist, moderate affinity for 5-HT2A, 5-HT2C, D2 and α1-adrenergic receptors.
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- HY-118638
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- HY-116379
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Adrenergic Receptor
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Metabolic Disease
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RS-100329 is an α1-adrenergic receptor (α1-AR) antagonist that effectively inhibits α1-adrenergic receptor-mediated contractions of lower urinary tract tissues in vitro and in vivo. RS-100329 can be used in the research of symptoms related to benign prostatic hyperplasia .
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- HY-111188
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Adrenergic Receptor
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Others
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A55453 is a prazosin analogue and a potent α1-adrenergic antagonist. 125I-A55453 is a high-affinity alpha 1-adrenergic receptor probe .
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- HY-U00367
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- HY-B0532S
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- HY-111984A
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Adrenergic Receptor
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Cardiovascular Disease
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Quinazosin dihydrochloride is an antihypertensive α1-adrenergic receptor antagonist whose activity is associated with inhibition of granulopoiesis, resulting in neutropenia and leukopenia. Quinazosin dihydrochloride exhibits dose-related myelosuppression that is correlated with the duration of suppression .
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- HY-112074A
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HOE 440 hydrochloride
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Adrenergic Receptor
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Cardiovascular Disease
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Tiamenidine hydrochloride (HOE 440 hydrochloride) is a centrally acting α1-adrenergic receptor antagonist with hypotensive activity. Tiamenidine hydrochloride regulates blood pressure levels by binding to α1 receptors. Tiamenidine hydrochloride can be used in the study of hypertension .
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- HY-121186R
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Adrenergic Receptor
Calcium Channel
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Neurological Disease
Metabolic Disease
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Bevantolol (hydrochloride) (Standard) is the analytical standard of Bevantolol (hydrochloride). This product is intended for research and analytical applications. Bevantolol hydrochloride is a selective β1 and α1-adrenergic receptor antagonist with pKi values of 7.83, 6.9 in rat cerebral cortex, respectively. Bevantolol hydrochloride is a potent Ca 2+ antagonist .
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- HY-106617A
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5-HT Receptor
Adrenergic Receptor
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Neurological Disease
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Etoperidone hydrochloride, an antidepressant agent, is an orally active serotonin and nor-adrenaline re-uptake antagonist. Etoperidone hydrochloride shows Kd values of 36 nM, 38 nM, 85 nM, and 570 nM for 5-HT2 receptor, α1-adrenergic receptor, 5-HT1A receptor, and α2-adrenergic receptor, respectively .
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- HY-106617
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5-HT Receptor
Adrenergic Receptor
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Neurological Disease
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Etoperidone, an antidepressant agent, is an orally active serotonin and nor-adrenaline re-uptake antagonist. Etoperidone shows Kd values of 36 nM, 38 nM, 85 nM, and 570 nM for 5-HT2 receptor, α1-adrenergic receptor, 5-HT1A receptor, and α2-adrenergic receptor, respectively .
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- HY-12962
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iGluR
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Neurological Disease
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NMDA-IN-1 is a potent and NR2B-selective NMDA antagonist with Ki of 0.85 nM; NR2B Ca2+ influx IC50 is 9.7 nM; no activities on NR2A, NR2C, NR2D, hERG-channel and α1-adrenergic receptor.
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- HY-103413
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Dopamine Receptor
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Neurological Disease
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Eticlopride hydrochloride, a selective dopamine D2‐like receptor antagonist, exhibits high affinity for dopamine D2, α1‐adrenergic, α2‐adrenergic, 5HT1, 5HT2 receptors with Kis of 0.09, 112, 699, 6220, and 830 nM, respectively. Antipsychotic agent .
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- HY-B0532
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Dopamine Receptor
Adrenergic Receptor
P-glycoprotein
CaMK
Influenza Virus
Autophagy
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Neurological Disease
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Trifluoperazine, an antipsychotic agent, acts by blocking central dopamine receptors. Trifluoperazine is a potent α1-adrenergic receptor antagonist. Trifluoperazine is a potent NUPR1 inhibitor exerting anticancer activity. Trifluoperazine is a calmodulin inhibitor, and also inhibits P-glycoprotein. Trifluoperazine can be used for the research of schizophrenia. Trifluoperazine acts as a reversible inhibitor of influenza virus morphogenesis .
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- HY-B0532A
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Dopamine Receptor
Adrenergic Receptor
CaMK
P-glycoprotein
Influenza Virus
Autophagy
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Neurological Disease
Cancer
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Trifluoperazine dihydrochloride, an antipsychotic agent, acts by blocking central dopamine receptors. Trifluoperazine dihydrochloride is a potent α1-adrenergic receptor antagonist. Trifluoperazine dihydrochloride is a potent NUPR1 inhibitor exerting anticancer activity. Trifluoperazine dihydrochloride is a calmodulin inhibitor, and also inhibits P-glycoprotein. Trifluoperazine dihydrochloride can be used for the research of schizophrenia. Trifluoperazine dihydrochloride acts as a reversible inhibitor of influenza virus morphogenesis .
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- HY-19686
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TVX Q 7821 free base
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5-HT Receptor
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Neurological Disease
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Ipsapirone (TVX Q 7821) is an anxiolytic compound and a 5-HT1A receptor partial agonist. Ipsapirone (TVX Q 7821) also exhibits 5-HT1A receptor antagonistic effect, and only at high doses it can also produce an inhibitory effect on 5-HT2 and the α1-adrenergic function .
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- HY-19686A
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TVX Q 7821
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5-HT Receptor
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Neurological Disease
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Ipsapirone hydrochloride (TVX Q 7821) is an anxiolytic compound and a 5-HT1A receptor partial agonist. Ipsapirone hydrochloride (TVX Q 7821) also exhibits 5-HT1A receptor antagonistic effect, and only at high doses it can also produce an inhibitory effect on 5-HT2 and the α1-adrenergic function .
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- HY-103093
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5-HT Receptor
Histamine Receptor
Adrenergic Receptor
Dopamine Receptor
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Neurological Disease
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Zotepine, an antipsychotic agent, is a potent antagonist of 5-HT2A, 5-HT2C, Histamine H1, α1-adrenergic and Dopamine D2 receptors, with Kds of 2.6 nM, 3.2 nM, 3.3 nM, 7.3 nM and 8 nM, respectively. Zotepine exhibits antidepressive and anxiolytic effects in vivo .
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- HY-B0532AS
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Isotope-Labeled Compounds
Dopamine Receptor
Adrenergic Receptor
CaMK
P-glycoprotein
Influenza Virus
Autophagy
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Neurological Disease
Cancer
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Trifluoperazine-d3 (dihydrochloride) is deuterium labeled Trifluoperazine (dihydrochloride). Trifluoperazine dihydrochloride, an antipsychotic agent, acts by blocking central dopamine receptors. Trifluoperazine dihydrochloride is a potent α1-adrenergic receptor antagonist. Trifluoperazine dihydrochloride is a potent NUPR1 inhibitor exerting anticancer activity. Trifluoperazine dihydrochloride is a calmodulin inhibitor, and also inhibits P-glycoprotein. Trifluoperazine dihydrochloride can be used for the research of schizophrenia. Trifluoperazine dihydrochloride acts as a reversible inhibitor of influenza virus morphogenesis[1][2][3][4][5].
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- HY-B0532B
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Dopamine Receptor
Adrenergic Receptor
P-glycoprotein
CaMK
Influenza Virus
Autophagy
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Infection
Neurological Disease
Cancer
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Trifluoperazine dimaleate, an antipsychotic agent, acts by blocking central dopamine receptors. Trifluoperazine dimaleate is a potent α1-adrenergic receptor antagonist. Trifluoperazine dimaleate is a potent NUPR1 inhibitor exerting anticancer activity. Trifluoperazine dimaleate is a calmodulin inhibitor, and also inhibits P-glycoprotein. Trifluoperazine dimaleate can be used for the research of schizophrenia. Trifluoperazine dimaleate acts as a reversible inhibitor of influenza virus morphogenesis .
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- HY-10349A
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5-HT Receptor
Dopamine Receptor
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Neurological Disease
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WAY-100635 maleate is a potent and selective 5-hydroxytryptamine 1A (5-HT1A) receptor antagonist with an IC50 value of 0.91 nM and Ki value of 0.39 nM. WAY-100635 maleate has pIC50 values for 5-HT1A and α1-adrenergic receptors of 8.9 and 6.6, respectively. WAY-100635 maleate is also a potent dopamine D4 receptor agonist .
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- HY-B0532AR
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Dopamine Receptor
Adrenergic Receptor
CaMK
P-glycoprotein
Influenza Virus
Autophagy
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Neurological Disease
Cancer
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Trifluoperazine (dihydrochloride) (Standard) is the analytical standard of Trifluoperazine (dihydrochloride). This product is intended for research and analytical applications. Trifluoperazine dihydrochloride, an antipsychotic agent, acts by blocking central dopamine receptors. Trifluoperazine dihydrochloride is a potent α1-adrenergic receptor antagonist. Trifluoperazine dihydrochloride is a potent NUPR1 inhibitor exerting anticancer activity. Trifluoperazine dihydrochloride is a calmodulin inhibitor, and also inhibits P-glycoprotein. Trifluoperazine dihydrochloride can be used for the research of schizophrenia. Trifluoperazine dihydrochloride acts as a reversible inhibitor of influenza virus morphogenesis .
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- HY-B0193A
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Adrenergic Receptor
Autophagy
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Cardiovascular Disease
Endocrinology
Cancer
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Prazosin hydrochloride is a well-tolerated, CNS-active α1-adrenergic receptor antagonist for the research of high blood pressure and alcohol use disorders . Prazosin hydrochloride potently inhibits Norepinephrine (NE)-stimulated 45Ca efflux with an IC50 of 0.15 nM .Prazosin hydrochloride inhibits organic cation transporters OCT-1 and OCT-3 with IC50s of 1.8, and 13 μM, respectively .
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- HY-103093R
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5-HT Receptor
Histamine Receptor
Adrenergic Receptor
Dopamine Receptor
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Neurological Disease
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Zotepine (Standard) is the analytical standard of Zotepine. This product is intended for research and analytical applications. Zotepine, an antipsychotic agent, is a potent antagonist of 5-HT2A, 5-HT2C, Histamine H1, α1-adrenergic and Dopamine D2 receptors, with Kds of 2.6 nM, 3.2 nM, 3.3 nM, 7.3 nM and 8 nM, respectively. Zotepine exhibits antidepressive and anxiolytic effects in vivo .
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- HY-10349
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5-HT Receptor
Dopamine Receptor
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Neurological Disease
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WAY-100635 is a potent and selective 5-HT1A Receptor antagonist with a pIC50 of 8.87, an apparent pA2 of 9.71.
WAY-100635 is a potent and selective 5-hydroxytryptamine 1A (5-HT1A) receptor antagonist with an IC50 value of 0.91 nM and Ki value of 0.39 nM. WAY-100635 has pIC50 values for 5-HT1A and α1-adrenergic receptors of 8.9 and 6.6, respectively. WAY-100635 is also a potent dopamine D4 receptor agonist .
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- HY-B0193AR
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Adrenergic Receptor
Autophagy
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Cardiovascular Disease
Endocrinology
Cancer
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Prazosin (hydrochloride) (Standard) is the analytical standard of Prazosin (hydrochloride). This product is intended for research and analytical applications. Prazosin hydrochloride is a well-tolerated, CNS-active α1-adrenergic receptor antagonist for the research of high blood pressure and alcohol use disorders . Prazosin hydrochloride potently inhibits Norepinephrine (NE)-stimulated 45Ca efflux with an IC50 of 0.15 nM .Prazosin hydrochloride inhibits organic cation transporters OCT-1 and OCT-3 with IC50s of 1.8, and 13 μM, respectively .
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- HY-U00110
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- HY-105798
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- HY-12882
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RC 61-91; NP-120
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iGluR
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Neurological Disease
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Ifenprodil (RC 61-91) is a noncompetitive NMDA receptor antagonist with anti-excitotoxic activity. Ifenprodil significantly improves long-term sensorimotor and spatial learning deficits in mice after acute subarachnoid hemorrhage. Ifenprodil reduces neuronal cell death in the basal cortex and CA1 region of the hippocampus induced by experimental subarachnoid hemorrhage. Ifenprodil attenuates Ca2+ overload in basal cortical cells and mitochondria, as well as brain edema in blood-brain barrier damage and early brain injury. Ifenprodil reduces the intracellular Ca2+ increase and apoptosis of primary cortical neurons under conditions of high glutamate concentrations. Ifenprodil also reduces the increase in endothelial permeability caused by high glutamate concentrations in human brain microvascular endothelial cells. Ifenprodil also inhibits GIRK channels and interacts with α1-adrenergic, 5-HT, and σ receptors .
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- HY-B0192AS1
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- HY-B0192AS
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- HY-101690
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- HY-12717
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Adrenergic Receptor
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Endocrinology
Cancer
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Phentolamine is a potent, selective and orally active α1 adrenergic and α2 adrenergic receptor antagonist. Phentolamine can be used for the research of erectile dysfunction .
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- HY-N2037
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Norcoclaurine; Demethyl-Coclaurine
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MAP3K
MDM-2/p53
Adrenergic Receptor
ROS Kinase
Apoptosis
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Cardiovascular Disease
Endocrinology
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Higenamine (Norcoclaurine), a β2-AR agonist with antioxidant capability, is a key component of the Chinese herb aconite root that prescribes for treating symptoms of heart failure in the oriental Asian countries. Higenamine is also a α1-adrenergic receptor antagonist with hypotensive effect. is a selective LSD1 inhibitor (IC50=1.47 μM) that can be isolated from aconite. Higenamine hydrochloride has anti-inflammatory and antibacterial activity. Higenamine protects myocyte Apoptosis and ischemia/reperfusion (I/R) injury through selective activation of beta2-adrenergic receptor (β2-AR). Higenamine also reduces I/R-induced myocardial infarction in mice. Higenamine can attenuate IL-1β-induced Apoptosis through ROS-mediated PI3K/Akt signaling pathway. Higenamine protects brain cells from oxygen deprivation. Higenamine can promote bone formation in osteoporosis through the SMAD2/3 pathway. Higenamine can be used to study cancer, inflammation, cardiorenal syndrome and other diseases .
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- HY-100980
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BE2254 hydrochloride
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Adrenergic Receptor
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Neurological Disease
Cancer
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HEAT (BE2254) hydrochloride is a selective alpha 1 adrenergic receptor antagonist. HEAT hydrochloride, a phenethylamine derivative, shows pKis of 9, 9.1, and 8.57 for alpha 1a, alpha 1b and alpha 1c, respectively .
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- HY-10791
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- HY-12717R
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Adrenergic Receptor
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Endocrinology
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Phentolamine (Standard) is the analytical standard of Phentolamine. This product is intended for research and analytical applications. Phentolamine is a potent, selective and orally active α1 adrenergic and α2 adrenergic receptor antagonist. Phentolamine can be used for the research of erectile dysfunction .
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- HY-137387
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Drug Metabolite
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Cardiovascular Disease
Others
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Carvedilol Glucuronide is the metabolite of Carvedilol (HY-B0006). Carvedilol (BM 14190) is an antagonist for β/α-1 adrenergic receptor. Carvedilol inhibits lipid peroxidation with an IC50 of 5 μM. Carvedilol is an antihypertensive agent with potential use in angina and congestive heart failure. Carvedilol is an autophagy inducer that inhibits the NLRP3 inflammasome .
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- HY-N0584B
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6-Hydroxyhyoscyamine hydrochloride
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Adrenergic Receptor
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Inflammation/Immunology
Cancer
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Anisodamine hydrochloride is an anticholinergic and α1 adrenergic receptor antagonist. Anisodamine hydrochloride can be used for improving blood flow in circulatory disorders such as septic shock, Anisodamine hydrochloride displays a spectrum of pharmacological effects similar to Atropine (HY-B1205) and Sopolamine (HY-B2065) including inhibition of salivation, gastrointestinal and sweat secretion, gastrointestinal motility, respiratory secretion and urinary bladder contraction in vivo .
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- HY-B1435A
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Thymoxamine
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Others
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Neurological Disease
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Moxisylyte (Thymoxamine) is an alpha 1-selective antagonist with activity that improves bladder emptying. Moxisylyte is used to suppress urinary difficulties in patients with multiple system atrophy (MSA) by blocking alpha 1-adrenergic receptors to reduce the amount of residual urine after urination. Moxisylyte is also used to suppress erectile dysfunction and can improve blood circulation problems caused by Raynaud's syndrome in the short term. In addition, Moxisylyte can be applied topically to the eye to reverse the mydriasis caused by phenylephrine and other sympathetic stimulants .
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- HY-136693
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Others
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Neurological Disease
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L-654284 is an α2-adrenergic receptor antagonist with significant selectivity. L-654284 competes with the binding of 3H-clonidine and 3H-rauwolscine in vitro and shows Ki values of 0.8 nM and 1.1 nM, respectively. L-654284 can block the protrusion effect of clonidine in isolated vas deferens in rats, with a pA2 value of 9.1. L-654284 exhibits remarkable selectivity for α2 and α1 adrenergic receptors, and exhibits a Ki of 110 nM in inhibiting 3H-prazosin binding. L-654284 can significantly increase the turnover rate of norepinephrine in rat cerebral cortex in vivo, showing α2-adrenergic receptor blocking activity in the central nervous system .
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
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- HY-B0781S
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Promethazine-d4 (hydrochloride) is the deuterium labeled Promethazine hydrochloride. Promethazine hydrochloride is the first-generation antihistamine; strong antagonist of the H1 receptor and moderate mACh receptor antagonist, moderate affinity for 5-HT2A, 5-HT2C, D2 and α1-adrenergic receptors.
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- HY-B0532S
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Trifluoperazine-d8 is a deuterium labeled Trifluoperazine. Trifluoperazine is an antipsychotic phenothiazine agent and a selective α1-adrenergic receptor antagonist. Trifluoperazine is also a potent dopamine D2 receptor inhibitor [1][2].
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- HY-B0532AS
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Trifluoperazine-d3 (dihydrochloride) is deuterium labeled Trifluoperazine (dihydrochloride). Trifluoperazine dihydrochloride, an antipsychotic agent, acts by blocking central dopamine receptors. Trifluoperazine dihydrochloride is a potent α1-adrenergic receptor antagonist. Trifluoperazine dihydrochloride is a potent NUPR1 inhibitor exerting anticancer activity. Trifluoperazine dihydrochloride is a calmodulin inhibitor, and also inhibits P-glycoprotein. Trifluoperazine dihydrochloride can be used for the research of schizophrenia. Trifluoperazine dihydrochloride acts as a reversible inhibitor of influenza virus morphogenesis[1][2][3][4][5].
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- HY-B0192AS1
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Alfuzosin-d7 (hydrochloride) is the deuterium labeled Alfuzosin hydrochloride. Alfuzosin hydrochloride is an α1 adrenergic receptor antagonist used to treat benign prostatic hyperplasia (BPH).
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- HY-B0192AS
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Alfuzosin-d3 hydrochloride is the deuterium labeled Alfuzosin hydrochloride. Alfuzosin hydrochloride is an α1 adrenergic receptor antagonist used to treat benign prostatic hyperplasia (BPH).
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