DBO-83 (Synonyms:DBO-83 dihydrochloride)
目录号 : KCM12306 CAS No. : 195211-53-1 纯度 : ≥98%
DBO-83 is an agonist of nicotinic acetylcholine receptors (nAChRs) with antinociceptive and anti-amnesic activities. It binds to nAChRs in rat cortical membranes with a K value of 4.1 nM in a radioligand binding assay with the α4β2 nAChR partial agonist and α7 nAChR agonist [H]cytisine. DBO-83 dose-dependently increases the latency to paw licking in mice in the hot plate test and reduces the number of abdominal constrictions in mice in the acetic acid abdominal constriction test, effects that can be reduced by the nAChR antagonist mecamylamine . DBO-83 also dose-dependently prevents amnesia induced by mecamylamine, the muscarinic receptor antagonist scopolamine, and the nAChR antagonist dihydro-β-erythroidine in mice in the passive avoidance test.
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1mg
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5mg
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10mg
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生物活性

DBO-83 is a brain-penetrant nicotinic acetylcholine receptor (nAChR) agonist. DBO-83  activates peripheral nicotinic acetylcholine receptors to evoke non-stimulated ileum contractions. DBO-83 shows antinociceptive and anti-amnesic activities.

体外研究

DBO-83  (10 µM) exhibits high selectivity towards [3H] - cytisine labeled nicotinic receptors, inhibiting 85% of binding at a concentration of 10 µM and showing no activity towards a group of other receptor types.
DBO-83  can contract the isolated ileum fragment of guinea pigs, with an EC50 of 3.05 μM.

体内研究

DBO-83 (1-20 mg/kg; intraperitoneal injection;  (5-7.5 µg per mouse; intraventricular injection) can induce dose-dependent central mediated analgesic effects in mouse hot plate tests.
DBO-83 (5-20 mg/kg; subcutaneous injection)  induced dose-dependent analgesic effects in mouse abdominal contraction test.
DBO-83 (10-20 mg/kg; intraperitoneal injection)  induced dose-dependent analgesic effects in the paw pressure test in rats. The maximum paw pressure threshold measured 15 minutes after intraperitoneal injection of 20 mg/kg was 104.6 g .
DBO-83 (1-10 mg/kg; intraperitoneal injection)  has anti forgetting effects on mice.

 

Animal Model: Swiss albino mice in the hot-plate tests (male, 23-30 g)
Dosage:
1 mg/kg; 5 mg/kg; 10 mg/kg; 20 mg/kg (i.p.); 5 µg per mouse; 7.5 µg per mouse (i.c.v.)
Administration: i.p.; i.c.v.
Result: Produced a dose-dependent increase in licking latency, peaking 15-30 minutes after injection.
Reached licking latencies of 32.3 sec at 15 minutes, 30.4 sec at 30 minutes, and 25.9 sec at 45 minutes at 10 mg/kg i.p..
Animal Model: Amnesic mice
Dosage: 1, 5, 10 mg/kg
Administration: i.p.
Result:
Prevented amnesia induced by Scopolamine, Mecamylamine and dihydro-β-erythroidine.
 
分子式
C10H13ClN4.2HCl
分子量
297.61
CAS号
195211-53-1
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
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