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187665-60-7

187665-60-7 Structure

187665-60-7 Structure
IdentificationBack Directory
[Name]

PNU 109291
[CAS]

187665-60-7
[Synonyms]

PNU 109291
(S)-3,4-DIHYDRO-1-[2-[4-(4-METHOXYPHENYL)-1-PIPERAZINYL]ETHYL]-N-METHYL-1H-2-BENZOPYRAN-6-CARBOXAMIDE
1H-2-Benzopyran-6-carboxamide, 3,4-dihydro-1-[2-[4-(4-methoxyphenyl)-1-piperazinyl]ethyl]-N-methyl-, (1S)-
[Molecular Formula]

C24H31N3O3
[MDL Number]

MFCD10687095
[MOL File]

187665-60-7.mol
[Molecular Weight]

409.52
Chemical PropertiesBack Directory
[Boiling point ]

595.8±50.0 °C(Predicted)
[density ]

1.143±0.06 g/cm3(Predicted)
[storage temp. ]

Store at +4°C
[solubility ]

Soluble to 100 mM in DMSO and to 100 mM in ethanol
[form ]

Powder
[pka]

15.27±0.40(Predicted)
Hazard InformationBack Directory
[Uses]

PNU 109291 is a 5-?HT receptor agonist.
[Biological Activity]

Potent and selective 5-HT 1D receptor agonist that displays > 600-fold selectivity over 5-HT 1A and 5-HT 2A receptors and no activity at 5-HT 1B , 5-HT 1E , 5-HT 2B , 5-HT 2C , 5-HT 6 and 5-HT 7 receptors. Reduces dural plasma extravasation evoked by trigeminal ganglion stimulation.
[in vivo]

PNU109291 (0.24, 2.4, 7.3, 24.4, 73.3 nmol/kg; s.c.) reduces dural plasma extravasation evoked by trigeminal ganglion stimulation in pigs[1].
PNU109291 (3 μM) inhibited evoked EPSCs (excitatory postsynaptic currents) in Freund's adjuvant (CFA) but not saline-injected rats[2].

Animal Model:200-500g, male Hartley guinea pigs[1]
Dosage:0.24, 2.4, 7.3, 24.4, 73.3 nmol/kg
Administration:S.c.; 60 min before electrical stimulation
Result:Dose-dependently decreased plasma protein extravasation with an IC50 value of 4.2 nmol/kg.
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