Introduction：Basic information about CAS 133737-32-3|Pagoclone, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | Pagoclone |
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| CAS Number | 133737-32-3 | Molecular Weight | 407.89300 |
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| Density | 1.273g/cm3 | Boiling Point | 582.1ºC at 760mmHg |
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| Molecular Formula | C23H22ClN3O2 | Melting Point | / |
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| MSDS | / | Flash Point | 305.9ºC |
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Names
| Name | pagoclone |
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| Synonym | More Synonyms |
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Pagoclone BiologicalActivity
| 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. |
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| Related Catalog | Signaling Pathways >>Membrane Transporter/Ion Channel >>GABA ReceptorSignaling Pathways >>Neuronal Signaling >>GABA ReceptorResearch Areas >>Neurological Disease |
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| 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]. |
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| 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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| 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. |
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| References | [1]. Atack JR, et al. The in vivo properties of pagoclone in rat are most likely mediated by 5'-hydroxy pagoclone. Neuropharmacology. 2006 May;50(6):677-89. |
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Chemical & Physical Properties
| Density | 1.273g/cm3 |
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| Boiling Point | 582.1ºC at 760mmHg |
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| Molecular Formula | C23H22ClN3O2 |
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| Molecular Weight | 407.89300 |
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| Flash Point | 305.9ºC |
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| Exact Mass | 407.14000 |
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| PSA | 63.16000 |
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| LogP | 5.44510 |
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| Vapour Pressure | 1.53E-13mmHg at 25°C |
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| Index of Refraction | 1.625 |
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| InChIKey | HIUPRQPBWVEQJJ-UHFFFAOYSA-N |
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| SMILES | CC(C)CCC(=O)CC1c2ccccc2C(=O)N1c1ccc2ccc(Cl)nc2n1 |
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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 |
