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Results for "

β subtype

" in MedChemExpress (MCE) Product Catalog:

84

Inhibitors & Agonists

2

Screening Libraries

1

Peptides

2

Inhibitory Antibodies

11

Natural
Products

11

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-P99020
    Fresolimumab
    1 Publications Verification

    GC1008

    		 TGF-beta/Smad Metabolic Disease Inflammation/Immunology Cancer
    Fresolimumab (GC1008) is a human monoclonal antibody against TGF-β that neutralizes all mammalian active subtypes of TGF-β. The binding affinity of Fresolimumab to TGF-β2 is 1.8 nM. Fresolimumab improves Bleomycin (HY-108345)-induced acute lung injury. Fresolimumab radiolabeled with 89Zr can be used for PET analysis of TGF-β expression, antibody uptake and organ distribution. Fresolimumab can be used in the study of cancer, osteogenesis imperfecta, fibrosis and kidney disease .
    Fresolimumab
  • HY-A0106
    Levamisole
    10+ Cited Publications

    (-)-Tetramisole

    		 nAChR Parasite Infection Inflammation/Immunology Cancer
    Levamisole ((-)-Levamisole), an anthelmintic agent with immunomodulatory properties. Levamisole acts as a positive allosteric modulator (PAM) for the α3β2 (EC50=300 μM) and α3β4 (EC50=100 μM) subtype of nAChRs. Orally active .
    Levamisole
  • HY-Y0313
    p-Hydroxybenzaldehyde

    		Endogenous Metabolite GABA Receptor Neurological Disease
    p-Hydroxybenzaldehyde is a one of the major components in vanilla aroma, with antagonistic effect on GABAA receptor of the α1β2γ2S subtype at high concentrations.
    p-Hydroxybenzaldehyde
  • HY-123012
    Lubabegron

    LY-488756

    		 Adrenergic Receptor Others
    Lubabegron is a potent modulator of β-adrenergic receptor (β-AR). Lubabegron demonstrates antagonistic behavior at the β1 and β 2 receptor subtypes and agonistic behavior at the β 3 receptor subtype in cattle. Lubabegron reduces NH3 gas emissions from an animal or its waste. Lubabegron is available as an animal supplement .
    Lubabegron
  • HY-W002112
    (±)-Nornicotine

    Nornicotine

    		 Endogenous Metabolite Drug Metabolite nAChR β-catenin Cardiovascular Disease Neurological Disease
    (±)-Nornicotine is a major metabolite of Nicotine. (±)-Nornicotine is a partial nAChRs agonist, specifically activating receptor subtypes containing α7 and α6 subunits. (±)-Nornicotine disrupts β-catenin and ZO-1, and induces F-actin depolymerization. (±)-Nornicotine supports self-administration behavior. (±)-Nornicotine can be used in the research of atherosclerosis, Alzheimer's disease, and schizophrenia .
    (±)-Nornicotine
  • HY-B2192
    Amylase

    		Amylases Metabolic Disease Cancer
    Amylase is an enzyme produced by pancreas and salivary glands, catalyzing the hydrolysis of starch into sugars. Amylase are broadly classified into α, β, and γ subtypes .
    Amylase
  • HY-P99017
    Eptinezumab

    ALD-403

    		 CGRP Receptor Neurological Disease
    Eptinezumab (ALD-403) is a human monoclonal antibody targeting the α and β subtypes of human calcitonin gene-related peptide (CGRP). Eptinezumab binds to the CGRP ligand and blocks its binding to endogenous CGRP receptors, thereby inhibiting receptor activation. Eptinezumab can be used in research related to migraine .
    Eptinezumab
  • HY-106353
    Smilagenin
    1 Publications Verification

    		 mAChR Endogenous Metabolite Neurological Disease
    Smilagenin (SMI) is a small-molecule steroidal sapogenin from Anemarrhena asphodeloides and Pelargonium hortorum widely used in traditional Chinese medicine for treating chronic neurodegeneration diseases . Smilagenin (SMI) improves memory of aged rats by increasing the muscarinic receptor subtype 1 (M1)-receptor density . Smilagenin (SMI) attenuates Aβ(25-35)-induced neurodegenerationvia stimulating the gene expression of brain-derived neurotrophic factor, may represents a novel therapeutic strategy for AD .
    Smilagenin
  • HY-W014589
    2,4-Di-tert-butylphenol
    2 Publications Verification

    2,4-DTBP

    		 Endogenous Metabolite Fungal Apoptosis RAR/RXR Amyloid-β Infection Neurological Disease Inflammation/Immunology Cancer
    2,4-Di-tert-butylphenol (2,4-DTBP) is an orally active RXRα activator and a human estrogen receptor ligand with anti-inflammatory and antioxidant activities, which can induce apoptosis in tumor cells. 2,4-Di-tert-butylphenol can activate the RXRα subtype in LXRα/RXRα, PPARγ/RXRα, and hormone receptor β/RXRα. 2,4-Di-tert-butylphenol also has antiviral and antifungal activities and has the potential to inhibit Aβ-induced neurotoxicity. 2,4-Di-tert-butylphenol can be used as an intermediate in the preparation of antioxidants and UV stabilizers, and is also used in the manufacture of drugs and fragrances .
    2,4-Di-tert-butylphenol
  • HY-100369A
    DMCM hydrochloride

    		GABA Receptor Neurological Disease
    DMCM hydrochloride is a nonselective full inverse agonist of benzodiazepine. DMCM shows bnding afinity at human recombinant GABAA αxβ3γ2 receptor subtypes with Kis of 10 nM, 13 nM, 7.5 nM, 2.2 nM for α1, α2, α3, and α5 receptors, respectively .
    DMCM hydrochloride
  • HY-15831
    L-838417-d9

    		Isotope-Labeled Compounds GABA Receptor Neurological Disease
    L-838417-d9 is the deuterium labeled L-838417 (HY-W009009). L-838417 is a selective partial agonist at the α2, α3 and α5 subtypes of the GABAA receptor and an antagonist at the α1, with binding Ki values of 0.79 nM, 0.67 nM, 1.67 nM, 267 nM, 2.25 nM and 2183 nM for α1β3γ2, α2β3γ2, α3β3γ2, α4β3γ2, α5β3γ2 and α6β3γ2. L-838417 has anti-anxiety activity .
    L-838417-d9
  • HY-13225B
    Rivanicline hemioxalate
    1 Publications Verification

    RJR-2403 hemioxalate; (E)-Metanicotine hemioxalate

    		 nAChR Neurological Disease
    Rivanicline (RJR-2403) hemioxalate is a neuronal nicotinic receptor agonist. Rivanicline hemioxalate is highly selective for the rat brain cortex nAChRs (Ki = 26 nM, EC50 of 732 nM) and α4β2 subtype (Ki = 26 nM, EC50 = 16 μM). Rivanicline hemioxalate can significantly restore the learning impairment and cognitive dysfunction. Rivanicline hemioxalate can be used for the study of neurodegenerative diseases (such as schizophrenia or Alzheimer's disease) .
    Rivanicline hemioxalate
  • HY-B1404
    Nylidrin hydrochloride

    Buphenine hydrochloride

    		 iGluR Influenza Virus Infection Cardiovascular Disease Inflammation/Immunology
    Nylidrin hydrochloride (Buphenine hydrochloride) is an orally active β-adrenergic agonist. Nylidrin hydrochloride antagonizes NR1A/2B NMDA receptors (IC50 = 0.18 μM in Xenopus oocytes). Nylidrin hydrochloride reduces the levels of NP, HA, and M1. Nylidrin hydrochloride has antiviral activity against multiple H1N1 subtype influenza A viruses. Nylidrin hydrochloride improves hemorrhagic shock and anti-allergic effects .
    Nylidrin hydrochloride
  • HY-110131
    A 85380 hydrochloride

    		nAChR Neurological Disease
    A 85380 hydrochloride is a novel, high affinity neuronal nicotinic acetylcholine receptor (nAChR) agonist. A 85380 hydrochloride exhibits selectivity for the α4β2 nAChR subtypes. A 85380 hydrochloride has a broad-spectrum analgesic profile .
    A 85380 hydrochloride
  • HY-163945
    ZTA-261

    		Thyroid Hormone Receptor Metabolic Disease
    ZTA-261 is a highly selective and low toxic thyroid hormone receptor β subtype (THR-β) agonist (IC50=6.3 nM) that reduces body weight and visceral fat through a liothyronine (HY-A0070A) mediated pathway. ZTA-261 can be used in the study of lipid metabolism and obesity prevalence .
    ZTA-261
  • HY-B1562B
    Bopindolol malonate

    (±)-Bopindolol malonate

    		 Adrenergic Receptor Renin 5-HT Receptor Cardiovascular Disease Neurological Disease
    Bopindolol ((±)-Bopindolol) malonate is an orally active antagonist of β-adrenoceptors (ARs) with partial agonist activity. Bopindolol malonate is non-selective for β1- and β2-ARs and has low affinity for β3-AR subtype. Bopindolol malonate has intrinsic sympathomimetic as well as membrane stabilizing actions, inhibits renin secretion, and interacts with 5-HT receptors. Bopindolol malonate is a proagent of Pindolol (HY-B0982). Bopindolol malonate can be used for essential and renovascular hypertension research.
    Bopindolol malonate
  • HY-136207
    TC-2559 difumarate

    		nAChR Neurological Disease
    TC-2559 idifumarate is a CNS-selective, orally active α4β2 subtype of nicotinic acetylcholine receptor (nAChR) partial agonist (EC50=0.18 μM). TC-2559 difumarate shows selectivity for α4β2 over α2β4, α4β4 and α3β4 receptors, with EC50s in the range of 10-30 µM. Antinociceptive effect .
    TC-2559 difumarate
  • HY-W009009
    L-838417

    		GABA Receptor Neurological Disease
    L-838417 is a selective partial agonist at the α2, α3 and α5 subtypes of the GABAA receptor and an antagonist at the α1, with binding Ki values of 0.79 nM, 0.67 nM, 1.67 nM, 267 nM, 2.25 nM and 2183 nM for α1β3γ2, α2β3γ2, α3β3γ2, α4β3γ2, α5β3γ2 and α6β3γ2. L-838417 has anti-anxiety activity .
    L-838417
  • HY-W014589R
    2,4-Di-tert-butylphenol (Standard)

    2,4-DTBP (Standard)

    		 Reference Standards Endogenous Metabolite Fungal Apoptosis RAR/RXR Amyloid-β Infection Neurological Disease Inflammation/Immunology Cancer
    2,4-Di-tert-butylphenol (Standard) is the analytical standard of 2,4-Di-tert-butylphenol (HY-W014589). This product is intended for research and analytical applications. 2,4-Di-tert-butylphenol (2,4-DTBP) is an orally active RXRα activator and a human estrogen receptor ligand with anti-inflammatory and antioxidant activities, which can induce apoptosis in tumor cells. 2,4-Di-tert-butylphenol can activate the RXRα subtype in LXRα/RXRα, PPARγ/RXRα, and hormone receptor β/RXRα. 2,4-Di-tert-butylphenol also has antiviral and antifungal activities, and has the potential to inhibit Aβ-induced neurotoxicity. 2,4-Di-tert-butylphenol can be used as an intermediate in the preparation of antioxidants and UV stabilizers, and is also used in the manufacture of pharmaceuticals and fragrances .
    2,4-Di-tert-butylphenol (Standard)
  • HY-W749327
    2,4-Di-tert-butylphenol-d21

    2,4-DTBP-d21

    		 Isotope-Labeled Compounds RAR/RXR Amyloid-β Fungal Apoptosis Endogenous Metabolite Infection Neurological Disease Inflammation/Immunology Cancer
    2,4-Di-tert-butylphenol-d21 (2,4-DTBP-d21) is the deuterium labeled 2,4-Di-tert-butylphenol (HY-W014589). 2,4-Di-tert-butylphenol (2,4-DTBP) is an orally active RXRα activator and a human estrogen receptor ligand with anti-inflammatory and antioxidant activities, which can induce apoptosis in tumor cells. 2,4-Di-tert-butylphenol can activate the RXRα subtype in LXRα/RXRα, PPARγ/RXRα, and hormone receptor β/RXRα. 2,4-Di-tert-butylphenol also has antiviral and antifungal activities and has the potential to inhibit Aβ-induced neurotoxicity. 2,4-Di-tert-butylphenol can be used as an intermediate in the preparation of antioxidants and UV stabilizers, and is also used in the manufacture of drugs and fragrances .
    2,4-Di-tert-butylphenol-d21
  • HY-W001692
    Ocinaplon

    DOV 273547

    		 GABA Receptor Neurological Disease
    Ocinaplon (DOV 273547) is an orally active positive allosteric modulator of GABAA receptor, with an EC50 ranging from 3.07 μM (α1β2γ2 subtype) to 10.03 μM (α1β2γ3 subtype). Ocinaplon enhances GABA-stimulated chloride currents across multiple GABAA receptor subtypes, with varying potency between different subtypes. Ocinaplon exerts anxiolytic and anticonvulsant effects, and causes motor impairment at high doses. Ocinaplon can be used for research on generalized anxiety disorder .
    Ocinaplon
  • HY-Y0313R
    p-Hydroxybenzaldehyde (Standard)

    		Reference Standards Endogenous Metabolite GABA Receptor Neurological Disease
    p-Hydroxybenzaldehyde (Standard) is the analytical standard of p-Hydroxybenzaldehyde. This product is intended for research and analytical applications. p-Hydroxybenzaldehyde is a one of the major components in vanilla aroma, with antagonistic effect on GABAA receptor of the α1β2γ2S subtype at high concentrations.
    p-Hydroxybenzaldehyde (Standard)
  • HY-135483A
    AR-R17779 hydrochloride

    		nAChR Neurological Disease
    AR-R17779 hydrochloride is a potent and selective full agonist of nAChR, with Kis of 92 and 16000 nM for α7 and α4β2 subtype, respectively. AR-R17779 hydrochloride can improve learning and memory in rats. AR-R17779 hydrochloride also has anxiolytic activity. AR-R17779 hydrochloride can reduce inflammation by activating antiinflammatory cholinergic (vagal) pathways .
    AR-R17779 hydrochloride
  • HY-W002112S
    (±)-Nornicotine-d4

    Nornicotine-d4

    		 nAChR Isotope-Labeled Compounds Endogenous Metabolite Drug Metabolite β-catenin Cardiovascular Disease Neurological Disease
    (±)-Nornicotine-d4 is the deuterium labeled (±)-Nornicotine (HY-W002112). (±)-Nornicotine is a major metabolite of Nicotine. (±)-Nornicotine is a partial nAChRs agonist, specifically activating receptor subtypes containing α7 and α6 subunits. (±)-Nornicotine disrupts β-catenin and ZO-1, and induces F-actin depolymerization. (±)-Nornicotine supports self-administration behavior. (±)-Nornicotine can be used in the research of atherosclerosis, Alzheimer's disease, and schizophrenia .
    (±)-Nornicotine-d4
  • HY-N12110
    SMU-CX1

    		Toll-like Receptor (TLR) SARS-CoV Infection
    SMU-CX1 is a specific TLR3 inhibitor (IC50: 0.11 μM) with IC50 ranging from 0.14-0.33 μM against multiple influenza A virus subtypes. SMU-CX1 inhibits the viral PB2 and NP proteins with an IC50 of 0.43 μM for SARS-CoV-2 activity. SMU-CX1 also inhibits inflammatory factors in host cells, including IFN-β, IP-10, and CCL-5 .
    SMU-CX1
  • HY-123012A
    Lubabegron fumarate

    LY-591281; LY-488756 fumarate

    		 Androgen Receptor Others
    Lubabegron fumarate is a potent modulator of β-adrenergic receptor (β-AR). Lubabegron fumarate demonstrates antagonistic behavior at the β1 and β 2 receptor subtypes and agonistic behavior at the β 3 receptor subtype in cattle. Lubabegron fumarate reduces NH3 gas emissions from an animal or its waste. Lubabegron fumarate is available as an animal supplement .
    Lubabegron fumarate
  • HY-Y0313S
    p-Hydroxybenzaldehyde-d4

    		Isotope-Labeled Compounds Endogenous Metabolite GABA Receptor Neurological Disease
    p-Hydroxybenzaldehyde-d4 is the deuterium labeled p-Hydroxybenzaldehyde. p-Hydroxybenzaldehyde is a one of the major components in Dendrocalamus asper bamboo shoots, with antagonistic effect on GABAA receptor of the α1β2γ2S subtype at high concentrations.
    p-Hydroxybenzaldehyde-d4
  • HY-13225A
    Rivanicline

    RJR-2403; (E)-Metanicotine

    		 nAChR Neurological Disease
    Rivanicline (RJR-2403) is a neuronal nicotinic receptor agonist. Rivanicline is highly selective for the rat brain cortex nAChRs (Ki = 26 nM, EC50 of 732 nM) and α4β2 subtype (Ki = 26 nM, EC50 = 16 μM). Rivanicline can significantly restore the learning impairment and cognitive dysfunction. Rivanicline can be used for the study of neurodegenerative diseases (such as schizophrenia or Alzheimer's disease) .
    Rivanicline
  • HY-175504
    MLS6357

    		Dopamine Receptor PERK Neurological Disease
    MLS6357 is a D3 dopamine receptor (D3R)-selective positive allosteric modulator (PAM)-antagonist. MLS6357 exhibits antagonist activity in the D3R-mediated and the BRET-based β-arrestin recruitment assay with IC50s of 13 and 14 μM, and no activity for other DAR subtypes (D1R/D2R/D4R/D5R) (IC50 > 100 μM). MLS6357 is also an antagonist in the D3R-mediated Go-BRET assay with an IC50 of 17 μM. MLS6357 can be used for the study of neuropsychiatric disorders, including substance use disorder .
    MLS6357
  • HY-169859
    EP4 receptor antagonist 7

    		Prostaglandin Receptor Interleukin Related Inflammation/Immunology Cancer
    EP4 receptor antagonist 7 (Compound 14) is an antagonist of the prostaglandin E2 (PGE2) receptor subtype EP4 with an IC50 value of 1.1 nM. EP4 receptor antagonist 7 inhibits PGE2-induced β-arrestin recruitment in HEK293 cells with an IC50 value of 0.9 nM. EP4 receptor antagonist 7 decreases PGE2-induced expression of mRNA encoding IL-4, macrophage mannose receptor 1 (Mrc1), chitinase-like protein 3 (Chil3), chemokine (C-X-C) motif ligand 1 (Cxcl1), triggering receptor expressed on myeloid cells 2 (Trem2), and arginase-1 (Arg1), in RAW 264.7 macrophages. EP4 receptor antagonist 7 combined with an anti-PD-1 antibody inhibits tumor growth and increases infiltration of CD 8+ T cells into tumors in a CT26 murine colon cancer model .
    EP4 receptor antagonist 7
  • HY-B1833R
    Afloqualone (Standard)

    HQ-495 (Standard)

    		 Reference Standards GABA Receptor Neurological Disease
    Afloqualone (Standard) is the analytical standard of Afloqualone. This product is intended for research and analytical applications. Afloqualone (HQ-495) is an orally active central muscle relaxant and antivertiginous agent that can increase the sensitivity of GABA receptors in neurons of the lateral vestibular nucleus. Afloqualone (HQ-495) can be used in the research of low back pain and neck-arm-shoulder syndrome .
    Afloqualone (Standard)
  • HY-168824
    Cypenamine hydrochloride

    		nAChR Neurological Disease
    Cypenamine hydrochloride is an antidepressant agent. Cypenamine binds to the human nAchR subtypes, α2β4, α3β4 and α4β4, with Ki values of 4.65 μM, 2.69 and 4.11 μM, respectively .
    Cypenamine hydrochloride
  • HY-14565
    Pozanicline

    ABT-089

    		 nAChR Neurological Disease
    Pozanicline (ABT-089) selectively activate neuronal nicotinic acetylcholine receptor (nAChR) subtypes, is a novel cholinergic agent that is a partial agonist at α4β2* nAChRs (Ki=16 nM) and shows high selectivity for α6β2* and α4α5β2 nAChR subtypes, the binding affinity (Ki, rat) for Pozanicline to [ 3H] cytisine sites is 16.7 nM. Pozanicline reverses nicotine withdrawal-induced cognitive deficits, may be an effective component of novel therapeutic strategies for nicotine addiction .
    Pozanicline
  • HY-14319B
    Sazetidine A dihydrochloride

    		nAChR Neurological Disease
    Sazetidine A dihydrochloride is a potent ligand for the α4β2 nAChR, with high binding affinity and selectivity for this subtype. Sazetidine A dihydrochloride exhibits favorable pharmacological properties and may contribute to research targeting nicotinic receptor-related diseases. Sazetidine A dihydrochloride has been mentioned in studies investigating the binding affinity of various analogs, highlighting its importance in understanding the nAChR ligand subtype selectivity .
    Sazetidine A dihydrochloride
  • HY-P5811
    Ceratotoxin-1

    CcoTx1; β-TRTX-cm1a

    		 Sodium Channel Neurological Disease
    Ceratotoxin-1 (CcoTx1), a peptide toxin, is an voltage-gated sodium channel subtypes inhibitor. Ceratotoxin-1 inhibits Nav1.1/β1, Nav1.2/β1, Nav1.4/β1, and Nav1.5/β1 with IC50 of 523 nM, 3 nM, 888 nM, and 323 nM, respectively. Ceratotoxin-1 also inhibits Nav1.8/β1 .
    Ceratotoxin-1
  • HY-Y0313S1
    p-Hydroxybenzaldehyde-13C

    		Isotope-Labeled Compounds Endogenous Metabolite GABA Receptor Neurological Disease
    p-Hydroxybenzaldehyde- 13C is the 13C-labeled p-Hydroxybenzaldehyde. p-Hydroxybenzaldehyde is a one of the major components in Dendrocalamus asper bamboo shoots, with antagonistic effect on GABAA receptor of the α1β2γ2S subtype at high concentrations.
    p-Hydroxybenzaldehyde-13C
  • HY-W747264
    P-Hydroxybenzaldehyde-13C6

    		Isotope-Labeled Compounds GABA Receptor Endogenous Metabolite Neurological Disease
    P-Hydroxybenzaldehyde- 13C6 is the 13C-labeled p-Hydroxybenzaldehyde (HY-Y0313). p-Hydroxybenzaldehyde is a one of the major components in vanilla aroma, with antagonistic effect on GABAA receptor of the α1β2γ2S subtype at high concentrations.
    P-Hydroxybenzaldehyde-13C6
  • HY-143279
    Topoisomerase II inhibitor 3

    		Topoisomerase Apoptosis Cancer
    Topoisomerase II inhibitor 3 (Compound 6 h ) is a acridone derivatives, as well as a Type II DNA topoisomerase (topo II) inhibitor , as a topo IIα/β inhibitor with the value of IC50 is 0.17 μM for topo IIα and the value of IC50 is 0.23 μM for topo IIβ subtypes, caused obvious DNA damage, and induced apoptosis by triggering the loss of mitochondrial membrane potential .
    Topoisomerase II inhibitor 3
  • HY-115766S
    Anabaseine-d4

    		Isotope-Labeled Compounds nAChR Neurological Disease
    Anabaseine-d4 is the deuterium labeled Anabaseine (HY-115766). Anabaseine is a non-selective nicotinic agonist. Anabaseine stimulates all AChRs, preferentially stimulates skeletal muscle and brain α7 subtypes . Anabaseine is also a weak partial agonist at α4β2 nAChRs .
    Anabaseine-d4
  • HY-131179
    Influenza A virus-IN-1

    		Influenza Virus Infection
    Influenza A virus-IN-1 is a dihydropyrrolidones derivative and is a potent inhibitor against wide subtypes of influenza A virus (IAV) with IC50 values from 3.11 μM to 7.13 μM. Influenza A virus-IN-1 efficiently inhibits replication of IAV, up-regulates the expression of key antiviral cytokines IFN-β and antiviral protein MxA .
    Influenza A virus-IN-1
  • HY-13225
    Rivanicline oxalate

    RJR-2403 oxalate; (E)-Metanicotine oxalate

    		 nAChR Neurological Disease
    Rivanicline (RJR-2403) oxalate is a neuronal nicotinic receptor agonist. Rivanicline oxalate is highly selective for the rat brain cortex nAChRs (Ki = 26 nM, EC50 of 732 nM) and α4β2 subtype (Ki = 26 nM, EC50 = 16 μM). Rivanicline oxalate can significantly restore the learning impairment and cognitive dysfunction. Rivanicline oxalate can be used for the study of neurodegenerative diseases (such as schizophrenia or Alzheimer's disease) .
    Rivanicline oxalate
  • HY-138879B
    CP-601932

    (1S,5R)-CP-601927

    		 nAChR Neurological Disease
    CP-601932 ((1S,5R)-CP-601927) is a high-affinity partial agonist at α3β4 nAChR (Ki=21 nM; EC50=~ 3 μM). CP-601932 has the same high-binding affinity at α4β2 nAChR (Ki=21 nM) and an order of magnitude lower affinity for α6 and α7 nAChR subtypes. CP-601932 selectively decreases ethanol but not sucrose consumption and operant self-administration following long-term exposure. CP-601932 can penetrate the CNS .
    CP-601932
  • HY-171807
    TC-2559 free base

    		nAChR STAT Neurological Disease Inflammation/Immunology
    TC-2559 free base is a α4β2 nicotinic acetylcholine receptor (nAChR) agonists with an EC50 of 0.18 μM. TC-2559 free base shows much weaker potencies on the group of b4-containing nAChR subtypes, α2β4, α4β4 and α3β4 receptors, with EC50s in the range of 10-30 µM. TC-2559 free base can increase the discharge of dopamine cells in the ventral tegmental area (VTA) of rats in vitro, enhancing the excitability and aggressive behavior of VTA dopamine neurons. TC-2559 free base inhibits STAT3 to exert anti-inflammatory properties and relieves mice mechanical allodynia and improve rats cognitive deficits. TC-2559 free base can be used for the study of nerve pain .
    TC-2559 free base
  • HY-117106
    PNU-107484A

    		GABA Receptor Others
    PNU-107484A is a GABAA receptor ligand that exhibits target activity mechanisms dependent on α isoforms. In the α1β2γ2 subtype, PNU-107484A acts as a positive allosteric modulator, enhancing GABA-induced Cl - currents, while it inhibits the currents in the α3β2γ2 and α6β2γ2 subtypes. The half-maximal concentrations for the α1β2γ2, α3β2γ2, and α6β2γ2 subtypes are 3.1, 4.2, and 3.5 μM, respectively. PNU-107484A can be used as a probe to investigate the physiological roles of different α isoform subtypes .
    PNU-107484A
  • HY-D1398
    LtIA-F

    		nAChR Neurological Disease
    LtIA-F, a novel fluorescent analogue of LtIA, provides a wealth of pharmacological tools to explore the structure–function relationship, distribution, and ligand binding domain of the α3β2 nAChR subtype.
    LtIA-F
  • HY-14312
    A85380

    		nAChR Neurological Disease
    A 85380 is a novel, high affinity neuronal nicotinic acetylcholine receptor (nAChR) agonist. A 85380 exhibits selectivity for the α4β2 nAChR subtypes. A 85380 has a broad-spectrum analgesic profile .
    A85380
  • HY-14319A
    Sazetidine A hydrochloride

    		nAChR Neurological Disease
    Sazetidine A hydrochloride is a potent ligand for the α4β2 nicotinic acetylcholine receptor, exhibiting high binding affinities and selectivity towards this subtype. Sazetidine A hydrochloride demonstrates promising pharmacological properties that could potentially contribute to the development of therapies targeting nicotinic receptor-related conditions. Sazetidine A hydrochloride has been implicated in studies examining the binding affinities of various analogs, highlighting its significance in understanding subtype selectivity among nAChR ligands.
    Sazetidine A hydrochloride
  • HY-136947
    RJR-2429

    		nAChR Neurological Disease
    RJR-2429 is a nAChR agonist (EC50: 59 nM). RJR-2429 binds with high affinity to α4β2 receptor subtype (Ki = 1 nM). RJR-2429 induces ileum contraction .
    RJR-2429
  • HY-B1562C
    Bopindolol fumarate

    (±)-Bopindolol fumarate

    		 Adrenergic Receptor Renin 5-HT Receptor Cardiovascular Disease Neurological Disease
    Bopindolol ((±)-Bopindolol) fumarate is an orally active antagonist of β-adrenoceptors (ARs) with partial agonist activity. Bopindolol fumarate is non-selective for β1- and β2-ARs and has low affinity for β3-AR subtype. Bopindolol fumarate has intrinsic sympathomimetic as well as membrane stabilizing actions, inhibits renin secretion, and interacts with 5-HT receptors. Bopindolol fumarate is a proagent of Pindolol (HY-B0982). Bopindolol fumarate can be used for essential and renovascular hypertension research.
    Bopindolol fumarate
  • HY-B1562
    Bopindolol

    (±)-Bopindolol

    		 Adrenergic Receptor Renin 5-HT Receptor Cardiovascular Disease Neurological Disease
    Bopindolol ((±)-Bopindolol) is an orally active antagonist of β-adrenoceptors (ARs) with partial agonist activity. Bopindolol is non-selective for β1- and β2-ARs and has low affinity for β3-AR subtype. Bopindolol has intrinsic sympathomimetic as well as membrane stabilizing actions, inhibits renin secretion, and interacts with 5-HT receptors. Bopindolol is a proagent of Pindolol (HY-B0982). Bopindolol can be used for essential and renovascular hypertension research.
    Bopindolol

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