Search Result
Results for "
α2-adrenoceptor
" in MedChemExpress (MCE) Product Catalog:
9
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-12710
-
α-Yohimbine; Corynanthidine; Isoyohimbine
|
Adrenergic Receptor
|
Cancer
|
Rauwolscine is a selective α2-adrenoceptor antagonist that inhibits tumor growth and induces apoptosis .
|
-
-
- HY-B0409A
-
-
-
- HY-155879
-
-
-
- HY-B0352
-
-
-
- HY-12380A
-
-
-
- HY-12380
-
-
-
- HY-136935
-
|
Adrenergic Receptor
|
Endocrinology
|
Alloyohimbine, an alkaloid, is a selective α2-adrenoceptor antagonist with K Dα1, K Dα2 of 0.28 μM and 0.006 μM, respectively .
|
-
-
- HY-W263279
-
(E)-Wy-8678
|
Adrenergic Receptor
|
Cardiovascular Disease
Neurological Disease
|
(E)-Guanabenz ((E)-Wy-8678) is an orally active central α2-adrenoceptor agonist. (E)-Guanabenz has antihypertensive activity, acts via stimulating central α2-adrenoceptors, and reducing net sympathetic outflow into the periphery. (E)-Guanabenz also directly binds to and inhibits GADD34, and has neuroprotective activity. (E)-Guanabenz can be used for researching hypertension and Parkinson disease [2].
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-
-
- HY-B0352S3
-
-
-
- HY-B0409AR
-
|
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
Cancer
|
Clonidine (hydrochloride) (Standard) is the analytical standard of Clonidine (hydrochloride). This product is intended for research and analytical applications. Clonidine hydrochloride is an agonist of α2-adrenoceptor and potent antihypertensive agent.
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-
-
- HY-B0409S
-
-
-
- HY-17034
-
|
Adrenergic Receptor
|
Neurological Disease
Endocrinology
|
Medetomidine is an orally active α2-adrenoceptor agonist (Ki: 1.08 nM). Medetomidine has sedative and analgesic effects. Medetomidine can cause peripheral vasoconstriction through the activation of α2 adrenoceptors on blood vessels [2] .
|
-
-
- HY-17034B
-
MPV785
|
Adrenergic Receptor
|
Neurological Disease
Endocrinology
|
Medetomidine hydrochloride is an orally active α2-adrenoceptor agonist (Ki: 1.08 nM). Medetomidine hydrochloride has sedative and analgesic effects. Medetomidine hydrochloride can cause peripheral vasoconstriction through the activation of α2 adrenoceptors on blood vessels [2] .
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-
-
- HY-A0008
-
-
-
- HY-U00165
-
-
-
- HY-106874B
-
rel-RS-15385-197
|
Adrenergic Receptor
Prostaglandin Receptor
|
Neurological Disease
|
rel-Delequamine (rel-RS-15385-197) is an orally active, brain-penetrant, potent and selective M2-adrenoceptor antagonist and α2-adrenoceptor antagonist. rel-Delequamine has a pKi of 9.45 for α2-adrenoceptors in the rat cortex. rel-Delequamine augments K +-evoked release of noradrenaline with an EC50 of 1 nM .
|
-
-
- HY-B1416A
-
-
-
- HY-148529
-
(±)-DG5128 free base; DG5128 free base
|
Adrenergic Receptor
|
Cardiovascular Disease
Metabolic Disease
|
Midaglizole ((±)-DG5128 free base; DG5128 free base) is a potent α2-adrenoceptor antagonist. Midaglizole is a hypoglycemic agent. Midaglizole increases blood pressure and reduces blood glucose levels in vivo [2] .
|
-
-
- HY-17034BS1
-
MPV785-13C,d3
|
Isotope-Labeled Compounds
Adrenergic Receptor
|
Endocrinology
|
Medetomidine-13C,d3 (hydrochloride) is a deuterated labeled Medetomidine (hydrochloride) . Medetomidine hydrochloride is an orally active α2-adrenoceptor agonist (Ki: 1.08 nM). Medetomidine hydrochloride has sedative and analgesic effects. Medetomidine hydrochloride can cause peripheral vasoconstriction through the activation of α2 adrenoceptors on blood vessels [2] .
|
-
-
- HY-103203
-
-
-
- HY-12724
-
|
Adrenergic Receptor
Parasite
|
Cardiovascular Disease
Cancer
|
Guanabenz is an orally active α-2-adrenoceptor agonist. Guanabenz has antihypertensive effect and antiparasitic activity. Guanabenz interferes ER stress-signalling and has protective effects in cardiac myocytes. Guanabenz also is used for the research of high blood pressure [2] .
|
-
-
- HY-12724A
-
|
Parasite
Adrenergic Receptor
|
Cardiovascular Disease
Cancer
|
Guanabenz hydrochloride is an orally active α-2-adrenoceptor agonist. Guanabenz hydrochloride has antihypertensive effect and antiparasitic activity. Guanabenz hydrochloride interferes ER stress-signalling and has protective effects in cardiac myocytes. Guanabenz hydrochloride also is used for the research of high blood pressure [2] .
|
-
-
- HY-101061
-
|
Adrenergic Receptor
|
Cardiovascular Disease
|
2-MPMDQ is a potent and selective α1-adrenoceptor (Ki=0.37 nM) antagonist over α2-adrenoceptor (Ki=1740 nM). 2-MPMDQ is potent anti-hypertensive agent and has the potential for hypertension research .
|
-
-
- HY-17034A
-
(+)-Medetomidine hydrochloride; (S)-Medetomidine hydrochloride
|
Adrenergic Receptor
|
Neurological Disease
Endocrinology
Cancer
|
Dexmedetomidine hydrochloride ((+)-Medetomidine hydrochloride) is a potent, selective and orally active agonist of α2-adrenoceptor, with a Ki of 1.08 nM. Dexmedetomidine hydrochloride shows 1620-fold selectivity against α1-adrenoceptor. Dexmedetomidine hydrochloride exhibits anxiolysis, sedation, and modest analgesia effects [2] .
|
-
-
- HY-12719
-
(+)-Medetomidine; (S)-Medetomidine
|
Adrenergic Receptor
|
Neurological Disease
Cancer
|
Dexmedetomidine ((+)-Medetomidine) is a potent, selective and orally active agonist of α2-adrenoceptor, with a Ki of 1.08 nM. Dexmedetomidine shows 1620-fold selectivity against α1-adrenoceptor. Dexmedetomidine exhibits anxiolysis, sedation, and modest analgesia effects [2] .
|
-
-
- HY-B0354A
-
-
-
- HY-14561A
-
RX 781094 hydrochloride
|
Adrenergic Receptor
Imidazoline Receptor
|
Neurological Disease
Endocrinology
|
Idazoxan hydrochloride (RX 781094 hydrochloride) is an α2-adrenoceptor antagonist and is also a imidazoline receptors (IRs) antagonist competitively antagonized the centrally induced hypotensive effect of imidazoline-like agents (IMs). Idazoxan hydrochloride also improves motor symptoms in Parkinson’s disease, L-DOPA-induced dyskinesias, and experimental Parkinsonism [2].
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-
-
- HY-12719R
-
|
Adrenergic Receptor
|
Neurological Disease
Cancer
|
Dexmedetomidine (Standard) is the analytical standard of Dexmedetomidine. This product is intended for research and analytical applications. Dexmedetomidine ((+)-Medetomidine) is a potent, selective and orally active agonist of α2-adrenoceptor, with a Ki of 1.08 nM. Dexmedetomidine shows 1620-fold selectivity against α1-adrenoceptor. Dexmedetomidine exhibits anxiolysis, sedation, and modest analgesia effects [2] .
|
-
-
- HY-17034AR
-
(+)-Medetomidine hydrochloride (Standard); (S)-Medetomidine hydrochloride (Standard)
|
Adrenergic Receptor
|
Neurological Disease
Endocrinology
Cancer
|
Dexmedetomidine (hydrochloride) (Standard) is the analytical standard of Dexmedetomidine (hydrochloride). This product is intended for research and analytical applications. Dexmedetomidine hydrochloride ((+)-Medetomidine hydrochloride) is a potent, selective and orally active agonist of α2-adrenoceptor, with a Ki of 1.08 nM. Dexmedetomidine hydrochloride shows 1620-fold selectivity against α1-adrenoceptor. Dexmedetomidine hydrochloride exhibits anxiolysis, sedation, and modest analgesia effects [2] .
|
-
-
- HY-17034AS
-
(+)-Medetomidine-13C,d3 hydrochloride; (S)-Medetomidine-13C,d3 hydrochloride
|
Isotope-Labeled Compounds
Adrenergic Receptor
|
Neurological Disease
Endocrinology
Cancer
|
Dexmedetomidine- 13C,d3 (hydrochloride) is the 13C- and deuterium labeled Dexmedetomidine (hydrochloride). Dexmedetomidine hydrochloride ((+)-Medetomidine hydrochloride) is a potent, selective and orally active agonist of α2-adrenoceptor, with a Ki of 1.08 nM. Dexmedetomidine hydrochloride shows 1620-fold selectivity against α1-adrenoceptor. Dexmedetomidine hydrochloride exhibits anxiolysis, sedation, and modest analgesia effects[1][2][3].
|
-
-
- HY-B0354AR
-
|
5-HT Receptor
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
Urapidil (hydrochloride) (Standard) is the analytical standard of Urapidil (hydrochloride). This product is intended for research and analytical applications. Urapidil hydrochloride is an orally active α1-adrenoceptor antagonist and 5-HT1A receptor agonist with a pIC50 of 6.13 and 4.38 against α1- and α2-adrenoceptor, respectively. Urapidil hydrochloride shows antihypertensive effect [2].
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-
-
- HY-B0352S2
-
-
-
- HY-B0352R
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Org3770 (Standard); 6-Azamianserin (Standard)
|
5-HT Receptor
Histamine Receptor
Adrenergic Receptor
|
Neurological Disease
Inflammation/Immunology
Cancer
|
Mirtazapine (Standard) is the analytical standard of Mirtazapine. This product is intended for research and analytical applications. Mirtazapine (Org3770) is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent. Mirtazapine is also a 5-HT2, 5-HT3, histamine H1 receptor and α2-adrenoceptor antagonist with pKi values of 8.05, 8.1, 9.3 and 6.95, respectively [2].
|
-
-
- HY-161836
-
|
Adrenergic Receptor
|
Cardiovascular Disease
|
α2AR agonist 1 (compound S6a), a new morpholine-containing pyrimidinone, acts as an agonist of α2-adrenoceptor. α2AR agonist 1 induces a concentration-dependent relaxation on aortic ring pre-contracted with Phenylephrine (HY-B0769; pEC50=6.81). α2AR agonist 1 increases NOx and NO levels in HUVECs .
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-
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- HY-101338
-
|
Adrenergic Receptor
|
Neurological Disease
|
RS-79948-197 is a non-imidazoline α2-adrenoceptor antagonist. RS-79948-197 shows Kd values of 0.42 nM, 0.18 nM, 0.19 nM, 0.60 nM, 0.46 nM, and 0.77 nM for rat α2A, rat α2B, rat α2C, human α2A, human α2B, and human α2C, respectively [2].
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-
-
- HY-101392S
-
|
Imidazoline Receptor
Monoamine Oxidase
Adrenergic Receptor
|
Neurological Disease
Cancer
|
Harmane-d is the deuterium labeled Harmane. Harmane, a β-Carboline alkaloid (BCA), is a potent neurotoxin that causes severe action tremors and psychiatric manifestations. Harmane shows 1000-fold selectivity for I1-Imidazoline receptor (IC50=30 nM) over α2-adrenoceptor (IC50=18 μM). Harmane is also a potent and selective inhibitor of monoamine oxidase (MAO) (IC50s=0.5 and 5 μM for human MAO A/B, respectively)[1][2][3][4].
|
-
-
- HY-101392S1
-
|
Isotope-Labeled Compounds
Imidazoline Receptor
Monoamine Oxidase
Adrenergic Receptor
|
Neurological Disease
Cancer
|
Harmane-d2 is the deuterium labeled Harmane. Harmane, a β-Carboline alkaloid (BCA), is a potent neurotoxin that causes severe action tremors and psychiatric manifestations. Harmane shows 1000-fold selectivity for I1-Imidazoline receptor (IC50=30 nM) over α2-adrenoceptor (IC50=18 μM). Harmane is also a potent and selective inhibitor of monoamine oxidase (MAO) (IC50s=0.5 and 5 μM for human MAO A/B, respectively)[1][2][3][4].
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- HY-101392R
-
|
Imidazoline Receptor
Monoamine Oxidase
Adrenergic Receptor
|
Neurological Disease
Cancer
|
Harmane (Standard) is the analytical standard of Harmane. This product is intended for research and analytical applications. Harmane, a β-Carboline alkaloid (BCA), is a potent neurotoxin that causes severe action tremors and psychiatric manifestations. Harmane shows 1000-fold selectivity for I1-Imidazoline receptor (IC50=30 nM) over α2-adrenoceptor (IC50=18 μM). Harmane is also a potent and selective inhibitor of monoamine oxidase (MAO) (IC50s=0.5 and 5 μM for human MAO A/B, respectively). Harmane exhibits comutagenic effect [2] .
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-
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- HY-101683
-
-
-
- HY-100850
-
-
-
- HY-12707
-
-
-
- HY-12707A
-
-
-
- HY-12707C
-
-
-
- HY-12707B
-
-
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- HY-N1163
-
-
-
- HY-106769
-
-
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- HY-106769C
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GR50360 hydrochloride
|
Adrenergic Receptor
|
Neurological Disease
|
Fluparoxan hydrochloride is an orally active, selective and competitive alpha 2-adrenoceptor antagonist. Fluparoxan hydrochloride is an anti-depressant agent [2].
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-
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- HY-160932
-
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Others
|
Endocrinology
|
RS-15385-198 is the enantiomer of Delequamine (RS-15385-197) (HY-106874). RS-15385-198 exhibits a pKi of 6.32 for α2-adrenoceptors in the rat cortex. RS-15385-198 is an antagonist for UK-14304 (HY-B0659) in the rat vas deferens and in the guinea-pig ileum .
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-
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- HY-B0528A
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(±)-p-Octopamine hydrochloride
|
Adrenergic Receptor
Endogenous Metabolite
|
Neurological Disease
Endocrinology
|
Octopamine ((±)-p-Octopamine) hydrochloride, a biogenic monoamine structurally related to noradrenaline, acts as a neurohormone, a neuromodulator and a neurotransmitter in invertebrates. Octopamine hydrochloride can stimulate alpha2-adrenoceptors (ARs) in Chinese hamster ovary cells transfected with human alpha2-ARs. Octopamine hydrochloride increased glycogenolysis, glycolysis, oxygen uptake, gluconeogenesis and the portal perfusion pressure [2] .
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-
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- HY-106874
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RS-15385-197
|
Adrenergic Receptor
|
Neurological Disease
|
Delequamine (RS-15385-197) is an orally active and selective α2-adrenergic receptor antagonist with a pKi of 9.5 for α2-adrenoceptors in rat cortex. Delequamine shows >1000 fold selectivity against 5-HT1A receptors and α1-adrenoceptors. Delequamine can be used for the study of erectile dysfunction .
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- HY-12707R
-
|
Dopamine Receptor
Adrenergic Receptor
Histone Methyltransferase
|
Neurological Disease
Endocrinology
Cancer
|
Piribedil (Standard) is the analytical standard of Piribedil. This product is intended for research and analytical applications. Piribedil is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil is also a α2-adrenoceptors antagonist. Piribedil can inhibit MLL1 methyltransferase activity (EC50: 0.18 μM). Piribedil has the potential for the research of parkinson's disease, circulatory disorders, cancers [2] .
|
-
- HY-121312
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ST-600
|
Adrenergic Receptor
|
Cardiovascular Disease
|
Flutonidine (ST-600) is a Clonidine (HY-12721) analogue that shows antihypertensive and sympatholytic effects. The initial hypertension produced by Flutonidine is due to stimulation of the peripheral α1, α2 adrenoceptors and the subsequent fall in blood pressure is due to the stimulation of central α2 adrenoceptors. Flutonidine reduces the arrhythmogenic and lethal effects of ouabain. Flutonidine is promising for research of ventricular arrhythmias caused by cardiac glycosides [2].
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- HY-106874A
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RS-15385-197 hydrochloride
|
Adrenergic Receptor
|
Neurological Disease
|
Delequamine (RS-15385-197) hydrochloride is an orally active and selective α2-adrenergic receptor antagonist with a pKi of 9.5 for α2-adrenoceptors in rat cortex. Delequamine hydrochloride shows >1000 fold selectivity against 5-HT1A receptors and α1-adrenoceptors. Delequamine hydrochloride can be used for the study of erectile dysfunction .
|
-
- HY-B0528AS
-
(±)-p-Octopamine-d4 hydrochloride
|
Adrenergic Receptor
Endogenous Metabolite
|
Neurological Disease
Endocrinology
|
Octopamine-d4 (hydrochloride) is the deuterium labeled Octopamine hydrochloride. Octopamine ((±)-p-Octopamine) hydrochloride, a biogenic monoamine structurally related to noradrenaline, acts as a neurohormone, a neuromodulator and a neurotransmitter in invertebrates. Octopamine hydrochloride can stimulate alpha2-adrenoceptors (ARs) in Chinese hamster ovary cells transfected with human alpha2-ARs. Octopamine hydrochloride increased glycogenolysis, glycolysis, oxygen uptake, gluconeogenesis and the portal perfusion pressure[1][2][3].
|
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- HY-B0528AR
-
|
Adrenergic Receptor
Endogenous Metabolite
|
Neurological Disease
Endocrinology
|
Octopamine (hydrochloride) (Standard) is the analytical standard of Octopamine (hydrochloride). This product is intended for research and analytical applications. Octopamine ((±)-p-Octopamine) hydrochloride, a biogenic monoamine structurally related to noradrenaline, acts as a neurohormone, a neuromodulator and a neurotransmitter in invertebrates. Octopamine hydrochloride can stimulate alpha2-adrenoceptors (ARs) in Chinese hamster ovary cells transfected with human alpha2-ARs. Octopamine hydrochloride increased glycogenolysis, glycolysis, oxygen uptake, gluconeogenesis and the portal perfusion pressure [2] .
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- HY-101690
-
-
- HY-106973A
-
CHF 1035
|
Dopamine Receptor
Adrenergic Receptor
|
Cardiovascular Disease
|
Nolomirole (CHF 1035) hydrochloride is an orally active and selective DA2 dopaminergic receptor/α2-adrenoceptor agonist. Nolomirole attenuates the heart failure signs in the Monocrotaline (HY-N0750)-induced congestive heart failure model. Nolomirole increases cardiac output [2].
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- HY-N3298
-
|
Adrenergic Receptor
|
Cardiovascular Disease
Neurological Disease
|
Meranzin is an absorbed bioactive compound from the Traditional Chinese Medicine (TCM) Chaihu-Shugan-San (CSS). Meranzin, isolated from leaves of Murraya exotica L., regulates the shared alpha 2-adrenoceptor and involves the AMPA-ERK1/2–BDNF signaling pathway. Meranzin has the potential for the prevention of the comorbidity of atherosclerosis and depression [2].
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-
- HY-103197
-
RX821002 hydrochloride
|
Adrenergic Receptor
|
Neurological Disease
|
2-Methoxyidazoxan monohydrochloride (RX821002 hydrochloride) is a highly selective alpha 2-adrenoceptor antagonist with little or no imidazoline antagonist effect. RX 821002 has markedly higher affinity for (guinea-pig) alpha 2D-adrenoceptors (pKd 9.7) than for (rabbit) alpha 2A-adrenoceptors (pKd 8.2) [2].
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- HY-B0371D
-
|
Adrenergic Receptor
|
Endocrinology
|
(S)-Terazosin is an active S-enantiomer of Terazosin. (S)-Terazosin is a potent and high-affinity α-adrenoceptor antagonist with Ki values of 3.91 nM, 0.79 nM and 1.16 nM for α1a, α1b and α1d-adrenoceptor, respectively. (S)-Terazosin also has high-affinity for α2a, α2B and α2c-adrenoceptor with Ki values of 729 nM, 3.5 nM and 46.4 nM, respectively .
|
-
- HY-103212
-
B-HT 933 dihydrochloride; Oxazoloazepin dihydrochloride
|
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
Azepexole (B-HT 933) dihydrochloride is a potent and selective alpha 2-adrenoceptor agonist with pKis of 8.3, 7.6, and 7.5 for α2A-, α2B- and α2C-adrenoceptor subtypes, resepctively . Azepexole dihydrochloride causes concentration-dependent inhibition of peristaltic contractions (IC50= 78.72 nM) [2].
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- HY-103212A
-
B-HT 933 hydrochloride; Oxazoloazepin hydrochloride
|
Adrenergic Receptor
|
Cardiovascular Disease
|
Azepexole hydrochloride (B-HT 933 dihydrochloride; Oxazoloazepin dihydrochloride) is a selective agonist for α 2-adrenoceptor, with pKi of 8.3, 7.6, and 7.5 for α2A-, α2B- and α2C-adrenoceptor subtypes, resepctively. Azepexole dihydrochloride causes concentration-dependent inhibition of peristaltic contractions with IC50 of 78.72 nM. Azepexole hydrochloride exhibits antitussive and analgesic efficacy [2].
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- HY-B0371B
-
|
Adrenergic Receptor
|
Endocrinology
|
(R)-Terazosin is an active R-enantiomer of Terazosin. (R)-Terazosin is a potent α1-adrenoceptor antagonist with Ki values of 6.51 nM, 1.01 nM and 1.97 nM for α1a, α1b and α1d-adrenoceptor, respectively .
|
-
- HY-100490
-
|
Imidazoline Receptor
Adrenergic Receptor
Apoptosis
Autophagy
|
Cardiovascular Disease
Cancer
|
Rilmenidine, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine is an alpha 2-adrenoceptor agonist. Rilmenidine induces autophagy. Rilmenidine acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na +/H + antiport. Rilmenidine modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells [2] .
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- HY-100490B
-
|
Imidazoline Receptor
Adrenergic Receptor
Apoptosis
Autophagy
|
Cardiovascular Disease
Cancer
|
Rilmenidine phosphate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine phosphate is an alpha 2-adrenoceptor agonist. Rilmenidine phosphate induces autophagy. Rilmenidine phosphate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na +/H + antiport. Rilmenidine phosphate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells [2] .
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- HY-N3298R
-
|
Adrenergic Receptor
|
Cardiovascular Disease
Neurological Disease
|
Meranzin (Standard) is the analytical standard of Meranzin. This product is intended for research and analytical applications. Meranzin is an absorbed bioactive compound from the Traditional Chinese Medicine (TCM) Chaihu-Shugan-San (CSS). Meranzin, isolated from leaves of Murraya exotica L., regulates the shared alpha 2-adrenoceptor and involves the AMPA-ERK1/2–BDNF signaling pathway. Meranzin has the potential for the prevention of the comorbidity of atherosclerosis and depression [2].
|
-
- HY-100490A
-
|
Imidazoline Receptor
Adrenergic Receptor
Apoptosis
Autophagy
|
Cardiovascular Disease
Cancer
|
Rilmenidine hemifumarate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine hemifumarate is an alpha 2-adrenoceptor agonist. Rilmenidine hemifumarate induces autophagy. Rilmenidine hemifumarate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na +/H + antiport. Rilmenidine hemifumarate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells [2] .
|
-
- HY-100490S
-
|
Isotope-Labeled Compounds
Imidazoline Receptor
Adrenergic Receptor
Apoptosis
Autophagy
|
Cardiovascular Disease
Cancer
|
Rilmenidine-d4 is the deuterium labeled Rilmenidine. Rilmenidine, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine is an alpha 2-adrenoceptor agonist. Rilmenidine induces autophagy. Rilmenidine acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells[1][2][3].
|
-
- HY-101392
-
Harmane
1 Publications Verification
|
Imidazoline Receptor
Monoamine Oxidase
Adrenergic Receptor
nAChR
GABA Receptor
Opioid Receptor
|
Neurological Disease
Inflammation/Immunology
|
Harmane is an inhibitor that binds to benzodiazepine receptors (with an IC50 value of 7 μM), has an IC50 of 24 μM for muscarinic acetylcholine receptors (QNB), an IC50 of 2.8 μM for opioid receptors, and IC50 values of 163 and 101 μM for spironolactone and serotonin, respectively. Harmane is a selective monoamine oxidase inhibitor (with IC50 values of 0.5 μM for MAO A and 5 μM for MAO B). Harman inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing levodopa (L-DOPA)-induced toxicity in PC12 cells. Harmane lowers blood pressure in rats through the I1 imidazoline receptor (I1 receptor) and has antidepressant, anxiolytic, anticonvulsant, and analgesic effects. Harmane enhances the mutagenicity induced by 2-acetylaminofluorene (AAF) [2] .
|
-
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-12710
-
-
-
- HY-N1163
-
-
-
- HY-B0528A
-
-
-
- HY-N3298
-
-
-
- HY-101392
-
Harmane
1 Publications Verification
|
Alkaloids
Structural Classification
other families
Source classification
Pyridine Alkaloids
Plants
Indole Alkaloids
|
Imidazoline Receptor
Monoamine Oxidase
Adrenergic Receptor
nAChR
GABA Receptor
Opioid Receptor
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Harmane is an inhibitor that binds to benzodiazepine receptors (with an IC50 value of 7 μM), has an IC50 of 24 μM for muscarinic acetylcholine receptors (QNB), an IC50 of 2.8 μM for opioid receptors, and IC50 values of 163 and 101 μM for spironolactone and serotonin, respectively. Harmane is a selective monoamine oxidase inhibitor (with IC50 values of 0.5 μM for MAO A and 5 μM for MAO B). Harman inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing levodopa (L-DOPA)-induced toxicity in PC12 cells. Harmane lowers blood pressure in rats through the I1 imidazoline receptor (I1 receptor) and has antidepressant, anxiolytic, anticonvulsant, and analgesic effects. Harmane enhances the mutagenicity induced by 2-acetylaminofluorene (AAF) [2] .
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- HY-136935
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- HY-101392R
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Structural Classification
Alkaloids
other families
Source classification
Plants
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Imidazoline Receptor
Monoamine Oxidase
Adrenergic Receptor
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Harmane (Standard) is the analytical standard of Harmane. This product is intended for research and analytical applications. Harmane, a β-Carboline alkaloid (BCA), is a potent neurotoxin that causes severe action tremors and psychiatric manifestations. Harmane shows 1000-fold selectivity for I1-Imidazoline receptor (IC50=30 nM) over α2-adrenoceptor (IC50=18 μM). Harmane is also a potent and selective inhibitor of monoamine oxidase (MAO) (IC50s=0.5 and 5 μM for human MAO A/B, respectively). Harmane exhibits comutagenic effect [2] .
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- HY-B0528AR
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Structural Classification
Monophenols
Source classification
Phenols
Endogenous metabolite
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Adrenergic Receptor
Endogenous Metabolite
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Octopamine (hydrochloride) (Standard) is the analytical standard of Octopamine (hydrochloride). This product is intended for research and analytical applications. Octopamine ((±)-p-Octopamine) hydrochloride, a biogenic monoamine structurally related to noradrenaline, acts as a neurohormone, a neuromodulator and a neurotransmitter in invertebrates. Octopamine hydrochloride can stimulate alpha2-adrenoceptors (ARs) in Chinese hamster ovary cells transfected with human alpha2-ARs. Octopamine hydrochloride increased glycogenolysis, glycolysis, oxygen uptake, gluconeogenesis and the portal perfusion pressure [2] .
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- HY-N3298R
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Structural Classification
other families
Source classification
Coumarins
Phenylpropanoids
Plants
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Adrenergic Receptor
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Meranzin (Standard) is the analytical standard of Meranzin. This product is intended for research and analytical applications. Meranzin is an absorbed bioactive compound from the Traditional Chinese Medicine (TCM) Chaihu-Shugan-San (CSS). Meranzin, isolated from leaves of Murraya exotica L., regulates the shared alpha 2-adrenoceptor and involves the AMPA-ERK1/2–BDNF signaling pathway. Meranzin has the potential for the prevention of the comorbidity of atherosclerosis and depression [2].
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Cat. No. |
Product Name |
Chemical Structure |
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- HY-101392S
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Harmane-d is the deuterium labeled Harmane. Harmane, a β-Carboline alkaloid (BCA), is a potent neurotoxin that causes severe action tremors and psychiatric manifestations. Harmane shows 1000-fold selectivity for I1-Imidazoline receptor (IC50=30 nM) over α2-adrenoceptor (IC50=18 μM). Harmane is also a potent and selective inhibitor of monoamine oxidase (MAO) (IC50s=0.5 and 5 μM for human MAO A/B, respectively)[1][2][3][4].
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- HY-B0528AS
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Octopamine-d4 (hydrochloride) is the deuterium labeled Octopamine hydrochloride. Octopamine ((±)-p-Octopamine) hydrochloride, a biogenic monoamine structurally related to noradrenaline, acts as a neurohormone, a neuromodulator and a neurotransmitter in invertebrates. Octopamine hydrochloride can stimulate alpha2-adrenoceptors (ARs) in Chinese hamster ovary cells transfected with human alpha2-ARs. Octopamine hydrochloride increased glycogenolysis, glycolysis, oxygen uptake, gluconeogenesis and the portal perfusion pressure[1][2][3].
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- HY-B0352S3
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Mirtazapine-d4 hydrochloride is deuterated labeled Mirtazapine (HY-B0352). Mirtazapine (Org3770) is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent. Mirtazapine is also a 5-HT2, 5-HT3, histamine H1 receptor and α2-adrenoceptor antagonist with pKi values of 8.05, 8.1, 9.3 and 6.95, respectively [2].
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- HY-B0409S
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Clonidine-d4 is the deuterium labeled Clonidine. Clonidine hydrochloride is an agonist of α2-adrenoceptor and potent antihypertensive agent[1][2][3][4][5].
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- HY-17034BS1
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Medetomidine-13C,d3 (hydrochloride) is a deuterated labeled Medetomidine (hydrochloride) . Medetomidine hydrochloride is an orally active α2-adrenoceptor agonist (Ki: 1.08 nM). Medetomidine hydrochloride has sedative and analgesic effects. Medetomidine hydrochloride can cause peripheral vasoconstriction through the activation of α2 adrenoceptors on blood vessels [2] .
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- HY-17034AS
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Dexmedetomidine- 13C,d3 (hydrochloride) is the 13C- and deuterium labeled Dexmedetomidine (hydrochloride). Dexmedetomidine hydrochloride ((+)-Medetomidine hydrochloride) is a potent, selective and orally active agonist of α2-adrenoceptor, with a Ki of 1.08 nM. Dexmedetomidine hydrochloride shows 1620-fold selectivity against α1-adrenoceptor. Dexmedetomidine hydrochloride exhibits anxiolysis, sedation, and modest analgesia effects[1][2][3].
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- HY-B0352S2
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Mirtazapine-d4 is deuterium labeled Mirtazapine. Mirtazapine (Org3770) is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent. Mirtazapine is also a 5-HT2, 5-HT3, histamine H1 receptor and α2-adrenoceptor antagonist with pKi values of 8.05, 8.1, 9.3 and 6.95, respectively[1][2].
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- HY-101392S1
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Harmane-d2 is the deuterium labeled Harmane. Harmane, a β-Carboline alkaloid (BCA), is a potent neurotoxin that causes severe action tremors and psychiatric manifestations. Harmane shows 1000-fold selectivity for I1-Imidazoline receptor (IC50=30 nM) over α2-adrenoceptor (IC50=18 μM). Harmane is also a potent and selective inhibitor of monoamine oxidase (MAO) (IC50s=0.5 and 5 μM for human MAO A/B, respectively)[1][2][3][4].
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- HY-100490S
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Rilmenidine-d4 is the deuterium labeled Rilmenidine. Rilmenidine, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine is an alpha 2-adrenoceptor agonist. Rilmenidine induces autophagy. Rilmenidine acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells[1][2][3].
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