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187665-65-2

187665-65-2 Structure

187665-65-2 Structure
IdentificationBack Directory
[Name]

(1S)-1-[2-[4-[4-(AMINOCARBONYL)PHENYL]-1-PIPERAZINYL]ETHYL]-3,4-DIHYDRO-N-METHYL-1H-2-BENZOPYRAN-6-CARBOXAMIDE
[CAS]

187665-65-2
[Synonyms]

PNU 142633
(1S)-1-[2-[4-[4-(AMINOCARBONYL)PHENYL]-1-PIPERAZINYL]ETHYL]-3,4-DIHYDRO-N-METHYL-1H-2-BENZOPYRAN-6-CARBOXAMIDE
[Molecular Formula]

C24H30N4O3
[MDL Number]

MFCD10687093
[MOL File]

187665-65-2.mol
[Molecular Weight]

422.52
Chemical PropertiesBack Directory
[Boiling point ]

652.5±55.0 °C(Predicted)
[density ]

1?+-.0.06 g/cm3(Predicted)
[storage temp. ]

Store at +4°C
[solubility ]

Soluble to 100 mM in DMSO
[form ]

Powder
[pka]

15.27±0.40(Predicted)
[color ]

White to off-white
Hazard InformationBack Directory
[Uses]

PNU 142633 is a high affinity SR-1D agonist.
[Biological Activity]

Very selective, high affinity 5-HT 1D receptor agonist (K i values are 6 and > 18000 nM at human 5-HT 1D and 5-HT 1B receptors respectively). Inhibits sympathetically-induced tachycardic responses and blocks neurogenic plasma protein extravasation in vivo .
[in vivo]

PNU-142633 (0.03-1 mg/kg; intravenous injection; male Hartley guinea pigs) treatment blocks neurogenic plasma protein extravasation. And PNU-142633 fails to alter resistance in these vascular beds[1].

Animal Model:Male Hartley guinea pigs (250-300 g) stimulated with bipolar electrode[1]
Dosage:0.03 mg/kg, 0.1 mg/kg, 0.3 mg/kg, 1 mg/kg
Administration:Intravenous injection
Result:Significantly reduced extravasation at the 0.1 and 0.3 mg/kg doses, but was without effect at the 0.03 and 1.0 mg/kg doses.
[IC 50]

5-HT1D Receptor: 6 nM (Ki)
[storage]

Store at +4°C
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