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α4β2 nicotinic acetylcholine receptor

" in MedChemExpress (MCE) Product Catalog:

55

Inhibitors & Agonists

6

Isotope-Labeled Compounds

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-10019
    Varenicline
    1 Publications Verification

    CP 526555

    nAChR Neurological Disease Inflammation/Immunology Cancer
    Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α7β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .
    Varenicline
  • HY-10021
    Varenicline Tartrate
    1 Publications Verification

    CP 526555-18

    nAChR ERK p38 MAPK Others Neurological Disease Cancer
    Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .
    Varenicline Tartrate
  • HY-B0942
    Benzethonium chloride
    1 Publications Verification

    Environmental Pollutants nAChR Bacterial Apoptosis Caspase Infection Neurological Disease Cancer
    Benzethonium chloride inhibits nicotinic acetylcholine receptors in human recombinant α7 and α4β2 neurons in Xenopus laevis oocytes, which has antibacterial, anticancer, antisepsis and disinfection activity. Benzethonium chloride induced Apoptosis and activated caspases in cancer cell lines. Benzethonium chloride ablates the tumor-forming ability of FaDu cells, delays the growth of xenograft tumors in vivo .
    Benzethonium chloride
  • HY-14564A
    GTS-21 dihydrochloride
    Maximum Cited Publications
    14 Publications Verification

    DMXB-A; DMBX-anabaseine

    nAChR 5-HT Receptor Inflammation/Immunology
    GTS-21 dihydrochloride is a selective alpha7 nicotinic acetylcholine receptor (α7-nAChR) agonist with anti inflammatory and cognition enhancing activities. GTS-21 dihydrochloride is also a α4β2 (Ki=20 nM for humanα4β2) and 5-HT3A receptor (IC50=3.1 μM) antagonist .
    GTS-21 dihydrochloride
  • HY-B0379A
    Adiphenine hydrochloride
    3 Publications Verification

    nAChR Neurological Disease
    Adiphenine hydrochloride is a non-competitive inhibitor of nicotinic acetylcholine receptor (nAChR), with an IC50s of 1.9, 1.8, 3.7, and 6.3 μM for α1, α3β4, α4β2, and α4β4, respectively. Adiphenine hydrochloride has anticonvulsant effects .
    Adiphenine hydrochloride
  • HY-10020

    CP 526555 hydrochloride

    nAChR Neurological Disease Inflammation/Immunology Cancer
    Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .
    Varenicline Hydrochloride
  • HY-107675

    Deformylflustrabromine hydrochloride; dFBr hydrochloride

    nAChR Neurological Disease
    Desformylflustrabromine hydrochloride is a selective agonist of α4β2 neuronal nicotinic acetylcholine receptor (nAChR) with a pEC50 of 6.48.
    Desformylflustrabromine hydrochloride
  • HY-110160

    ABT-089 dihydrochloride

    nAChR Neurological Disease
    Pozanicline dihydrochloride (ABT-089 dihydrochloride) is an orally bioavailable nicotinic acetylcholine receptor (nAChR) agonist with a Ki of 16.7 nM for binding to [ 3H]cytisine sites . Pozanicline is an α4β2-selective nAChR agonist, which binds to rat brain α4β2 nAChR with a Ki of 17 nM while binding to α7 nAChR is insignificant .
    Pozanicline dihydrochloride
  • HY-136146

    nAChR Neurological Disease
    SUVN-911 is a potent, selective, brain penetrated and orally bioavailable neuronal nicotinic acetylcholine α4β2 receptor antagonist, with a Ki of 1.5 nM. SUVN-911 has antidepressant activity .
    SUVN-911
  • HY-10019A

    CP 526555 dihydrochloride

    nAChR Neurological Disease Inflammation/Immunology Cancer
    Varenicline (CP 526555-18) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α7β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .
    Varenicline dihydrochloride
  • HY-110121A
    NS3861
    1 Publications Verification

    nAChR Neurological Disease
    NS3861 is an agonist of nicotinic acetylcholine receptors (nAChRs) and binds with high affinity to heteromeric α3β4 nAChR. The binding Ki values of 0.62, 25, 7.8, 55 nM for α3β4, α3β2, α4β4, α4β2, respectively .
    NS3861
  • HY-14840

    Carphedon

    nAChR Dopamine Transporter GABA Receptor iGluR Neurological Disease
    Phenylpiracetam (Carphedon) is a positive allosteric modulator of nicotinic acetylcholine receptors (nAChR) with an IC50 of 5.86 μM. Phenylpiracetam is applicable to studies on scopolamine (Scopolamine) (HY-N0296)-induced amnesia, depression and immune stress .
    Phenylpiracetam
  • HY-160959

    nAChR Neurological Disease
    AN317 is a selective agonist for α6β2-containing nicotinic acetylcholine receptor (nAChR) with Ki of 6.2 nM and 4.1 nM, for α6/α3β2β3 receptor and α4β2 receptor, respectively. AN317 induces dopamine release in the synaptosomes of the rat striatum, enhances dopaminergic neuronal activity in substantia nigra, and exhibits protective efficacy to rat neurons against dopamine neurotoxin MPP +. AN317 exhibits good pharmacokinetic characteristics in rats. AN317 penetrates the blood-brain barrier (BB) .
    AN317
  • HY-110131

    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-B0942R

    Reference Standards nAChR Bacterial Neurological Disease
    Benzethonium (chloride) (Standard) is the analytical standard of Benzethonium (chloride). This product is intended for research and analytical applications. Benzethonium chloride inhibits nicotinic acetylcholine receptors in human recombinant α7 and α4β2 neurons in Xenopus laevis oocytes.
    Benzethonium chloride (Standard)
  • HY-10063

    TC-1734; ACD3480

    nAChR Neurological Disease
    Ispronicline (TC-1734), an orally active, brain-selective α4β2 nicotine acetylcholine receptor (nAChR) partial agonist, has shown memory-enhancing properties in rodents and a good tolerability profile. Ispronicline binds to the α4β2 nAChR with high affinity (Ki=11 nM) and is highly selective to other nAChRs such as α7 nAChR and α3β4 nAChR .
    Ispronicline
  • HY-136207

    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-108069

    Potassium Channel nAChR Neurological Disease
    Iptakalim hydrochloride, a lipophilic para-amino compound, is a novel ATP-sensitive potassium channel (KATP) opener, as well as an α4β2-containing nicotinic acetylcholine receptor (nAChR) antagonist .
    Iptakalim hydrochloride
  • HY-107686

    5-I A-85380 dihydrochloride

    nAChR Neurological Disease
    5-Iodo-A-85380 dihydrochloride is a selective ligand of nAChR. 5-Iodo-A-85380 dihydrochloride binds to α4β2 nAChRs in rat and human brain with Kds of 12 and 14 pM,respectively .
    5-Iodo-A-85380 dihydrochloride
  • HY-115766

    nAChR Neurological Disease
    Anabaseine, a brain-penetrant occurring alkaloid toxin, is potent agonist of multiple nicotinic acetylcholine receptors (AChRs). Anabaseine stimulates the neuromuscular α12β1γδ or α12β1γɛ and α7 AChRs. Anabaseine is also a weak partial agonist at α4β2 nAChRs .
    Anabaseine
  • HY-139581

    SUVN-911 free base

    nAChR Neurological Disease
    Ropanicant (SUVN-911 free base) is a novel, potent, selective, and orally active neuronal nicotinic acetylcholine α4β2 receptor antagonist for the research of depression .
    Ropanicant
  • HY-110241

    nAChR Neurological Disease
    Dianicline dihydrochloride is a α4β2 nicotinic acetylcholine receptor partial agonist, a class of agents that includes varenicline and cytisine for smoking cessation. Dianicline dihydrochloride increases cessation rates in a dose-dependent manner .
    Dianicline dihydrochloride
  • HY-110121
    NS3861 fumarate
    1 Publications Verification

    nAChR Neurological Disease
    NS3861 fumarate is an agonist of nicotinic acetylcholine receptors (nAChRs) and binds with high affinity to heteromeric α3β4 nAChR. The binding Ki values of 0.62, 25, 7.8, 55 nM for α3β4, α3β2, α4β4, α4β2, respectively .
    NS3861 fumarate
  • HY-124110

    nAChR Neurological Disease
    TC299423 is an orally active, brain-penetrant, selective and potent agonist for α6β2 ? and α4β2 ? nicotinic acetylcholine receptors (nAChRs) with anxiolytic and antinociceptive properties. TC299423 acts primarily through α6β2 ? nAChRs that are implicated in the anxiolytic effects of nicotine. TC299423 elicits reward-related behavior mediated through α6β2 ? nAChRs in hypersensitive α6L90’S mice. TC299423 elicits dopamine release and dose not suppress nicotine self-administration in rats. TC299423 is proming for rasearch of addiction and Parkinson’s disease .
    TC299423
  • HY-10021R

    CP 526555-18 (Standard)

    Reference Standards nAChR ERK p38 MAPK Others Neurological Disease
    Varenicline (Tartrate) (Standard) is the analytical standard of Varenicline (Tartrate). This product is intended for research and analytical applications. Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .
    Varenicline Tartrate (Standard)
  • HY-14564

    nAChR 5-HT Receptor Inflammation/Immunology
    GTS-21 dihydrochloride is a selective alpha7 nicotinic acetylcholine receptor (α7-nAChR) agonist with anti inflammatory and cognition enhancing activities. GTS-21 dihydrochloride is also a α4β2 (Ki=20 nM for humanα4β2) and 5-HT3A receptor (IC50=3.1 μM) antagonist. GTS-21 can be used in age-associated memory impairment (AAMI) and Alzheimer's disease research .
    GTS-21
  • HY-169870

    (+)-Mecamylamine; TC-5214

    nAChR Neurological Disease
    Dexmecamylamine ((+)-Mecamylamine) is the antagonist for nicotinic acetylcholine receptor (nAChR), that antagonises the α3β4/α4β2/α7/α1β1γδ receptor with IC50 of micromolare levels. Dexmecamylamine exhibits anxiolytic and antidepressant-like activities .
    Dexmecamylamine
  • HY-18159

    AZD1446

    nAChR Neurological Disease
    TC-6683 (AZD1446) is a selective α4β2 nicotinic acetylcholine receptor (nAChR) agonist. TC-6683 does not show significant therapeutic effects in the animal model of DYT1 dystonia.TC-6683 can be used for the research of neurological disease, such as cognitive disorder .
    TC-6683
  • HY-14565

    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-116149

    nAChR Others
    A-424274 is a positive allosteric modulator of the α4β2 neuronal nicotinic acetylcholine receptor with activity to enhance the efficacy of analgesics. A-424274 selectively enhances the potency of a range of nicotinic acetylcholine receptor agonists at the α4β2 receptor and, in preclinical models, co-administration with an α4β2 PAM significantly enhances the analgesic efficacy of ABT-594 at clinically well-tolerated doses in humans.
    A-424274
  • HY-14316C

    Ebanicline tosylate; ABT-594 tosylate

    nAChR Neurological Disease
    Tebanicline tosylate, an analogue of epibatidine, is a neuronal nicotinic acetylcholine receptor agonist. Tebanicline tosylate exhibits potent antinociceptive effects and has a high affinity for the α4β2 neuronal nicotinic acetylcholine receptor subunit in the central nervous system.
    Tebanicline tosylate
  • HY-14316

    Ebanicline; ABT-594

    nAChR Neurological Disease
    Tebanicline, an analogue of epibatidine, is a neuronal nicotinic acetylcholine receptor agonist. Tebanicline exhibits potent antinociceptive effects and has a high affinity for the α4β2 neuronal nicotinic acetylcholine receptor subunit in the central nervous system.
    Tebanicline
  • HY-B0942S

    Isotope-Labeled Compounds nAChR Neurological Disease
    Benzethonium-d7 chloride is the deuterium labeled Benzethonium chloride. Benzethonium chloride inhibit human recombinant α7 and α4β2 neuronal nicotinic acetylcholine receptors in Xenopus oocytes.
    Benzethonium-d7 chloride
  • HY-171807

    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-14312

    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-120946

    nAChR Neurological Disease
    VMY-2-95 is an oral active and blood-brain barrier (BBB) penetrant α4β2 nicotinic acetylcholine receptor desensitizer. VMY-2-95 can be used for study of depression or addiction .
    VMY-2-95
  • HY-103066

    nAChR Neurological Disease
    Br-PBTC is a potent, 2/4 subtype-selective positive allosteric modulator of nAChRs (nicotinic acetylcholine receptors) with α2β2, α2β4, α4β2, α4β4, (α4β2)2α4 and (α4β2)2β2 EC50 ranges from 0.1-0.6 μM. Br-PBTC acts from the c-tail of an α subunit .
    Br-PBTC
  • HY-W680961

    nAChR Neurological Disease
    Hydrohydrastinine is a selective α4β2 nicotinic acetylcholine receptor antagonist with an IC50 of 2.6 μM and a Ki of 17 μM. Hydrohydrastinine exhibits weak activity at α4β4 and α3β4 nicotinic acetylcholine receptors. Hydrohydrastinine can be used for the research of depression .
    Hydrohydrastinine
  • HY-138879

    nAChR Neurological Disease
    CP-601927 is a selective α4β2 nicotinic acetylcholine receptor (nAChR) partial agonist (Ki=1.2 nM; EC50=2.6 μM). CP-601927 shows good brain penetration and antidepressant-like properties .
    CP-601927
  • HY-10019R

    CP 526555 (Standard)

    Reference Standards nAChR Neurological Disease Inflammation/Immunology Cancer
    Varenicline (Standard) is the analytical standard of Varenicline. This product is intended for research and analytical applications. Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α7β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .
    Varenicline (Standard)
  • HY-10019AR

    CP 526555 dihydrochloride (Standard)

    Reference Standards nAChR Neurological Disease Inflammation/Immunology Cancer
    Varenicline (dihydrochloride) (Standard) is the analytical standard of Varenicline (dihydrochloride). This product is intended for research and analytical applications. Varenicline (CP 526555-18) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α7β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .
    Varenicline dihydrochloride (Standard)
  • HY-10020R

    CP 526555 hydrochloride (Standard)

    Reference Standards nAChR Neurological Disease Inflammation/Immunology Cancer
    Varenicline (Hydrochloride) (Standard) is the analytical standard of Varenicline (Hydrochloride). This product is intended for research and analytical applications. Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .
    Varenicline Hydrochloride (Standard)
  • HY-10019S2

    CP 526555-13C,15N

    Isotope-Labeled Compounds nAChR Neurological Disease Inflammation/Immunology Cancer
    Varenicline- 13C 15N (CP 526555- 13C 15N) is 13C and 15N labeled Varenicline. Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α7β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .
    Varenicline-13C15N
  • HY-10019S1

    CP 526555-15N,13C,d2

    nAChR Isotope-Labeled Compounds Neurological Disease Inflammation/Immunology Cancer
    Varenicline- 15N, 13C,d2 is 15N and deuterated labeled Varenicline (HY-10019). Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50=250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α7β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .
    Varenicline-15N,13C,d2
  • HY-10020S

    CP 526555-15N3 Hydrochloride

    nAChR Isotope-Labeled Compounds Neurological Disease Inflammation/Immunology Cancer
    Varenicline-15N3 Hydrochloride (CP 526555-15N3 Hydrochloride) is the 15N labeled isotope of Varenicline hydrochloride (HY-10020). Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .
    Varenicline-15N3 hydrochloride
  • HY-14824A

    ABT 894 benzenesulfonate

    nAChR Neurological Disease
    Sofinicline benzenesulfonate (ABT 894 benzenesulfonate) is a novel nicotinic acetylcholine receptor agonist, specifically acting on the α4β2 subtype of nAChR (IC50=0.1 nM). Sofinicline benzenesulfonate has the potential to improve cognitive function, including attention, memory and working memory. Sofinicline benzenesulfonate can be used in studies of attention deficit, hyperactivity disorder (ADHD) .
    Sofinicline benzenesulfonate
  • HY-14319A

    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-121141

    nAChR Neurological Disease
    Adiphenine is a non-competitive inhibitor of nicotinic acetylcholine receptor (nAChR), with an IC50s of 1.9, 1.8, 3.7, and 6.3 μM for α1, α3β4, α4β2, and α4β4, respectively. Adiphenine has anticonvulsant effects .
    Adiphenine
  • HY-10019S

    CP 526555-d4

    Isotope-Labeled Compounds nAChR Neurological Disease
    Varenicline-d4 is deuterium labeled Varenicline. Varenicline (CP 526555) is a potent partial agonist for α4β2 nicotinic acetylcholine receptor (nAChR) with an EC50 value of 2.3 μM. Varenicline is a full agonist for α3β4 and α7 nAChRs with EC50 values of 55 μM and 18 μM, respectively . Varenicline is a nicotinic ligand based on the structure of cytisine, has the potential for smoking cessation treatment .
    Varenicline-d4
  • HY-14318

    SIB-1508Y free base

    nAChR Neurological Disease
    Altinicline (SIB-1508Y free base) is a selective α4β2 nicotinic acetylcholine receptor (nAChR) agonist, with no activity against α7 or α1β1γδ nAChRs and only extremely low activity against α3β4 nAChRs. Altinicline reverses escape deficits and increases avoidance responses. Altinicline is applicable to research related to depression .
    Altinicline

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