PF-04457845 Knowpia

JZP150
Clinical data
ATC code	None;
Legal status
Legal status	US: Investigational New Drug;
Pharmacokinetic data
Metabolism	CY3A4
Identifiers
	IUPAC name N-pyridazin-3-yl-4-[(3-[5-(trifluoromethyl)pyridin-2-yl]oxyphenyl)methylidene]piperidine-1-carboxamide;
CAS Number	1020315-31-4 ;
PubChem CID	24771824;
ChemSpider	26390839;
UNII	H4C81M8YYW;
ChEMBL	ChEMBL1651534;
CompTox Dashboard (EPA)	DTXSID00144539 ;
Chemical and physical data
Formula	C23H20F3N5O2
Molar mass	455.441 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES n4ncccc4NC(=O)N(CC3)CC\C3=C/c2cc(ccc2)Oc(cc1)ncc1C(F)(F)F;
	InChI InChI=1S/C23H20F3N5O2/c24-23(25,26)18-6-7-21(27-15-18)33-19-4-1-3-17(14-19)13-16-8-11-31(12-9-16)22(32)29-20-5-2-10-28-30-20/h1-7,10,13-15H,8-9,11-12H2,(H,29,30,32); Key:BATCTBJIJJEPHM-UHFFFAOYSA-N;

JZP150 (formerly PF-04457845) is an inhibitor of the enzyme fatty acid amide hydrolase (FAAH), with an IC₅₀ of 7.2nM, and both analgesic and antiinflammatory effects in animal studies comparable to naproxen.^[1]

JZP150 is currently being developed by Jazz Pharmaceuticals and is in a Phase 2 trial in the US for PTSD. Patients will be given 0.3mg orally once per day for up to 12 weeks, or 4.0mg orally once per day for up to 12 weeks, or a placebo.^[2]

References edit

^ Johnson DS, Stiff C, Lazerwith SE, Kesten SR, Fay LK, Morris M, et al. (February 2011). "Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor". ACS Medicinal Chemistry Letters. 2 (2): 91–96. doi:10.1021/ml100190t. PMC 3109749. PMID 21666860.
^ "A Study of JZP150 in Adults With Posttraumatic Stress Disorder - Full Text View - ClinicalTrials.gov". clinicaltrials.gov.

[Johnson2011-1] Johnson DS, Stiff C, Lazerwith SE, Kesten SR, Fay LK, Morris M, et al. (February 2011). "Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor". ACS Medicinal Chemistry Letters. 2 (2): 91–96. doi:10.1021/ml100190t. PMC 3109749. PMID 21666860.

[2] "A Study of JZP150 in Adults With Posttraumatic Stress Disorder - Full Text View - ClinicalTrials.gov". clinicaltrials.gov.

[1]

[2]

Summary

See also edit

References edit

Clinical data

ATC code	None
Legal status
Legal status	US: Investigational New Drug
Pharmacokinetic data
Metabolism	CY3A4
Identifiers
IUPAC name N-pyridazin-3-yl-4-[(3-[5-(trifluoromethyl)pyridin-2-yl]oxyphenyl)methylidene]piperidine-1-carboxamide
CAS Number	1020315-31-4^Y
PubChem CID	24771824
ChemSpider	26390839
UNII	H4C81M8YYW
ChEMBL	ChEMBL1651534
CompTox Dashboard (EPA)	DTXSID00144539
Chemical and physical data
Formula	C₂₃H₂₀F₃N₅O₂
Molar mass	455.441 g·mol⁻¹
3D model (JSmol)	Interactive image
SMILES n4ncccc4NC(=O)N(CC3)CC\C3=C/c2cc(ccc2)Oc(cc1)ncc1C(F)(F)F
InChI InChI=1S/C23H20F3N5O2/c24-23(25,26)18-6-7-21(27-15-18)33-19-4-1-3-17(14-19)13-16-8-11-31(12-9-16)22(32)29-20-5-2-10-28-30-20/h1-7,10,13-15H,8-9,11-12H2,(H,29,30,32) Key:BATCTBJIJJEPHM-UHFFFAOYSA-N