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JNJ-5207852

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JNJ-5207852
Names

Preferred IUPAC name 1-(3-{4-[(piperidin-1-yl)methyl]phenoxy}propyl)piperidine
Identifiers
CAS Number	398473-34-2^N
3D model (JSmol)	Interactive image
Abbreviations	JNJ-5207852
ChEMBL	ChEMBL129542^Y
ChemSpider	2046959^Y
IUPHAR/BPS	1256
MeSH	JNJ-5207852
PubChem CID	2766326
UNII	4I9OVB1G7D
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
Properties
Chemical formula	C₂₀H₃₂N₂O
Molar mass	316.480 g/mol
Except where otherwise noted, data are given for materials in theirstandard state (at 25 °C [77 °F], 100 kPa). N verify (what is ^YN ?) Infobox references

Chemical compound

JNJ-5207852 is ahistamine antagonist selective for theH₃ subtype. It hasstimulant andnootropic effects in animal studies,^[1] and has been suggested as a possible treatment for some memory defects associated withepilepsy.^[2] JNJ-5207852 itself did not progress to clinical development due to poor pharmacokinetic characteristics, but the related compoundJNJ-17216498 was in a Phase II clinical trial for the treatment ofnarcolepsy in 2007.^[3]

References

[edit]

^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.S2CID 39844562.
^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

Antagonists

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 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

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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