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smoking cessation

" in MedChemExpress (MCE) Product Catalog:

32

Inhibitors & Agonists

7

Natural
Products

6

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-N8505
    Lobelanine

    8,10-Diphenyllobelidione

    		 Others Others
    Lobelanine (8,10-Diphenyllobelidione) is a chemical precursor for the biosynthesis of Lobeline. Lobeline is a partial nicotinic agonist and is used as a smoking cessation agent .
    Lobelanine
  • HY-10019
    Varenicline

    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 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
  • HY-10020
    Varenicline Hydrochloride

    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-10019A
    Varenicline dihydrochloride

    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 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 dihydrochloride
  • HY-10021
    Varenicline Tartrate

    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-10019AS1
    Varenicline-d4 hydrochloride

    		Isotope-Labeled Compounds nAChR Inflammation/Immunology
    Varenicline-d4 hydrochloride is a deuterium labeled Varenicline (dihydrochloride) (HY-10019A) . Varenicline (CP 526555) dihydrochloride is a potent partial agonist for α4β2 nicotinic acetylcholine receptor (nAChR) with an EC50 value of 2.3 μM. Varenicline dihydrochloride is a full agonist for α3β4 and α7 nAChRs with EC50 values of 55 μM and 18 μM, respectively . Varenicline dihydrochloride is a nicotinic ligand based on the structure of cytosine, and has the potential for smoking cessation treatment .
    Varenicline-d4 hydrochloride
  • HY-155456
    CYP2A6-IN-1

    		Cytochrome P450 Metabolic Disease
    CD-6 is a flavonoid CYP2A6 inhibitor (IC50: 1.566 μM). CYP2A6 inhibits the metabolism of nicotine to cotinine, resulting in an increase in the amount of nicotine available in the blood, leading to increased smoking behavior. CD-6 mediates CYP2A6 inhibition and can be used in research on smoking cessation or smoking-related diseases .
    CYP2A6-IN-1
  • HY-128420
    Lobeline sulfate

    α-Lobeline sulfate; L-Lobeline sulfate

    		 nAChR Dopamine Transporter Neurological Disease
    Lobeline (α-Lobeline) sulfate is a brain-penetrant nicotinic receptor agonist. Lobeline sulfate increases dopamine (DA) release by inhibiting DA uptake into synaptic vesicles, and altering presynaptic DA storage. Lobeline sulfate is effective in smoking cessation .
    Lobeline sulfate
  • HY-131479A
    Threo-dihydrobupropion

    		Drug Metabolite Neurological Disease
    Threo-dihydrobupropion is a major metabolite of Bupropion, formed via oxidation and reduction exhibit pharmacological activity. Bupropion, a dual dopamine-norepinephrine uptake inhibitor and a nicotine receptor antagonist, is widely used in the management of depression and as a smoking cessation aid .
    Threo-dihydrobupropion
  • HY-10021R
    Varenicline Tartrate (Standard)

    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-10019R
    Varenicline (Standard)

    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 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 (Standard)
  • HY-10019AR
    Varenicline dihydrochloride (Standard)

    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 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 dihydrochloride (Standard)
  • HY-10020R
    Varenicline Hydrochloride (Standard)

    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-10019S1
    Varenicline-15N,13C,d2

    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 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-15N,13C,d2
  • HY-110241
    Dianicline dihydrochloride

    		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-11058
    BHF177

    		GABA Receptor Neurological Disease
    BHF177 is a positive modulator of GABAB receptors that can block the interaction between nicotine and the brain's dopamine system, thereby reducing the addictive properties of nicotine. BHF177 is expected to be used in research related to smoking cessation .
    BHF177
  • HY-B0979
    Lobeline hydrochloride

    α-Lobeline hydrochloride; L-Lobeline hydrochloride

    		 nAChR Dopamine Transporter Neurological Disease
    Lobeline (α-Lobeline) hydrochloride is a brain-penetrant nicotinic receptor agonist. Lobeline hydrochloride increases dopamine (DA) release by inhibiting DA uptake into synaptic vesicles, and altering presynaptic DA storage. Lobeline hydrochloride is effective in smoking cessation .
    Lobeline hydrochloride
  • HY-B1423
    Lobeline

    α-Lobeline; L-Lobeline

    		 nAChR Dopamine Transporter Neurological Disease
    Lobeline (α-Lobeline) is a brain-penetrant nicotinic receptor agonist. Lobeline increases dopamine (DA) release by inhibiting DA uptake into synaptic vesicles, and altering presynaptic DA storage. Lobeline is effective in smoking cessation .
    Lobeline
  • HY-12766
    Bupropion morpholinol

    		Dopamine Transporter nAChR Neurological Disease
    Bupropion morpholinol (Hydroxy Bupropion) is a major metabolite of Bupropion. Bupropion morpholinol inhibits Dopamine, Norepinephrine transporters and the α4β2 nicotinic receptor in vitro. Bupropion morpholinol contributes to antidepressant and smoking cessation activities .
    Bupropion morpholinol
  • HY-100637
    Hydroxybupropion

    		Drug Metabolite Adrenergic Receptor nAChR Neurological Disease
    Hydroxybupropion is the major active metabolite of Bupropion. Hydroxybupropion is metabolized by CYP2B6. Bupropion is an atypical antidepressant and smoking-cessation agent. Hydroxybupropion inhibits norepinephrine uptake with an IC50 value of 1.7 μM. Hydroxybupropion is also a nACh receptor antagonist .
    Hydroxybupropion
  • HY-N0175
    Cytisinicline
    1 Publications Verification

    Cytisine; Sophorine; Baptitoxine

    		 nAChR Metabolic Disease Cancer
    Cytisinicline (Cytisine) is an alkaloid. Cytisinicline (Cytisine) is a partial agonist of α4β2 nAChRs , and partial to full agonist at β4 containing receptors and α7 receptors . Has been used medically to help with smoking cessation .
    Cytisinicline
  • HY-12766S
    Bupropion morpholinol-d6

    		Isotope-Labeled Compounds nAChR Dopamine Transporter Neurological Disease
    Bupropion morpholinol-d6 is the deuterated form of Bupropion morpholinol. Bupropion morpholinol is a major metabolite of Bupropion. Bupropion morpholinol inhibits Dopamine, Norepinephrine transporters and the α4β2 nicotinic receptor in vitro. Bupropion morpholinol contributes to antidepressant and smoking cessation activities .
    Bupropion morpholinol-d6
  • HY-B0979R
    Lobeline hydrochloride (Standard)

    		nAChR Dopamine Transporter Neurological Disease
    Lobeline (hydrochloride) (Standard) is the analytical standard of Lobeline (hydrochloride). This product is intended for research and analytical applications. Lobeline (α-Lobeline) hydrochloride is a brain-penetrant nicotinic receptor agonist. Lobeline hydrochloride increases dopamine (DA) release by inhibiting DA uptake into synaptic vesicles, and altering presynaptic DA storage. Lobeline hydrochloride is effective in smoking cessation .
    Lobeline hydrochloride (Standard)
  • HY-117799
    LY-426965

    		5-HT Receptor Endocrinology
    LY426965 is a potent arylpiperazine compound known for its role as a full antagonist of the serotonin 1A receptor, lacking partial agonist activity. It is identified as a selective 5-HT1A antagonist, showing promise in preclinical studies for treating conditions associated with serotonin dysregulation, such as smoking cessation and depression-related disorders .
    LY-426965
  • HY-117799A
    LY-426965 hydrochloride

    		5-HT Receptor Endocrinology
    LY-426965 hydrochloride is a potent arylpiperazine compound known for its role as a full antagonist of the serotonin 1A receptor, lacking partial agonist activity. It is identified as a selective 5-HT1A antagonist, showing promise in preclinical studies for treating conditions associated with serotonin dysregulation, such as smoking cessation and depression-related disorders .
    LY-426965 hydrochloride
  • HY-N0175R
    Cytisinicline (Standard)

    		nAChR Metabolic Disease Cancer
    Cytisinicline (Standard) is the analytical standard of Cytisinicline. This product is intended for research and analytical applications. Cytisinicline (Cytisine) is an alkaloid. Cytisinicline (Cytisine) is a partial agonist of α4β2 nAChRs , and partial to full agonist at β4 containing receptors and α7 receptors . Has been used medically to help with smoking cessation .
    Cytisinicline (Standard)
  • HY-10019S
    Varenicline-d4

    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[1]. Varenicline is a nicotinic ligand based on the structure of cytisine, has the potential for smoking cessation treatment[2].
    Varenicline-d4
  • HY-135783
    AT 1001
    1 Publications Verification

    		 nAChR Neurological Disease
    AT 1001 is a high-affinity and selective antagonist of the α3β4 nicotinic acetylcholine receptor (α3β4 nAChR) (Ki=2.64 nM). AT 1001 reversibly blocks inward currents induced by Epibatidine (HY-101078) in HEK cells transfected with α3β4 nAChR. AT-1001 dose-dependently inhibits nicotine self-administration behavior in rats without affecting food-reinforced responding. AT 1001 can be utilized in the research of nicotine addiction and smoking cessation therapies .
    AT 1001
  • HY-14202
    Lazabemide hydrochloride

    Ro 19-6327 hydrochloride

    		 Monoamine Oxidase Neurological Disease
    Lazabemide hydrochloride (Ro 19-6327 hydrochloride) is a selective, reversible inhibitor of monoamine oxidase B (MAO-B) (IC50=0.03 μM) but less active for MAO-A (IC50>100 μM). Lazabemide  inhibits monoamine uptake at high concentrations, the IC50 values are 86 μM, 123 μM and >500 μM for noradrenalin, serotonin and dopamine uptake, respectively. Lazabemide can be used for the research of parkinson and alzheimer′s disease .
    Lazabemide hydrochloride
  • HY-14201
    Lazabemide

    Ro 19-6327

    		 Monoamine Oxidase Neurological Disease
    Lazabemide (Ro 19-6327) is a selective, reversible inhibitor of monoamine oxidase B (MAO-B) (IC50=0.03 μM) but less active for MAO-A (IC50>100 μM). Lazabemide ?inhibits monoamine uptake at high concentrations, the IC50 values are 86 μM, 123 μM and >500 μM for noradrenalin, serotonin and dopamine uptake, respectively. Lazabemide can be used for the research of parkinson and?alzheimer′s disease .
    Lazabemide
  • HY-10019S2
    Varenicline-13C15N

    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 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-13C15N
  • HY-10020S
    Varenicline-15N3 hydrochloride

    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