Sofiniclin (Synonyms: ABT 894) |
| رقم الكتالوجGC37662 |
سوفينيكلين (ABT 894) ، ناهض لمستقبلات الأسيتيل كولين النيكوتين (nAChR) ، يستخدم كبحث غير منشط محتمل لاضطراب نقص الانتباه / فرط النشاط (ADHD)
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 799279-80-4
Sample solution is provided at 25 µL, 10mM.
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Sofiniclin (ABT 894) is an agonist of nicotinic acetylcholine receptor (nAChR), used as a potential non-stimulant treatment for attention-deficit/hyperactivity disorder (ADHD).
Sofiniclin is more potent than ABT-089 at both receptor subtypes, with Ki values of 1.9 nM for 125I-α-conotoxinMII binding and of 1.3 nM for 125I-epibatidine binding[1].
Sofiniclin (0.001 to 0.10 mg/kg, p.o.) produces significant reductions in LIDs compared to vehicle monkey[1]. Sofiniclin (0.1 mg/kg) does not decrease LIDs in monkeys with severe nigrostriatal damage[2].
[1]. Zhang D, et al. ABT-089 and ABT-894 reduce levodopa-induced dyskinesias in a monkey model of Parkinson's disease. Mov Disord. 2014 Apr;29(4):508-17. [2]. Zhang D, ET AL. α7 nicotinic receptor agonists reduce levodopa-induced dyskinesias with severe nigrostriatal damage. Mov Disord. 2015 Dec;30(14):1901-11.
Kinase experiment: | Receptor studies with ABT-089 and Sofiniclin are done using rat striatal sections. α6β2* nAChR levels are assayed using 125I-α-conotoxinMII (α-CtxMII) (specific activity, 2200 Ci/mmol). α4β2* nAChRs are measured by determining the binding of 125I-epibatidine (specific activity, 2200 Ci/mmol) in the presence of 100 nM α-CtxMII to block α6β2* nAChRs. After assay, sections are exposed to Kodak MR film. To evaluate binding, optical density readings are converted fmol/mg tissue using 125I-standards. |
Animal experiment: | Monkeys: Once stable dyskinesias develops, the effects of ABT-089 and Sofiniclin are determined on LIDs. For these studies, there are two sets of MPTP-lesioned monkeys, Set A (n = 17) and Set B (n = 16). Set A monkeys have previously been treated with nicotine and/or nAChR drugs, followed by a 10 week ishout period (nAChR drug-primed). Set B monkeys have not received any nAChR drug when ABT-089 treatment is initiated (nAChR drug-naive). Our rationale for the use of these two sets of monkeys is to determine if prior treatment with nAChR drugs altered their ability to decrease LIDs. For both sets, there are 3 experimental groups of monkeys, a vehicle-treated group (n = 6), a nAChR drug-treated group (n = 5 or 6) and a nicotine-treated group (n = 5), as a positive control. The monkeys are assigned to the groups such that there are similar number of males and females, with comparable average LID scores. |
References: [1]. Zhang D, et al. ABT-089 and ABT-894 reduce levodopa-induced dyskinesias in a monkey model of Parkinson's disease. Mov Disord. 2014 Apr;29(4):508-17. | |
| Cas No. | 799279-80-4 | SDF | |
| المرادفات | ABT 894 | ||
| Canonical SMILES | ClC1=C(Cl)C=C(N2C[C@]3([H])CN[C@]3([H])C2)C=N1 | ||
| Formula | C10H11Cl2N3 | M.Wt | 244.12 |
| الذوبان | DMSO : 35.71 mg/mL (146.28 mM; ultrasonic and warming and heat to 60°C) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 4.0963 mL | 20.4817 mL | 40.9635 mL |
| 5 mM | 0.8193 mL | 4.0963 mL | 8.1927 mL |
| 10 mM | 0.4096 mL | 2.0482 mL | 4.0963 mL |
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