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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
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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

Verwandte Kategorien

Anwendung

Varenicline tartrate has been used to investigate its effect on sensorimotor gating in rats under prepulse inhibition (PPI).[1] 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.[2] It is also suitable for use for testing its effect on locomotor and nonlocomotor behavioral deficits in rats.[3]

Biochem./physiol. Wirkung

Varenicline tartrate is a partial α4β2 nicotinic receptor agonist and α7 full agonist.
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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Helen M Kamens et al.
Brain research bulletin, 138, 20-25 (2017-08-06)
Adolescence is a critical period in brain development that coincides with the initiation of alcohol use. Nicotinic acetylcholine receptors (nAChR) have been shown to modulate ethanol behaviors in adult humans and in animal models; however, the role of these receptors
Rachel L Schassburger et al.
Psychopharmacology, 232(5), 975-983 (2014-09-12)
Varenicline (VAR), a smoking cessation aid that is a partial agonist at nicotinic receptors, mimics the reinforcement-enhancing effects of nicotine. Varenicline, when accompanied by non-drug cues, is self-administered by rats, though it is unclear whether this results from varenicline acting
Effect of varenicline on behavioral deficits in a rat model of Parkinson?s disease induced by unilateral 6-hydroxydopamine lesion of substantia nigra
Tan R, et al.
Behavioural Pharmacology, 29(4), 327-335 (2018)
Hiroyuki Mizoguchi et al.
Behavioural brain research, 359, 935-941 (2018-06-24)
Patients suffering from neuropsychiatric disorders such as substance use and addiction disorders show impaired decision-making, which may be associated with their psychiatric disorders. Previously, using a gambling test for rodents, we demonstrated that methamphetamine-dependent rats showed alterations in their decision-making
Nathan M Holmes et al.
Addiction biology, 24(5), 849-859 (2018-06-20)
Restricting when and where smoking can occur is a major focus of public health policies in Western countries. In conjunction with increased taxation, these approaches have contributed to a reduction in smoking uptake among adolescents, yet the consequences for established

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