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PF-3845

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Chemical compound

Pharmaceutical compound

PF-3845
Clinical data

ATC code	None
Legal status
Legal status	US: Investigational New Drug
Identifiers
IUPAC name N-3-pyridinyl-4-([3-([5-(trifluoromethyl)-2-pyridinyl]oxy)phenyl]methyl)-1-piperidinecarboxamide
CAS Number	1196109-52-0
PubChemCID	25154867
ChemSpider	26232165
UNII	Q3PW846TYN
CompTox Dashboard(EPA)	DTXSID40648905
Chemical and physical data
Formula	C₂₄H₂₃F₃N₄O₂
Molar mass	456.469 g·mol⁻¹
3D model (JSmol)	Interactive image
SMILES O=C(NC1=CN=CC=C1)N(CC2)CCC2CC3=CC=CC(OC4=NC=C(C(F)(F)F)C=C4)=C3
InChI InChI=1S/C24H23F3N4O2/c25-24(26,27)19-6-7-22(29-15-19)33-21-5-1-3-18(14-21)13-17-8-11-31(12-9-17)23(32)30-20-4-2-10-28-16-20/h1-7,10,14-17H,8-9,11-13H2,(H,30,32) Key:NBOJHRYUGLRASX-UHFFFAOYSA-N

PF-3845 is a selectiveinhibitor offatty acid amide hydrolase.^[1] It results in increased levels ofanandamide and results incannabinoid receptor-based effects. It hasanti-inflammatory action inmice colitis models.Antidiarrheal andantinociceptive effects were also seen in mouse models of pain.^[2]

A 2017 study published in the Journal of Psychiatry and Neuroscience found that PF-3845 exerts rapid and long-lasting anti-anxiety effects in mice exposed acutely to stress or chronically to the stress hormone corticosterone.^[3]

References

[edit]

^Ahn K, Johnson DS, Mileni M, Beidler D, Long JZ, McKinney MK, et al. (April 2009)."Discovery and characterization of a highly selective FAAH inhibitor that reduces inflammatory pain".Chemistry & Biology.16 (4):411–20.doi:10.1016/j.chembiol.2009.02.013.PMC 2692831.PMID 19389627.
^Fichna J, Sałaga M, Stuart J, Saur D, Sobczak M, Zatorski H, et al. (April 2014)."Selective inhibition of FAAH produces antidiarrheal and antinociceptive effect mediated by endocannabinoids and cannabinoid-like fatty acid amides".Neurogastroenterology and Motility.26 (4):470–81.doi:10.1111/nmo.12272.PMID 24460851.S2CID 2473356.
^Duan T, Gu N, Wang Y, Wang F, Zhu J, Fang Y, et al. (June 2017)."Fatty acid amide hydrolase inhibitors produce rapid anti-anxiety responses through amygdala long-term depression in male rodents".Journal of Psychiatry & Neuroscience.42 (4):230–241.doi:10.1503/jpn.160116.PMC 5487270.PMID 28234213.

Cannabinoid receptor modulators

Receptor
(ligands)

CB₁Tooltip Cannabinoid receptor type 1

Agonists (abridged, full list)	2-AG 2-AGE (noladin ether) 11-Hydroxy-THC α-Amyrin · β-Amyrin AB-CHMINACA AM-1172 AM-1220 AM-1221 AM-1235 AM-2201 AM-2232 Anandamide Arvanil AZ-11713908 Cannabinol CB-13 CP 47,497 CP 55,940 Dimethylheptylpyran DEA ECG EGCG Epicatechin Gallocatechol (gallocatechin) Honokiol HU-210 JWH-007 JWH-015 JWH-018 JWH-073 Kavain L-759,633 Levonantradol Menabitan Nabilone Nabitan NADA O-1812 Oleamide Pravadoline Serinolamide A THC (dronabinol) UR-144 WIN 55,212-2 Yangonin
Inverse agonists	AM-251 INV-202 Monlunabant Rimonabant Surinabant Taranabant TM-38837 Zevaquenabant
Antagonists	AM-6545 Cannabidiol Cannabigerol Drinabant Falcarinol (carotatoxin) Hemopressin Ibipinabant LY-320,135 MK-9470 NESS-0327 O-2050 Otenabant PF-514273 PipISB Rosonabant Selonabant THCV VCHSR Virodhamine

CB₂Tooltip Cannabinoid receptor type 2

Agonists

Antagonists

NAGly
(GPR18)

Agonists	Abnormal cannabidiol ACPA AM251 Anandamide Cannabidiol NADGly THC (dronabinol) O-1602
Antagonists	PSB-CB5 O-1918

GPR55

Agonists	2-AGE (noladin ether) 2-ALPI Abnormal cannabidiol AM-251 CID1011163 CID1252842 CID1792579 CP 55,940 GSK-494581A Lysophosphatidylinositol ML-184 ML-185 ML-186 O-1602 Oleoylethanolamide Palmitoylethanolamide THC (dronabinol)
Antagonists	Cannabidiol CID-16020046 ML-191 ML-192 ML-193 O-1918 PSB-SB-487 PSB-SB-1202 PSB-SB-1203 Tetrahydromagnolol

GPR119

Agonists	2-Oleoylglycerol Anandamide APD668 AR-231,453 AS-1269574 MBX-2982 N-Oleoyldopamine Oleoylethanolamide Olvanil PSN-375,963 PSN-632,408

Transporter
(modulators)

eCBTsTooltip Endocannabinoid transporter	Inhibitors:5'-DMH-CBD AM-404 AM-1172 Arachidonoyl serotonin Arvanil Cannabidiol Guineensine LY-2183240 O-2093 OMDM-2 Paracetamol (acetaminophen) SB-FI-26 UCM-707 URB-597 VDM-11 WOBE490 WOBE491 WOBE492

Enzyme
(modulators)

FAAHTooltip Fatty acid amide hydrolase	Inhibitors:4-Nonylphenylboronic acid AACOCF₃ AM-404 Arachidonoyl serotonin BIA 10-2474 Biochanin A BMS-986368 Genistein IDFP JNJ-1661010 JNJ-42165279 JZL-195 Kaempferol LY-2183240 MAFP Palmitoylisopropylamide Paracetamol (acetaminophen) PF-3845 PF-750 Redafamdastat (JZP-150, PF-04457845) SA-47 SA-57 TAK 21d TC-F 2 TPT-0201 UCM710 URB-597 Activators:PDP-EA
MAGL	Inhibitors:BMS-986368 Elcubragistat (ABX-1431; Lu-AG06466) IDFP JJKK 048 JW 642 JZL-184 JZL-195 JZP-361 KML 29 Lu-AG06474 MAFP MJN110 NAM PF-6818883 Pristimerin RG-6182 TPT-0201 TPT-0801 URB-602 URB-754
ABHD6	Inhibitors:JZP-169 JZP-430 KT182 KT185 KT195 KT203 LEI-106 ML294 ML295 ML296 UCM710 WWL-70
ABHD12	Inhibitors:Betulinic acid Maslinic acid MAFP Oleanolic acid Orlistat (tetrahydrolipstatin) Ursolic acid

Others

Others:2-PG(directly potentiates activity of 2-AG at CB₁ receptor)
ARN-272(FAAH-like anandamide transporter inhibitor)

See also: Receptor/signaling modulators; Cannabinoids (cannabinoids by structure)

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