NP118809

Names

[ Name ]:
NP118809

[Synonym ]:
1-benzhydryl-4-(3,3-diphenyl-propionyl)-piperazine
1-[4-(Diphenylmethyl)-1-piperazinyl]-3,3-diphenyl-1-propanone
1-Propanone, 1-[4-(diphenylmethyl)-1-piperazinyl]-3,3-diphenyl-
1-(4-Benzhydryl-piperazin-1-yl)-3,3-diphenyl-propan-1-one
1-(3,3-diphenylpropionyl)-4-benzhydryl piperazine
NP-118809
NP118809

Biological Activity

[Description]:

NP118809 is a potent N-type calcium channel blocker, with an IC50 of 0.11 μM; also less potently inhibits L-type calcium channel with an IC50 of 12.2 μM.

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> Calcium Channel

Research Areas >> Cardiovascular Disease

[Target]

N-Type Ca2+ Channel:0.11 μM (IC50)

L-type calcium channel:12.2 μM (IC50)

[In Vitro]

NP118809 is a potent N-type calcium channel blocker, with an IC50 of 0.11 μM; also inhibits L-type calcium channel with an IC50 of 12.2 μM. NP118809 inhibits the hERG potassium channel in HEK cells, with an IC50 of 7.4 μM[1].

[In Vivo]

NP118809 (25 mg/kg, i.p.) shows significant analgesic activity in the phase IIA portions of the rat formalin model[1]. NP118809 (30 mg/kg, p.o.) results in 80.3% inhibition of mechanical allodynia and 96.3% inhibition of thermal hyperalgesia in the rat spinal nerve ligation model[2].

[References]

[1]. Zamponi GW, et al. Scaffold-based design and synthesis of potent N-type calcium channel blockers. Bioorg Med Chem Lett. 2009 Nov 15;19(22):6467-72.

[2]. Pajouhesh H, et al. Structure-activity relationships of diphenylpiperazine N-type calcium channel inhibitors. Bioorg Med Chem Lett. 2010 Feb 15;20(4):1378-83.

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.1±0.1 g/cm3

[ Boiling Point ]:
618.9±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C₃₂H₃₂N₂O

[ Molecular Weight ]:
460.609

[ Flash Point ]:
251.4±23.9 °C

[ Exact Mass ]:
460.251465

[ PSA ]:
23.55000

[ LogP ]:
6.51

[ Vapour Pressure ]:
0.0±1.8 mmHg at 25°C

[ Index of Refraction ]:
1.622

[ Storage condition ]:
2-8℃

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Related Compounds

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