PHA-543,613

Today, PHA-543,613 is a topic that arouses the interest of people of all ages and backgrounds. From its impact on society to its implications on daily life, PHA-543,613 has generated discussions and debates around the world. Its relevance is undeniable, and its influence extends to various areas of knowledge. In this article, we will explore different perspectives and approaches on PHA-543,613, analyzing its importance and impact on life today. Through detailed analysis, we will seek to shed light on this complex and multidimensional topic, providing the reader with a broad and complete view of PHA-543,613 and its impact on our society.
PHA-543,613
Identifiers
  • N-oct-3-yl]furopyridine-5-carboxamide
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.189.975 Edit this at Wikidata
Chemical and physical data
FormulaC15H17N3O2
Molar mass271.320 g·mol−1
3D model (JSmol)
  • C1CN2CCC1(C2)NC(=O)C3=NC=C4C(=C3)C=CO4
  • InChI=1S/C15H17N3O2/c19-15(12-7-11-3-6-20-14(11)8-16-12)17-13-9-18-4-1-10(13)2-5-18/h3,6-8,10,13H,1-2,4-5,9H2,(H,17,19)/t13-/m0/s1
  • Key:IPKZCLGGYKRDES-ZDUSSCGKSA-N
  (verify)

PHA-543,613 is a drug that acts as a potent and selective agonist for the α7 subtype of neural nicotinic acetylcholine receptors, with a high level of brain penetration and good oral bioavailability. It is under development as a possible treatment for cognitive deficits in schizophrenia.[1] It reduces excitotoxicity[2] and protects striatal dopaminergic neurons in rat models.[3] It also potentiates cognitive enhancement from memantine,[4][5] decreases dynorphin release[6] and inhibits GSK-B3.[7]

See also

References

  1. ^ Wishka DG, Walker DP, Yates KM, Reitz SC, Jia S, Myers JK, et al. (July 2006). "Discovery of N-oct-3-yl]furopyridine-5-carboxamide, an agonist of the alpha7 nicotinic acetylcholine receptor, for the potential treatment of cognitive deficits in schizophrenia: synthesis and structure--activity relationship". Journal of Medicinal Chemistry. 49 (14): 4425–36. doi:10.1021/jm0602413. PMID 16821801.
  2. ^ Foucault-Fruchard L, Doméné A, Page G, Windsor M, Emond P, Rodrigues N, Dollé F, Damont A, Buron F, Routier S, Chalon S, Antier D (July 2017). "Neuroprotective effect of the alpha 7 nicotinic receptor agonist PHA 543613 in an in vivo excitotoxic adult rat model". Neuroscience. 356: 52–63. doi:10.1016/j.neuroscience.2017.05.019. PMID 28527955. S2CID 4827887.
  3. ^ Sérrière S, Doméné A, Vercouillie J, Mothes C, Bodard S, Rodrigues N, Guilloteau D, Routier S, Page G, Chalon S (2015). "Assessment of the Protection of Dopaminergic Neurons by an α7 Nicotinic Receptor Agonist, PHA 543613 Using [(18)F]LBT-999 in a Parkinson's Disease Rat Model". Frontiers in Medicine. 2: 61. doi:10.3389/fmed.2015.00061. PMC 4556971. PMID 26389120.
  4. ^ Bruszt N, Bali ZK, Tadepalli SA, Nagy LV, Hernádi I (August 2021). "Potentiation of cognitive enhancer effects of Alzheimer's disease medication memantine by alpha7 nicotinic acetylcholine receptor agonist PHA-543613 in the Morris water maze task". Psychopharmacology. 238 (11): 3273–3281. doi:10.1007/s00213-021-05942-4. PMC 8605977. PMID 34387707.
  5. ^ Bali ZK, Bruszt N, Tadepalli SA, Csurgyók R, Nagy LV, Tompa M, Hernádi I (2019). "Cognitive Enhancer Effects of Low Memantine Doses Are Facilitated by an Alpha7 Nicotinic Acetylcholine Receptor Agonist in Scopolamine-Induced Amnesia in Rats". Frontiers in Pharmacology. 10: 73. doi:10.3389/fphar.2019.00073. PMC 6371842. PMID 30804787.
  6. ^ Ji L, Chen Y, Wei H, Feng H, Chang R, Yu D, Wang X, Gong X, Zhang M (July 2019). "Activation of alpha7 acetylcholine receptors reduces neuropathic pain by decreasing dynorphin A release from microglia". Brain Research. 1715: 57–65. doi:10.1016/j.brainres.2019.03.016. PMID 30898676. S2CID 81981843.
  7. ^ Krafft PR, Altay O, Rolland WB, Duris K, Lekic T, Tang J, Zhang JH (March 2012). "α7 nicotinic acetylcholine receptor agonism confers neuroprotection through GSK-3β inhibition in a mouse model of intracerebral hemorrhage". Stroke. 43 (3): 844–50. doi:10.1161/STROKEAHA.111.639989. PMC 3293395. PMID 22207510.
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