Description
3-pyr-Cytisine is a partial agonist of α4β2 receptor with Ki values of 0.91, 119 and 1100 nM for α4β2, α3β4 and α7 receptors, respectively . The alpha-4 beta-2 nicotinic receptor (α4β2 receptor) is a nicotinic acetylcholine receptor participated in learning and is widely expressed in the central nervous system. Also, α4β2 receptor has the highest affinity for nicotine. 3-pyr-Cytisine is an α4β2 receptor partial agonist. In cells expressed α4β2 receptor, 3-pyr-Cyt reduced the agonist response by ACh, which relayed on the intrinsic activity of 3-pyr-Cyt and 3-pyr-Cyt concentration . In PC12 cells, 3-pyr-Cyt significantly induced release of norepinephrine (NE) in a time-, dose- and Ca2+-dependent way. Also, 3-pyr-Cyt inhibited nicotine-induced NE release and increased the mRNA levels of tyrosine hydroxylase (TH), which is necessary for catecholamine biosynthetic . In the tail suspension test, mice treated with 3-pyr-Cyt (0.6 mg/kg) spent significantly less time immobile in a dose-dependent way. In the forced swim test, mice treated with 3-pyr-Cyt (0.3, 0.6 or 0.9 mg/kg) were significantly less immobile in a dose-dependent way, which suggested that 3-pyr-Cyt exhibited antidepressant-like effects in a dose-dependent way .
Product information
CAS Number: 948027-43-8
Molecular Weight: 267.33
Formula: C16H17N3O
Chemical Name: (1R,9S)-5-(pyridin-3-yl)-7,11-diazatricyclo[7.3.1.0²,⁷]trideca-2,4-dien-6-one
Smiles: O=C1C(=CC=C2[C@@H]3C[C@@H](CNC3)CN21)C1=CN=CC=C1
InChiKey: GOYASQWDLRLAPK-WCQYABFASA-N
InChi: InChI=1S/C16H17N3O/c20-16-14(12-2-1-5-17-8-12)3-4-15-13-6-11(7-18-9-13)10-19(15)16/h1-5,8,11,13,18H,6-7,9-10H2/t11-,13+/m0/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
Products are for research use only. Not for human use.
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