PAGOCLONE
PAGOCLONE Basic information
- Product Name:
- PAGOCLONE
- Synonyms:
-
- 2-(7-Chloro-1,8-naphthyridin-2-yl)-3-(5-methyl-2-oxohexyl)-1-isoindolinone
- RP 59037
- Ip 456
- Rp 62955
- 2-(7-Chloro-1,8-naphthyridin-2-yl)-3-(5-Methyl-2-oxohexyl)isoindolin-1-one
- (+)-RP-59037; IP-456; RP-62955; CI-1043
- CI-1043
- AGOCLONE
- CAS:
- 133737-32-3
- MF:
- C23H22ClN3O2
- MW:
- 407.89
- EINECS:
- 225-799-5
- Mol File:
- 133737-32-3.mol
PAGOCLONE Chemical Properties
- Boiling point:
- 582.1±50.0 °C(Predicted)
- Density
- 1.273±0.06 g/cm3(Predicted)
- pka
- 1.62±0.30(Predicted)
- form
- Solid
- color
- White to off-white
- InChI
- InChI=1S/C23H22ClN3O2/c1-14(2)7-10-16(28)13-19-17-5-3-4-6-18(17)23(29)27(19)21-12-9-15-8-11-20(24)25-22(15)26-21/h3-6,8-9,11-12,14,19H,7,10,13H2,1-2H3
- InChIKey
- HIUPRQPBWVEQJJ-UHFFFAOYSA-N
- SMILES
- C1(=O)C2=C(C=CC=C2)C(CC(=O)CCC(C)C)N1C1=CC=C2C(=N1)N=C(Cl)C=C2
PAGOCLONE Usage And Synthesis
Description
Pagoclone is a drug that belongs to the class of cyclopyrrolones. It binds to the benzodiazepine binding site on GABAA receptors and acts as a negative allosteric modulator, thereby enhancing the inhibitory effects of GABA and reducing neuronal excitability.
Uses
Anti-anxiety agent.
Application
Pagoclone has been shown to have anti-inflammatory properties in an animal model of inflammatory bowel disease and may be useful for the treatment of this condition.
brand name
Bextra (Interneuron).
in vivo
Pagoclone (3 mg/kg, p.o.) has significant anxiolytic-like activity, but at all three doses tested (0.3, 1 and 3 mg/kg p.o.) it produces a significant reduction in the total distance travelled. Pagoclone (3 mg/kg, p.o.) produces a dose-dependent increase in time spent on the open arms compared to control. Pagoclone (1, 3 or 10 mg/kg) lowers the cumulative chain-pulling response in the response sensitivity test. Plasma pagoclone concentrations are dose-dependent but not linear, with plasma concentrations of pagoclone being 0.4±0.1, 1.1±0.2 and 2.2±0.2 ng/mL, respectively. Pagoclone (0.3, 1 or 3 mg/kg) reduces locomotor activity in rats in a dose dependent manner[1].
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