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Fosnetupitant (Pronetupitant)

Names

[ CAS No. ]:
1703748-89-3

[ Name ]:
Fosnetupitant (Pronetupitant)

Biological Activity

[Description]:

Fosnetupitant (Pronetupitant) a methylene phosphate prodrug of Netupitant. Fosnetupitant (Pronetupitant) exhibits a pKi of 9.5 for human NK1 receptor[1].

[Related Catalog]:

Signaling Pathways >> Neuronal Signaling >> Neurokinin Receptor
Research Areas >> Neurological Disease
Signaling Pathways >> GPCR/G Protein >> Neurokinin Receptor

[In Vitro]

Fosnetupitant (Pronetupitant) displays micromolar affinity for the 5-HT6 (pKi ∼ 5.2) receptor and type L Ca2+ channels (pKi ∼ 5.7) and does not bind all the other proteins investigated[1].

[In Vivo]

Pronetupitant is rapidly and extensively converted to Netupitant after i.v. injection in rats[1].

[References]

[1]. Ruzza C, et al. In vitro and in vivo pharmacological characterization of Pronetupitant, a prodrug of the neurokinin 1 receptor antagonist Netupitant. Peptides. 2015 Jul;69:26-32.

Chemical & Physical Properties

[ Molecular Formula ]:
C31H35F6N4O5P

[ Molecular Weight ]:
688.598

[ Exact Mass ]:
688.224915

[ LogP ]:
1.86


Related Compounds

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