product name Varenicline Tartrate
Description: Varenicline Tartrate is a nicotinic AChR partial agonist, used to treat nicotine addiction.Varenicline is a partial agonist with 45% of nicotines maximal efficacy atalpha4beta2 nAChRs in HEK cells expressing nAChRs. Varenicline is a potent, partial agonist at alpha4beta2 receptors, with an EC50 of 2.3 mM and an efficacy (relative to acetylcholine) of 13.4%.
References: Neuropharmacology. 2007 Mar;52(3):985-94; Psychopharmacology (Berl). 2010 Feb;208(3):365-76.
361.35
Formula
C13H13N3·C4H6O6
CAS No.
375815-87-5
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: <1 mg/mL
Water: 72 mg/mL (199.3 mM)
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
CP 526555-18
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19392952
| In Vitro |
In vitro activity: Varenicline is a partial agonist with 45% of nicotines maximal efficacy atalpha4beta2 nAChRs in HEK cells expressing nAChRs. Varenicline is a potent, partial agonist at alpha4beta2 receptors, with an EC50 of 2.3 mM and an efficacy (relative to acetylcholine) of 13.4%. Varenicline has lower potency and higher efficacy at alpha3beta4 receptors, with an EC50 of 55 mM and an efficacy of 75%. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Varenicline has significantly lower (40-60%) efficacy than nicotine in stimulating [(3)H]-dopamine release from rat brain slices in vitro and in increasing dopamine release from rat nucleus accumbens in vivo, while it is more potent than Nicotine. Varenicline effectively attenuates the nicotine-induced dopamine release to the level of the effect of Varenicline alone, consistent with partial agonism. Varenicline reduces nicotine self-administration in rats and supports lower self-administration break points than nicotine. Varenicline dose-dependently reduces nicotine self-administration and attenuates both nicotine prime and combined nicotine prime plus nicotine-paired cue-induced reinstatement. Varenicline, a partial agonist at thealpha4beta2 nAChRs, reduces nicotine intake and was recently approved as a smoking cessation aid. Varenicline selectively reduces ethanol but not sucrose seeking using an operant self-administration drinking paradigm and also decreases voluntary ethanol but not water consumption in animals chronically exposed to ethanol for 2 months before Varenicline treatment. |
| Animal model | |
| Formulation & Dosage | |
| References | Neuropharmacology. 2007 Mar;52(3):985-94; Psychopharmacology (Berl). 2010 Feb;208(3):365-76. |
Related Posts
product name Varenicline Tartrate
Description: Varenicline Tartrate is a nicotinic AChR partial agonist, used to treat nicotine addiction.Varenicline is a partial agonist with 45% of nicotines maximal efficacy atalpha4beta2 nAChRs in HEK cells expressing nAChRs. Varenicline is a potent, partial agonist at alpha4beta2 receptors, with an EC50 of 2.3 mM and an efficacy (relative to acetylcholine) of 13.4%.
References: Neuropharmacology. 2007 Mar;52(3):985-94; Psychopharmacology (Berl). 2010 Feb;208(3):365-76.
361.35
Formula
C13H13N3·C4H6O6
CAS No.
375815-87-5
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: <1 mg/mL
Water: 72 mg/mL (199.3 mM)
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
CP 526555-18
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19392952
| In Vitro |
In vitro activity: Varenicline is a partial agonist with 45% of nicotines maximal efficacy atalpha4beta2 nAChRs in HEK cells expressing nAChRs. Varenicline is a potent, partial agonist at alpha4beta2 receptors, with an EC50 of 2.3 mM and an efficacy (relative to acetylcholine) of 13.4%. Varenicline has lower potency and higher efficacy at alpha3beta4 receptors, with an EC50 of 55 mM and an efficacy of 75%. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Varenicline has significantly lower (40-60%) efficacy than nicotine in stimulating [(3)H]-dopamine release from rat brain slices in vitro and in increasing dopamine release from rat nucleus accumbens in vivo, while it is more potent than Nicotine. Varenicline effectively attenuates the nicotine-induced dopamine release to the level of the effect of Varenicline alone, consistent with partial agonism. Varenicline reduces nicotine self-administration in rats and supports lower self-administration break points than nicotine. Varenicline dose-dependently reduces nicotine self-administration and attenuates both nicotine prime and combined nicotine prime plus nicotine-paired cue-induced reinstatement. Varenicline, a partial agonist at thealpha4beta2 nAChRs, reduces nicotine intake and was recently approved as a smoking cessation aid. Varenicline selectively reduces ethanol but not sucrose seeking using an operant self-administration drinking paradigm and also decreases voluntary ethanol but not water consumption in animals chronically exposed to ethanol for 2 months before Varenicline treatment. |
| Animal model | |
| Formulation & Dosage | |
| References | Neuropharmacology. 2007 Mar;52(3):985-94; Psychopharmacology (Berl). 2010 Feb;208(3):365-76. |