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Merck

PZ0004

Sigma-Aldrich

Varenicline tartrate

≥98% (HPLC)

Synonym(e):

7,8,9,10-Tetrahydro-6,10-methano-6H-pyrazino[2,3-h][3]benzazepine tartrate, Champix

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About This Item

Empirische Formel (Hill-System):
C13H13N3 · C4H6O6
CAS-Nummer:
Molekulargewicht:
361.35
MDL-Nummer:
UNSPSC-Code:
12352200
PubChem Substanz-ID:
NACRES:
NA.77

Qualitätsniveau

Assay

≥98% (HPLC)

Form

powder

Farbe

white to beige

Löslichkeit

DMSO: >5 mg/mL

Lagertemp.

room temp

SMILES String

O[C@H]([C@@H](O)C(O)=O)C(O)=O.C1NC[C@H]2C[C@@H]1c3cc4nccnc4cc23

InChI

1S/C13H13N3.C4H6O6/c1-2-16-13-5-11-9-3-8(6-14-7-9)10(11)4-12(13)15-1;5-1(3(7)8)2(6)4(9)10/h1-2,4-5,8-9,14H,3,6-7H2;1-2,5-6H,(H,7,8)(H,9,10)/t8-,9+;1-,2-/m.1/s1

InChIKey

TWYFGYXQSYOKLK-CYUSMAIQSA-N

Anwendung

Varenicline tartrate has been used to investigate its effect on sensorimotor gating in rats under prepulse inhibition (PPI). It is suitable for use as a reference standard in capillary isotachophoresis (ITP) coupled on-line with capillary zone electrophoresis (CZE) for the quantification of varenicline metabolite in urine samples. It is also suitable for use for testing its effect on locomotor and nonlocomotor behavioral deficits in rats.

Biochem./physiol. Wirkung

Varenicline tartrate is a partial α4β2 nicotinic receptor agonist and α7 full agonist. Varenicline competitively binds to α4β2 receptors and partially stimulates without creating a full nicotine effect, while simultaneoudly blocking the ability of nicotine to bind to the receptors. Varenicline thus blocks the ability of nicotine to activate α4β2 receptors and stimulate the central nervous mesolimbic dopamine system, believed to be the neuronal mechanism underlying reinforcement and reward experienced upon smoking.

Leistungsmerkmale und Vorteile

This compound is a featured product for ADME Tox research. Click here to discover more featured ADME Tox products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
This compound is featured on the Acetylcholine Receptors (Nicotinic) page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

Piktogramme

Exclamation markEnvironment

Signalwort

Warning

H-Sätze

Gefahreneinstufungen

Acute Tox. 4 Oral - Aquatic Acute 1

Lagerklassenschlüssel

11 - Combustible Solids

WGK

WGK 3

Flammpunkt (°F)

Not applicable

Flammpunkt (°C)

Not applicable


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Die Dokumentenbibliothek aufrufen

Anne Jackson et al.
Addiction biology, 22(5), 1316-1328 (2016-07-22)
There is recognition that cognitive problems can contribute to renewed drug taking in former addicts. Our previous work has indicated that current smokers show reduced performance on a probabilistic reversal learning (PRL) task, relative to former smokers. To further explore
On-line column coupled isotachophoresis-capillary zone electrophoresis hyphenated with tandem mass spectrometry in drug analysis: Varenicline and its metabolite in human urine
Pievstansky J, et al.
Analytica Chimica Acta, 826, 84-93 (2014)
Patrick A Randall et al.
Psychopharmacology, 232(14), 2443-2454 (2015-02-07)
Varenicline, a smoking-cessation agent, may be useful in treating alcohol use disorders. An important consideration when studying factors that influence drinking/relapse is influence of the pharmacological effects of alcohol on these behaviors. Pre-exposure to alcohol (priming) can increase craving, drinking
Andrea de Bejczy et al.
Alcoholism, clinical and experimental research, 39(11), 2189-2199 (2015-09-29)
Alcohol dependence is a devastating illness affecting a large population, and new pharmacological treatments with good efficacy are greatly needed. One potential candidate is varenicline, a smoking cessation agent with partial agonist action at α4 β2 nicotinic acetylcholine receptors. A
Toshiki Kurosawa et al.
Journal of pharmaceutical sciences, 106(9), 2576-2582 (2017-04-30)
Varenicline is a selective partial α

Artikel

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