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Results for "

α-2A adrenergic receptors

" in MedChemExpress (MCE) Product Catalog:

29

Inhibitors & Agonists

3

Isotope-Labeled Compounds

Targets Recommended:
Cat. No. 상품명 Target 연구분야 Chemical Structure
  • HY-B0527A
    Amitriptyline hydrochloride
    Maximum Cited Publications
    8 Publications Verification

    		 Serotonin Transporter 5-HT Receptor mAChR Histamine Receptor Adrenergic Receptor Trk Receptor Sodium Channel Potassium Channel Dopamine Transporter Apoptosis Neurological Disease Inflammation/Immunology Endocrinology
    Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with Ki = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity .
    Amitriptyline hydrochloride
  • HY-B0527
    Amitriptyline
    Maximum Cited Publications
    8 Publications Verification

    		 Serotonin Transporter Trk Receptor Sodium Channel 5-HT Receptor Histamine Receptor Adrenergic Receptor mAChR Potassium Channel Dopamine Transporter Apoptosis Neurological Disease Inflammation/Immunology Endocrinology
    Amitriptyline is an orally active tricyclic antidepressant (TCA). Amitriptyline mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline can reduce inflammation, angiogenesis and fibrosis. Amitriptyline binds to DAT (with Ki = 2.58 μM). Amitriptyline has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity .
    Amitriptyline
  • HY-B1052
    Lofexidine hydrochloride

    Baq-168; MDL-14042

    		 Adrenergic Receptor Imidazoline Receptor Neurological Disease Metabolic Disease
    Lofexidine hydrochloride (Baq-168) is an orally active agonist of the imidazoline I1 receptor (imidazoline I1 receptor) (Ki: 1.9 nM) and α2-adrenergic receptor (α2-adrenergic receptor). Lofexidine hydrochloride binds to the α2A-adrenergic receptor, reduces sympathetic outflow, lowers blood pressure, and exhibits vasoconstrictive effects. Lofexidine hydrochloride regulates the expression of c-fos and alleviates opioid withdrawal symptoms. Lofexidine hydrochloride is applicable to research on opioid addiction and withdrawal .
    Lofexidine hydrochloride
  • HY-12716A
    BRL-44408 maleate

    		Adrenergic Receptor ERK p38 MAPK Dopamine Receptor Cardiovascular Disease Neurological Disease
    BRL-44408 maleate is a selective, blood-brain barrier-permeable α2A-adrenergic receptor antagonist with a Ki value of 8.56 nM against human targets. BRL-44408 maleate exhibits activities such as antidepressant, analgesic effects and attenuation of sepsis-induced acute lung injury by regulating the release of neurotransmitters such as norepinephrine and dopamine, or inhibiting signaling pathways including ERK1/2, p38MAPK and p65. BRL-44408 maleate can be used in studies related to acute respiratory distress syndrome, depression and visceral pain .
    BRL-44408 maleate
  • HY-B1052A
    Lofexidine

    Baq-168 free base; MDL-14042 free base

    		 Imidazoline Receptor Adrenergic Receptor Neurological Disease Metabolic Disease
    Lofexidine (Baq-168 free base) is an orally active agonist of the imidazoline I1 receptor (imidazoline I1 receptor) (Ki: 1.9 nM) and α2-adrenergic receptor (α2-adrenergic receptor). Lofexidine binds to the α2A-adrenergic receptor, reduces sympathetic outflow, lowers blood pressure, and exhibits vasoconstrictive effects. Lofexidine regulates the expression of c-fos and alleviates opioid withdrawal symptoms. Lofexidine is applicable to research on opioid addiction and withdrawal .
    Lofexidine
  • HY-B0527AR
    Amitriptyline hydrochloride (Standard)
    4 Publications Verification

    		 Reference Standards Serotonin Transporter 5-HT Receptor Histamine Receptor mAChR Adrenergic Receptor Trk Receptor Sodium Channel Potassium Channel Dopamine Transporter Apoptosis Neurological Disease Inflammation/Immunology Endocrinology
    Amitriptyline hydrochloride (Standard) is the analytical standard of Amitriptyline hydrochloride (HY-B0527A). This product is intended for research and analytical applications. Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with Ki = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity.
    Amitriptyline hydrochloride (Standard)
  • HY-101610
    OPC-28326

    		Adrenergic Receptor Cardiovascular Disease Endocrinology
    OPC-28326 is a selective peripheral vasodilator and an angatonist of α2-adrenergic receptor, with Ki of 2040, 285, and 55 nM for α2A-, α2B- and α2C-adrenoceptors, respectively.
    OPC-28326
  • HY-B0527AS
    Amitriptyline-d6 hydrochloride

    		Isotope-Labeled Compounds Serotonin Transporter 5-HT Receptor Histamine Receptor mAChR Adrenergic Receptor Trk Receptor Sodium Channel Potassium Channel Dopamine Transporter Apoptosis Neurological Disease Inflammation/Immunology Endocrinology
    Amitriptyline-d6 hydrochloride is the deuterium labeled Amitriptyline hydrochloride (HY-B0527A). Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with Ki = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity.
    Amitriptyline-d6 hydrochloride
  • HY-U00123A
    Guanoxabenz hydrochloride

    Hydroxyguanabenz hydrochloride

    		 Adrenergic Receptor Neurological Disease
    Guanoxabenz (Hydroxyguanabenz) hydrochloride is an α2 adrenergic receptor agonist, with a Ki of 4000 nM and the fully activated form 40 nM for an α2A adrenoceptor .
    Guanoxabenz hydrochloride
  • HY-B1052S
    Lofexidine-d4 hydrochloride

    Baq-168-d4; MDL-14042-d4

    		 Isotope-Labeled Compounds Imidazoline Receptor Adrenergic Receptor Neurological Disease Metabolic Disease
    Lofexidine-d4 hydrochloride (Baq-168-d4) is the deuterium labeled Lofexidine hydrochloride (HY-B1052). Lofexidine hydrochloride (Baq-168) is an orally active agonist of the imidazoline I1 receptor (imidazoline I1 receptor) (Ki: 1.9 nM) and α2-adrenergic receptor (α2-adrenergic receptor). Lofexidine hydrochloride binds to the α2A-adrenergic receptor, reduces sympathetic outflow, lowers blood pressure, and exhibits vasoconstrictive effects. Lofexidine hydrochloride regulates the expression of c-fos and alleviates opioid withdrawal symptoms. Lofexidine hydrochloride is applicable to research on opioid addiction and withdrawal .
    Lofexidine-d4 hydrochloride
  • HY-12716
    BRL-44408

    		Adrenergic Receptor p38 MAPK Dopamine Receptor ERK Cardiovascular Disease Neurological Disease
    BRL-44408 is a selective, blood-brain barrier-permeable α2A-adrenergic receptor antagonist with a Ki value of 8.56 nM against human targets. BRL-44408 exhibits activities such as antidepressant, analgesic effects and attenuation of sepsis-induced acute lung injury by regulating the release of neurotransmitters such as norepinephrine and dopamine, or inhibiting signaling pathways including ERK1/2, p38MAPK and p65. BRL-44408 can be used in studies related to acute respiratory distress syndrome, depression and visceral pain .
    BRL-44408
  • HY-U00117
    Lusaperidone

    R107474

    		 Adrenergic Receptor Neurological Disease Endocrinology
    Lusaperidone (R107474) is an α2 adrenergic receptor antagonist with Kis of 0.13 and 0.15 nM for α2A and α2C, respectively.
    Lusaperidone
  • HY-U00244
    Benzquinamide

    P2647; BZQ; Benzoquinamide

    		 Adrenergic Receptor Dopamine Receptor Metabolic Disease
    Benzquinamide (P2647; BZQ; Benzoquinamide) is an orally active binder of dopamine receptors and adrenergic receptors. Benzquinamide specifically targets dopamine D2, D3, D4 receptors and α-2A, α-2B, α-2C adrenergic receptors. Benzquinamide regulates blood pressure and heart rate, attenuates the pressor effect of adrenaline, and exhibits activities such as antiemesis, anxiolysis, and reduction of histamine-induced bronchoconstriction. Benzquinamide has good safety and does not deplete serotonin or norepinephrine in the brain. Benzquinamide can be used in studies related to nausea/vomiting, mental disorders, anxiety states, neurosis, and psychosis .
    Benzquinamide
  • HY-117046
    AVN-101

    		5-HT Receptor Histamine Receptor Adrenergic Receptor Neurological Disease
    AVN-101 is a potent, brain-penetrant and orally active 5-HT7 receptor antagonist (Ki of 153 pM), with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors (Ki values of 2.04 nM, 1.56  nM, and 1.17  nM, respectively). AVN-101 also exhibits a rather high affinity toward histamine H1 (Ki of 0.58 nM) and adrenergic α2A, α2B, and α2C (Ki= 0.41-3.6 nM) receptors. AVN-101 can be studied in such diseases as general anxiety disorders, depression, schizophrenia, Alzheimer’s disease, and multiple sclerosis .
    AVN-101
  • HY-U00123
    Guanoxabenz

    Hydroxyguanabenz

    		 Adrenergic Receptor Cardiovascular Disease Endocrinology
    Guanoxabenz is an α2 adrenergic receptor agonist, with a Ki of 4000 nM and the fully activated form 40 nM for an α2A adrenoceptor .
    Guanoxabenz
  • HY-162620
    α2A-AR agonist 1

    		Adrenergic Receptor Cancer
    α2A-AR agonist 1 (Compound B9) is a selective agonist for α2-adrenergic receptor (α2A-AR) with EC50 of 0.23 nM. α2A-AR agonist 1 exhibits a hypnotic effect, with ED50 of 0.138 mg/kg in the loss of righting reflex (LORR) experiment. α2A-AR agonist 1 exhibits metabolic stability in mouse liver microsomes .
    α2A-AR agonist 1
  • HY-W042920A
    TDIQ hydrochloride

    		Adrenergic Receptor Neurological Disease
    TDIQ hydrochloride is an analog of Amphetamine with high affinity for α2-adrenergic receptor. TDIQ hydrochloride is a selective α2-adrenoceptor ligand with the Ki values of 75 nM, 95 nM, and 65 nM for α2A-, α2B-, and α2C-adrenergic receptors, respectively .
    TDIQ hydrochloride
  • HY-106444
    Fipamezole

    MPV 1730; JP-1730

    		 Adrenergic Receptor Neurological Disease
    Fipamezole (MPV 1730; JP-1730) is a potent and orally active α2-adrenergic receptor antagonist with Ki values of 9.2 nM, 17 nM, and 55 nM for human α2A, α2B, and α2C, receptors, respectively. Fipamezole is an anti-dyskinetic agent, and can be used for the study of Parkinson's disease .
    Fipamezole
  • HY-100300
    AGN 192836

    		Adrenergic Receptor Cardiovascular Disease Endocrinology
    AGN 192836 is a potent and selective α2 adrenergic agonist with EC50s of 8.7, 41 and 6.6 nM for α2A, α2B and α2C receptor, respectively.
    AGN 192836
  • HY-B1052R
    Lofexidine hydrochloride (Standard)

    Baq-168 (Standard); MDL-14042 (Standard)

    		 Adrenergic Receptor Reference Standards Neurological Disease Metabolic Disease
    Lofexidine (Baq-168) hydrochloride Standard is the analytical standard of Lofexidine hydrochloride (HY-B1052). This product is intended for research and analytical applications. Lofexidine hydrochloride (Baq-168) is an orally active agonist of the imidazoline I1 receptor (imidazoline I1 receptor) (Ki: 1.9 nM) and α2-adrenergic receptor (α2-adrenergic receptor). Lofexidine hydrochloride binds to the α2A-adrenergic receptor, reduces sympathetic outflow, lowers blood pressure, and exhibits vasoconstrictive effects. Lofexidine hydrochloride regulates the expression of c-fos and alleviates opioid withdrawal symptoms. Lofexidine hydrochloride is applicable to research on opioid addiction and withdrawal .
    Lofexidine hydrochloride (Standard)
  • HY-B1052S1
    Lofexidine-d4

    Baq-168 free base-d4; MDL-14042 free base-d4

    		 Isotope-Labeled Compounds Imidazoline Receptor Adrenergic Receptor Neurological Disease Metabolic Disease
    Lofexidine-d4 (Baq-168 free base-d4) is deuterium labeled Lofexidine (HY-B1052A). Lofexidine (Baq-168 free base) is an orally active agonist of the imidazoline I1 receptor (imidazoline I1 receptor) (Ki: 1.9 nM) and α2-adrenergic receptor (α2-adrenergic receptor). Lofexidine binds to the α2A-adrenergic receptor, reduces sympathetic outflow, lowers blood pressure, and exhibits vasoconstrictive effects. Lofexidine regulates the expression of c-fos and alleviates opioid withdrawal symptoms. Lofexidine is applicable to research on opioid addiction and withdrawal .
    Lofexidine-d4
  • HY-U00244A
    Benzquinamide hydrochloride

    P2647 hydrochloride; BZQ hydrochloride; Benzoquinamide hydrochloride

    		 Adrenergic Receptor Dopamine Receptor Neurological Disease
    Benzquinamide (P2647; BZQ; Benzoquinamide) hydrochloride is an orally active binder of dopamine receptors and adrenergic receptors. Benzquinamide hydrochloride specifically targets dopamine D2, D3, D4 receptors and α-2A, α-2B, α-2C adrenergic receptors. Benzquinamide hydrochloride regulates blood pressure and heart rate, attenuates the pressor effect of adrenaline, and exhibits activities such as antiemesis, anxiolysis, and reduction of histamine-induced bronchoconstriction. Benzquinamide hydrochloride has good safety and does not deplete serotonin or norepinephrine in the brain. Benzquinamide hydrochloride can be used in studies related to nausea/vomiting, mental disorders, anxiety states, neurosis, and psychosis .
    Benzquinamide hydrochloride
  • HY-117046A
    AVN-101 hydrochloride

    		5-HT Receptor Histamine Receptor Adrenergic Receptor Neurological Disease
    AVN-101 hydrochloride is a potent, brain-penetrant and orally active 5-HT7 receptor antagonist (Ki of 153 pM), with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors (Ki values of 2.04 nM, 1.56  nM, and 1.17  nM, respectively). AVN-101 hydrochloride also exhibits a rather high affinity toward histamine H1 (Ki of 0.58 nM) and adrenergic α2A, α2B, and α2C (Ki= 0.41-3.6 nM) receptors. AVN-101 hydrochloride can be studied in such diseases as general anxiety disorders, depression, schizophrenia, Alzheimer’s disease, and multiple sclerosis .
    AVN-101 hydrochloride
  • HY-106444A
    Fipamezole hydrochloride

    MPV-1730 hydrochloride; JP-1730 hydrochloride

    		 Adrenergic Receptor Neurological Disease
    Fipamezole hydrochloride is a potent and orally active α2-adrenergic receptor antagonist with Ki values of 9.2 nM, 17 nM, and 55 nM for human α2A, α2B, and α2C, receptors, respectively. Fipamezole hydrochloride is an anti-dyskinetic agent, and can be used for the study of Parkinson's disease .
    Fipamezole hydrochloride
  • HY-100300R
    AGN 192836 (Standard)

    		Adrenergic Receptor Reference Standards Cardiovascular Disease Endocrinology
    AGN 192836 (Standard) is the analytical standard of AGN 192836 (HY-100300). This product is intended for research and analytical applications. AGN 192836 is a potent and selective α2 adrenergic agonist with EC50s of 8.7, 41 and 6.6 nM for α2A, α2B and α2C receptor, respectively.
    AGN 192836 (Standard)
  • HY-182597
    Tracizoline

    		Imidazoline Receptor 5-HT Receptor Adrenergic Receptor Neurological Disease
    Tracizoline is an orally active I2-imidazoline receptor agonist. Tracizoline functionally modulates I2-imidazoline receptors, regulates hippocampal FADD cell fate adaptor, attenuates mechanical and thermal hyperalgesia, activates α2A-adrenergic receptors with very weak partial agonism, and induces antidepressant-like activity via 5-HT1A receptor activation. Tracizoline can be used for the research of inflammatory pain, neuropathic pain, and depression .
    Tracizoline
  • HY-100323
    AGN-201781

    		Adrenergic Receptor Neurological Disease
    AGN-201781 is an orally active α-2B adrenergic receptor agonist. AGN-201781 can be used in studies related to neuropathic pain .
    AGN-201781
  • HY-181878
    Z8779877149

    Z7149

    		 Serotonin Transporter Adrenergic Receptor 5-HT Receptor Neurological Disease
    Z8779877149 (Z7149) is a blood-brain barrier-permeable multi-target ligand that targets SERT (Ki=198 nM), α2A adrenergic receptor (Ki=180 nM; EC50=440 nM) and 5-HT2A receptor (EC50=172 nM, Emax=76%). Z8779877149 inhibits 5-HT reuptake and activates Gi and Gq protein signaling pathways, respectively. Z8779877149 effectively alleviates pain responses as well as depression- and anxiety-like behaviors, while exhibiting favorable safety without inducing sedation or motor impairment. Z8779877149 is available for the research of pain, depression and anxiety disorders .
    Z8779877149
  • HY-182091
    CYD-1-79

    		5-HT Receptor Dopamine Receptor Dopamine Transporter Adrenergic Receptor Calcium Channel Neurological Disease
    CYD-1-79 is a selective positive allosteric modulator of 5-HT2C receptor. CYD-1-79 potentiates 5-HT-evoked intracellular calcium release via a topographically distinct allosteric site. CYD-1-79 shows significant inhibition of binding at dopamine D3 receptor, DAT, and α2A/α2B adrenergic receptors. CYD-1-79 modulates 5-HT2C receptor-mediated spontaneous ambulation in rodents and synergizes with a low dose of a 5-HT2C receptor agonist. CYD-1-79 attenuates relapse vulnerability of psychoactive substance in a rodent self-administration model. CYD-1-79 can be used for the research of neurological disease .
    CYD-1-79

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