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PF-03654746

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Chemical compound

Pharmaceutical compound

PF-03654746
Identifiers

IUPAC name trans-N-Ethyl-3-fluoro-3-[3-fluoro-4-(1-pyrrolidinylmethyl)phenyl]cyclobutanecarboxamide
CAS Number	935840-31-6^Y
PubChemCID	16119086
ChemSpider	25069700
UNII	G3QE979K1X
Chemical and physical data
Formula	C₁₈H₂₄F₂N₂O
Molar mass	322.400 g·mol⁻¹
3D model (JSmol)	Interactive image
SMILES CCNC(=O)[C@H]1C[C@@](C1)(F)C2=CC(=C(C=C2)CN3CCCC3)F
InChI InChI=1S/C18H24F2N2O/c1-2-21-17(23)14-10-18(20,11-14)15-6-5-13(16(19)9-15)12-22-7-3-4-8-22/h5-6,9,14H,2-4,7-8,10-12H2,1H3,(H,21,23)/t14-,18- Key:SXMBKHYDZOCBMT-PPUGGXLSSA-N
(verify)

PF-03654746 is a potent and selectivehistamine H₃ receptor antagonist developed byPfizer and currently undergoingclinical trials for the treatment ofADHD,Tourette syndrome^[1] as well as potential anti-allergy applications.^[2]^[3]^[4]^[5]

^Clinical trial numberNCT01475383 for "Study Evaluating The Safety And Efficacy Of PF-03654746 In Adult Subjects With Tourette's Syndrome" atClinicalTrials.gov
^Soares H, Wager TT, Schmidt AW, Sweeney FJ, McLellan TJ, Nelson FR, Spracklin D, Wang EQ, Faessel H, Pinter GW, Li X (2010)."The Effects of an H3 Receptor Antagonist in a Nasal Allergen Challenge Model".Journal of Allergy and Clinical Immunology.125 (2): AB191.doi:10.1016/j.jaci.2009.12.750.
^"H3 receptor antagonism increases methylhistamine levels in the cerebrospinal fluid of dogs and healthy human volunteers".Alzheimer's & Dementia.5 (4): P254.doi:10.1016/j.jalz.2009.04.272.S2CID 54316270.
^Gemkow MJ, Davenport AJ, Harich S, Ellenbroek BA, Cesura A, Hallett D (May 2009). "The histamine H3 receptor as a therapeutic drug target for CNS disorders".Drug Discovery Today.14 (9–10):509–15.doi:10.1016/j.drudis.2009.02.011.PMID 19429511.
^Wijtmans M, Denonne F, Célanire S, Gillard M, Hulscher S, Delaunoy C, Bakker RA, Defays S, Gérard J, Grooters L, Hubert D (2010). "Histamine H3 receptor ligands with a 3-cyclobutoxy motif: a novel and versatile constraint of the classical 3-propoxy linker".MedChemComm.1: 39.doi:10.1039/c0md00056f.

Agonists

Antagonists

Agonists	Amthamine Betazole Dimaprit Histamine HTMT Impromidine L-Histidine UR-AK49
Antagonists	Bisfentidine Burimamide Cimetidine Dalcotidine Donetidine Ebrotidine Etintidine Famotidine Isolamtidine Lafutidine Lamtidine Lavoltidine (loxtidine) Lupitidine Metiamide Mifentidine Niperotidine Nizatidine Osutidine Oxmetidine Pibutidine Quisultazine (quisultidine) Ramixotidine Ranitidine Roxatidine Sufotidine Tiotidine Tuvatidine Venritidine Xaltidine Zolantidine

Agonists	α-Methylhistamine BP 2.94 Cipralisant (GT-2331) GT-2203 (VUF-5296) Histamine Imetit Immepip Immethridine (BP-1-5375) L-Histidine Methimepip Proxyfan SCH-50971 VUF-5297
Antagonists	A-349821 A-423579 ABT-239 ABT-652 AZD5213 Bavisant Betahistine Burimamide Ciproxifan Clobenpropit Conessine Enerisant GSK-189254 Impentamine Iodophenpropit Irdabisant JNJ-5207852 NNC 38-1049 PF-03654746 Pitolisant SCH-79687 Thioperamide VUF-5681

Agonists	4-Methylhistamine α-Methylhistamine Histamine L-Histidine OUP-16 VUF-8430
Antagonists	JNJ-7777120 Mianserin Seliforant Thioperamide Toreforant VUF-6002

See also: Receptor/signaling modulators; Monoamine metabolism modulators; Monoamine reuptake inhibitors

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