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Results for "

α4β2 nAChR partial agonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	nAChR (16) ERK (1) Isotope-Labeled Compounds (3) p38 MAPK (1)
By Research Areas:	Cancer (3) Inflammation/Immunology (5) Metabolic Disease (1) Neurological Disease (15)

Inhibitors & Agonists

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: nAChR

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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 .

HY-10020

Varenicline Hydrochloride CP 526555 hydrochloride	nAChR	Neurological Disease Inflammation/Immunology
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 .

HY-10021

Varenicline Tartrate CP 526555-18	nAChR ERK p38 MAPK	Others Neurological Disease
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 .

HY-10019A

Varenicline dihydrochloride CP 526555 dihydrochloride	nAChR	Neurological Disease Inflammation/Immunology
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 .

HY-107680

3-Pyr-Cytisine 3-Pyr-Cyt	nAChR	Neurological Disease
3-Pyr-Cytisine (3-Pyr-Cyt) is a cytisine derivative. 3-Pyr-Cytisine is a very weak **α4β2 nAChR** partial agonist that has been studied as an antidepressant .

HY-10063

Ispronicline 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 (K_i=11 nM) and is highly selective to other nAChRs such as α7 nAChR and α3β4 nAChR .

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 .

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 .

HY-107688A

UB-165 fumarate	nAChR	Neurological Disease
UB-165 fumarate is a *nAChR* agonist, being a full agonist of the α3β2 isoform and a partial agonist of the α4β2* isoform, with a K_i value of 0.27 nM for [ ³H]-nicotine binding in rat brain .

HY-107688

UB-165	nAChR	Neurological Disease
UB-165 is a *nAChR* agonist, being a full agonist of the α3β2 isoform and a partial agonist of the α4β2* isoform, with a K_i value of 0.27 nM for [ ³H]-nicotine binding in rat brain .

HY-115766

Anabaseine	nAChR	Neurological Disease
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 .

HY-138879

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

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 .

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].

HY-10019AS1

Varenicline-d4 hydrochloride	Isotope-Labeled Compounds	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 .

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 (K_i=16 nM) and shows high selectivity for α6β2* and α4α5β2 nAChR subtypes, the binding affinity (K_i, 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 .

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 (K_i=21 nM; EC₅₀=~ 3 μM). CP-601932 has the same high-binding affinity at α4β2 nAChR (K_i=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 .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N0175

Cytisinicline 1 Publications Verification Cytisine; Sophorine; Baptitoxine	Alkaloids Classification of Application Fields Leguminosae Source classification Pyridine Alkaloids Metabolic Disease Plants Thermopsis lanceolala R.Br. Disease Research Fields	nAChR
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 .

Cat. No.	Product Name	Chemical Structure

HY-10019AS1

Varenicline-d4 hydrochloride
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

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 .

HY-10019S1

Varenicline-15N,13C,d2
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

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 .

HY-10019S

Varenicline-d4
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

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].

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