PF-04457845
Chemical compound
- None
- US: Investigational New Drug
- N-pyridazin-3-yl-4-[(3-[5-(trifluoromethyl)pyridin-2-yl]oxyphenyl)methylidene]piperidine-1-carboxamide
- 1020315-31-4 Y
- 24771824
- 26390839
- H4C81M8YYW
- ChEMBL1651534
- DTXSID00144539
- Interactive image
- 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]
See also
- FAAH inhibitor
- 4-Nonylphenylboronic acid
- LY-2183240
- URB-597
- BIA 10-2474, problems in phase 1
References
- ^ 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.
- v
- t
- e
(comparison)
Cannabibutols |
|
---|---|
Cannabichromenes | |
Cannabicyclols |
|
Cannabidiols | |
Cannabielsoins |
|
Cannabigerols | |
Cannabiphorols |
|
Cannabinols | |
Cannabitriols |
|
Cannabivarins |
|
Delta-8-tetrahydrocannabinols |
|
Delta-9-tetrahydrocannabinols | |
Delta-10-Tetrahydrocannabinols | |
Miscellaneous cannabinoids |
|
Active metabolites |
- Arachidonoyl ethanolamide (AEA; anandamide)
- 2-Arachidonoylglycerol (2-AG)
- 2-Arachidonyl glyceryl ether (2-AGE; noladin ether)
- 2-Oleoylglycerol (2-OG)
- N-Arachidonoyl dopamine (NADA)
- N-Arachidonylglycine (NAGly)
- 2-Arachidonoyl lysophosphatidylinositol (2-ALPI)
- N-Arachidonoyl serotonin (AA-5-HT)
- Docosatetraenoylethanolamide (DEA)
- Lysophosphatidylinositol (LPI)
- Oleamide
- Oleoylethanolamide (OEA)
- Palmitoylethanolamide (PEA)
- RVD-Hpα
- Stearoylethanolamide (SEA)
- O-Arachidonoyl ethanolamine (O-AEA; virodhamine)
cannabinoid
receptor
agonists /
neocannabinoids
Classical cannabinoids (dibenzopyrans) |
|
---|---|
Non-classical cannabinoids |
|
Adamantoylindoles |
|
Benzimidazoles | |
Benzoylindoles |
|
Cyclohexylphenols | |
Eicosanoids |
|
Hydrocarbons | |
Indazole carboxamides | |
Indazole-3- carboxamides |
|
Indole-3-carboxamides |
|
Indole-3-carboxylates | |
Naphthoylindazoles | |
Naphthoylindoles |
|
Naphthoylpyrroles | |
Naphthylmethylindenes | |
Naphthylmethylindoles | |
Phenylacetylindoles | |
Pyrazolecarboxamides |
|
Pyrrolobenzoxazines | |
Quinolinyl esters | |
Tetramethylcyclo- propanoylindazoles | |
Tetramethylcyclo- propanoylindoles | |
Tetramethylcyclo- propylindoles | |
Others |
|
enhancers
(inactivation inhibitors)
- 4-Nonylphenylboronic acid
- AM-404
- Arachidonoyl serotonin
- Arvanil
- BIA 10-2474
- Biochanin A
- CAY-10401
- CAY-10429
- Genistein
- Guineesine
- IDFP
- JNJ 1661010
- JNJ-42165279
- JZL184
- JZL195
- Kaempferol
- LY-2183240
- MK-4409
- O-1624
- O-2093
- Oleoylethanolamide (OEA)
- Olvanil
- Palmitoylethanolamide (PEA)
- PF-04457845
- PF-622
- PF-750
- PF-3845
- PHOP
- URB-447
- URB-597
- URB-602
- URB-754
- VDM-11
(antagonists/inverse
agonists/antibodies)
- AM-251
- AM-281
- AM-630
- AM-1387
- AM-4113
- AM-6527
- AM-6545
- BML-190
- Brizantin (Бризантин)
- CAY-10508
- CB-25
- CB-52
- CB-86
- Dietressa (Диетресса)
- Drinabant (AVE1625)
- Hemopressin
- Ibipinabant (SLV319)
- JTE-907
- LH-21
- LY-320,135
- MDA-77
- MJ-15
- MK-9470
- NESS-0327
- NIDA-41020
- O-606
- O-1184
- O-1248
- O-1918
- O-2050
- O-2654
- Otenabant (CP-945,598)
- PF-514273
- PipISB
- PSB-SB-487
- Rimonabant (SR141716)
- Rosonabant (E-6776)
- SR-144,528
- Surinabant (SR147778)
- Taranabant (MK-0364)
- TM-38837
- VCHSR
- See also: Cannabinoid receptor modulators (cannabinoids by pharmacology)
- List of: AM cannabinoids
- JWH cannabinoids
- Designer drugs § Synthetic cannabimimetics