JNJ-5207852

JNJ-5207852 is a histamine antagonist selective for the H₃ subtype. It has stimulant and nootropic effects in animal studies,[1] and has been suggested as a possible treatment for memory defects associated with epilepsy.[2] JNJ-5207852 itself did not progress to clinical development due to poor pharmacokinetic characteristics, but the related compound JNJ-17216498 is currently in Phase II clinical trials for the treatment of narcolepsy.[3]

JNJ-5207852
Names

Preferred IUPAC name 1-{3-[4-(Piperidin-1-ylmethyl)phenoxy]propyl}piperidine
Systematic IUPAC name 1-({4-[3-(Piperidin-1-yl)propoxy]phenyl}methyl)piperidine
Identifiers
3D model (JSmol)	Interactive image Interactive image
Abbreviations	JNJ-5207852
ChEBI	CHEBI:312531^N
ChEMBL	ChEMBL129542^Y
ChemSpider	2046959^Y
IUPHAR/BPS	1256
MeSH	JNJ-5207852
PubChem CID	2766326
CompTox Dashboard (EPA)	DTXSID70377579
InChI InChI=1S/C20H32N2O/c1-3-12-21(13-4-1)16-7-17-23-20-10-8-19(9-11-20)18-22-14-5-2-6-15-22/h8-11H,1-7,12-18H2^Y Key: PTKHFRNHJULJKT-UHFFFAOYSA-N^Y
SMILES O(c1ccc(cc1)CN2CCCCC2)CCCN3CCCCC3 O(c1ccc(cc1)CN2CCCCC2)CCCN3CCCCC3
Properties
Chemical formula	C₂₀H₃₂N₂O
Molar mass	316.480 g/mol
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
N verify (what is ^YN ?)
Infobox references

References

Barbier AJ, Berridge C, Dugovic C, et al. (November 2004). "Acute wake-promoting actions of JNJ-5207852, a novel, diamine-based H3 antagonist". Br. J. Pharmacol. 143 (5): 649–61. doi:10.1038/sj.bjp.0705964. PMC 1575430. PMID 15466448.
Jia F, Kato M, Dai H, Xu A, Okuda T, Sakurai E, Okamura N, Lovenberg TW, Barbier A, Carruthers NI, Iinuma K, Yanai K (Mar 2006). "Effects of histamine H(3) antagonists and donepezil on learning and mnemonic deficits induced by pentylenetetrazol kindling in weanling mice". Neuropharmacology. 50 (4): 404–11. doi:10.1016/j.neuropharm.2005.09.017. PMID 16310812.
Esbenshade TA, Browman KE, Bitner RS, Strakhova M, Cowart MD, Brioni JD (July 2008). "The histamine H3 receptor: an attractive target for the treatment of cognitive disorders". Br. J. Pharmacol. 154 (6): 1166–81. doi:10.1038/bjp.2008.147. PMC 2483387. PMID 18469850.

Histamine receptor modulators
H₁	Agonists: 2-Pyridylethylamine Betahistine Histamine HTMT L-Histidine UR-AK49 Antagonists: First-generation: 4-Methyldiphenhydramine Alimemazine Antazoline Azatadine Bamipine Benzatropine (benztropine) Bepotastine Bromazine Brompheniramine Buclizine Captodiame Carbinoxamine Chlorcyclizine Chloropyramine Chlorothen Chlorphenamine Chlorphenoxamine Cinnarizine Clemastine Clobenzepam Clocinizine Cloperastine Cyclizine Cyproheptadine Dacemazine Decloxizine Deptropine Dexbrompheniramine Dexchlorpheniramine Dimenhydrinate Dimetindene Diphenhydramine Diphenylpyraline Doxylamine Embramine Etodroxizine Etybenzatropine (ethylbenztropine) Etymemazine Fenethazine Flunarizine Histapyrrodine Homochlorcyclizine Hydroxyethylpromethazine Hydroxyzine Isopromethazine Isothipendyl Meclozine Medrylamine Mepyramine (pyrilamine) Mequitazine Methafurylene Methapyrilene Methdilazine Moxastine Orphenadrine Oxatomide Oxomemazine Perlapine Phenindamine Pheniramine Phenyltoloxamine Pimethixene Piperoxan Pipoxizine Promethazine Propiomazine Pyrrobutamine Talastine Thenalidine Thenyldiamine Thiazinamium Thonzylamine Tolpropamine Tripelennamine Triprolidine Second/third-generation: Acrivastine Alinastine Astemizole Azelastine Bamirastine Barmastine Bepiastine Bepotastine Bilastine Cabastinen Carebastine Cetirizine Clemastine Clemizole Clobenztropine Desloratadine Dorastine Ebastine Efletirizine Emedastine Epinastine Fexofenadine Flezelastine Ketotifen Latrepirdine Levocabastine Levocetirizine Linetastine Loratadine Mapinastine Mebhydrolin Mizolastine Moxastine Noberastine Octastine Olopatadine Perastine Pibaxizine Piclopastine Quifenadine (phencarol) Rocastine Rupatadine Setastine Sequifenadine (bicarphen) Talastine Temelastine Terfenadine Vapitadine Zepastine Others: Atypical antipsychotics (e.g., aripiprazole, asenapine, brexpiprazole, brilaroxazine, clozapine, iloperidone, olanzapine, paliperidone, quetiapine, risperidone, ziprasidone, zotepine) Phenylpiperazine antidepressants (e.g., hydroxynefazodone, nefazodone, trazodone, triazoledione) Tetracyclic antidepressants (e.g., amoxapine, loxapine, maprotiline, mianserin, mirtazapine, oxaprotiline) Tricyclic antidepressants (e.g., amitriptyline, butriptyline, clomipramine, desipramine, dosulepin (dothiepin), doxepin, imipramine, iprindole, lofepramine, nortriptyline, protriptyline, trimipramine) Typical antipsychotics (e.g., chlorpromazine, flupenthixol, fluphenazine, loxapine, perphenazine, prochlorperazine, thioridazine, thiothixene) Unknown/unsorted: Azanator Belarizine Elbanizine Flotrenizine GSK1004723 Napactadine Tagorizine Trelnarizine Trenizine
H₂	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
H₃	Agonists: α-Methylhistamine Cipralisant Histamine Imetit Immepip Immethridine L-Histidine Methimepip Proxyfan 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
H₄	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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