From Wikipedia, the free encyclopedia
JNJ-5207852
Names
Preferred IUPAC name
1-(3-{4-[(piperidin-1-yl)methyl]phenoxy}propyl)piperidine
Identifiers
3D model ( JSmol)
Abbreviations JNJ-5207852
ChEMBL
ChemSpider
MeSH JNJ-5207852
PubChem CID
UNII
  • 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 checkY
    Key: PTKHFRNHJULJKT-UHFFFAOYSA-N checkY
  • O(c1ccc(cc1)CN2CCCCC2)CCCN3CCCCC3
Properties
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 checkY☒N ?)

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 some 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 was in a Phase II clinical trial for the treatment of narcolepsy in 2007. [3]

References

  1. ^ 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.
  2. ^ 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.
  3. ^ 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.


From Wikipedia, the free encyclopedia
JNJ-5207852
Names
Preferred IUPAC name
1-(3-{4-[(piperidin-1-yl)methyl]phenoxy}propyl)piperidine
Identifiers
3D model ( JSmol)
Abbreviations JNJ-5207852
ChEMBL
ChemSpider
MeSH JNJ-5207852
PubChem CID
UNII
  • 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 checkY
    Key: PTKHFRNHJULJKT-UHFFFAOYSA-N checkY
  • O(c1ccc(cc1)CN2CCCCC2)CCCN3CCCCC3
Properties
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 checkY☒N ?)

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 some 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 was in a Phase II clinical trial for the treatment of narcolepsy in 2007. [3]

References

  1. ^ 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.
  2. ^ 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.
  3. ^ 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.



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