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1977-11-3

1977-11-3 Structure

1977-11-3 Structure
IdentificationBack Directory
[Name]

perlapine
[CAS]

1977-11-3
[Synonyms]

HF 2333
Hypnodin
AW 14-2333
6-(4-Methyl-1-piperazinyl)-11H-dibenz[b,e]azepin
6-(4-Methyl-1-piperazinyl)-11H-dibenz[b,e]azepine
11H-Dibenz[b,e]azepine, 6-(4-methyl-1-piperazinyl)-
6-(4-methylpiperazin-1-yl)-11H-benzo[c][1]benzazepine
[Molecular Formula]

C19H21N3
[MDL Number]

MFCD00867539
[MOL File]

1977-11-3.mol
[Molecular Weight]

291.39
Chemical PropertiesBack Directory
[Melting point ]

136-138°
[Boiling point ]

423.4°C (rough estimate)
[density ]

1.0521 (rough estimate)
[refractive index ]

1.6080 (estimate)
[storage temp. ]

Store at -20°C
[solubility ]

DMF: 10 mg/ml; DMSO: 10 mg/ml; DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml; Ethanol: 5 mg/ml
[form ]

A crystalline solid
[pka]

8.00±0.20(Predicted)
[color ]

White
Hazard InformationBack Directory
[Uses]

Perlapine exhibits antipsychotic activity and blocks dopamine and serotonin receptors. Perlapine is also a novel agonist of hM3Dq, a designer receptor exclusively activated by designer drugs (DREADD).
[Uses]

Perlapine is an atypical neuroleptic that blocks dopamine and serotonin (5-HT) receptors (Kis = 60, 30, and 30 nM for D2, D4, and 5-HT2A, respectively). Perlapine is also an agonist for hM3Dq, a designer receptor exclusively activated by designer drugs (DREADD) derived from the human muscarinic acetylcholine M3 receptor that activates neuronal firing. Perlapine displays >10,000-fold selectivity for hM3Dq over hM3.
[Definition]

ChEBI: Perlapine is an organic molecular entity.
[storage]

Store at -20°C
Safety DataBack Directory
[Toxicity]

LD50 in male, female mice, rats (mg/kg): 61, 61, 60, 66 i.v.; 250, 300, 480, 420 s.c., 270, 280, 660, 720 orally (Yokotani)
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