133737-32-3
133737-32-3 structure
- Name: Pagoclone
- Chemical Name: pagoclone
- CAS Number: 133737-32-3
- Molecular Formula: C23H22ClN3O2
- Molecular Weight: 407.89300
- Catalog: Signaling Pathways Membrane Transporter/Ion Channel GABA Receptor
- Create Date: 2018-06-12 13:02:15
- Modify Date: 2024-01-06 10:52:39
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Pagoclone is an active (+)-enantiomer of the racemate RP 59037. Pagoclone is a partial GABA(A) receptor agonist used for the treatment of panic and anxiety disorders.
| Name | pagoclone |
|---|---|
| Synonyms |
rac-pagoclone
2-(7-Chloro-1,8-naphthyridin-2-yl)-3-(5-Methyl-2-oxohexyl)isoindolin-1-one 2-(7-chloro-1,8-naphthyridine-2-yl)-3-(5-methyl-2-oxo-hexyl)-1-isoindolinone Ip 456 |
| Description | Pagoclone is an active (+)-enantiomer of the racemate RP 59037. Pagoclone is a partial GABA(A) receptor agonist used for the treatment of panic and anxiety disorders. |
|---|---|
| Related Catalog | |
| In Vitro | Pagoclone has high and approximately equivalent affinity (Ki values=0.7-9.1 nM) for recombinant human GABAA receptors containing either an α1, α2, α3 or α5 subunit. Pagoclone has significant agonist activity at all four diazepam-sensitive GABAA receptor subtypes, with EC50 of 3.1-6.6 nM[1]. |
| 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]. |
| Animal Admin | The rat chain-pulling assay is a test for sedation. In brief, food-deprived PVG rats (250-300 g, n=12/group) are trained on a random probability interval schedule of 60 s following which animals are given doses of either vehicle (0.5% methyl cellulose, 1 mL/kg p.o.), pagoclone (1, 3 or 10 mg/kg p.o.) or, as a positive control, diazepam (10 mg/kg p.o.). Immediately after dosing, animals are placed in the operant box and the rates at which rats pulled a chain for a food reward are recorded over a 60 min period. Data is expressed as a mean percentage of the baseline chain pulls per minute and then analysed using an ANOVA followed by Dunnett's t-tests to compare each treatment group to the vehicle control group. |
| References |
| Density | 1.273g/cm3 |
|---|---|
| Boiling Point | 582.1ºC at 760mmHg |
| Molecular Formula | C23H22ClN3O2 |
| Molecular Weight | 407.89300 |
| Flash Point | 305.9ºC |
| Exact Mass | 407.14000 |
| PSA | 63.16000 |
| LogP | 5.44510 |
| Vapour Pressure | 1.53E-13mmHg at 25°C |
| Index of Refraction | 1.625 |