PF 04479745

Names

[ Name ]:
PF 04479745

[Synonym ]:
MFCD28137682
PF-04479745
5H-Pyrimido[4,5-d]azepin-4-amine, 6,7,8,9-tetrahydro-N,9-dimethyl-2-(phenylmethyl)-, (9S)-
(9S)-2-Benzyl-N,9-dimethyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-d]azepin-4-amine
(9S)-6,7,8,9-Tetrahydro-N,9-dimethyl-2-(phenylmethyl)-5H-pyrimido[4,5-d]azepin-4-amine
PF-4479745

Biological Activity

[Description]:

PF-4479745 is a potent and selective 5-HT2C receptor agonist (EC50: 10 nM, ki: 15 nM). PF-4479745 can be used in the research of cardiovascular disease like hypertension[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

[Target]

5-HT2C Receptor:10 nM (EC50)

5-HT2C Receptor:15 nM (Ki)

5-HT2A Receptor:360 nM (IC50)

5-HT2B Receptor:67 nM (IC50)

5-HT1A Receptor:500 nM (IC50)

5-HT6 Receptor:280 nM (IC50)

[In Vitro]

PF-4479745 (copmpound 17) exhibits metabolic stability in both human liver microsomes (HLM) and human hepatocytes[1].

[In Vivo]

PF-4479745 (compound 17, intravenous injection) shows high clearance rate (104 mL/min/kg)[1]. PF-4479745 demonstrates a robust dose-dependent effect in canine PUP (peak urethral pressure) model of SUI (stress urinary incontinence)[1].

[References]

[1]. R Ian Storer, et al. Multiparameter optimization in CNS drug discovery: design of pyrimido[4,5-d]azepines as potent 5-hydroxytryptamine 2C (5-HT₂C) receptor agonists with exquisite functional selectivity over 5-HT₂A and 5-HT₂B receptors. J Med Chem. 2014 Jun 26;57(12):5258-69.

Chemical & Physical Properties

[ Density]:
1.1±0.1 g/cm3

[ Boiling Point ]:
473.4±45.0 °C at 760 mmHg

[ Molecular Formula ]:
C₁₇H₂₂N₄

[ Molecular Weight ]:
282.383

[ Flash Point ]:
240.1±28.7 °C

[ Exact Mass ]:
282.184448

[ LogP ]:
2.68

[ Vapour Pressure ]:
0.0±1.2 mmHg at 25°C

[ Index of Refraction ]:
1.590

Safety Information

[ RIDADR ]:
NONH for all modes of transport

Related Compounds

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