ChemicalBook CAS DataBase List 1621164-74-6

1621164-74-6

Name	camlipixant
CAS	1621164-74-6
Molecular Formula	C23H24F2N4O4
Molecular Weight	458.46
MOL File	1621164-74-6.mol

Chemical Properties

form	Solid
color	White to off-white
InChIKey	SEHLMRJSQFAPCJ-HNNXBMFYSA-N
SMILES	N1(C(OC)=O)CCO[C@@H](CC2N3C(=NC=2C2=C(F)C=C(C(NC)=O)C=C2F)C=C(C)C=C3)C1

Hazard Information

Chemical Properties

Camlipixant is a purinoreceptor antagonist.

Uses

Camlipixant (BLU-5937) a potent, selective, non-competitive and orally active P2X3 homotrimeric receptor antagonist with an IC50 of 25 nM against hP2X3 homotrimeric. Camlipixant shows potent anti-tussive effect and no taste alteration. Camlipixant can be used for the research of unexplained, refractory chronic cough[1].

Biological Activity

in vivo

Camlipixant (BLU-5937; 3-30 mg/kg; oral) reduces histamine- and ATP- induced cough hypersensitivity in guinea pigs^[1].
Camlipixant (BLU-5937; 10-20 mg/kg; i.p.) does not alter taste perception as compared to control animals^[1].
Camlipixant (BLU-5937) exhibits excellent drug-like characteristics, including good oral bioavailability, low predicted clearance in human, no blood-brain barrier permeability and high safety margin versus human predicted efficacious exposure^[1].

Animal Model:	Male Dunkin Hartley guinea pigs^[1]
Dosage:	0.3, 3, 30 mg/kg
Administration:	PO, approximately 2 h prior to tussive agent exposure
Result:	Significantly reduced the histamine-induced enhancement in the number of citric acid-induced coughs. Reduced significantly and dose-dependently the ATP-induced enhancement of citric acid-induced coughs.

References

[1] Garceau D, Chauret N. BLU-5937: A selective P2X3 antagonist with potent anti-tussive effect and no taste alteration. Pulm Pharmacol Ther. 2019 Jun;56:56-62. DOI:10.1016/j.pupt.2019.03.007

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