Leteprinim

Leteprinim
Clinical data
ATC code
  • none
Identifiers
  • 4-{[3-(6-oxo-3,6-dihydro-9H-purin-9-yl)propanoyl]amino}benzoic acid
CAS Number
PubChem CID
ChemSpider
UNII
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC15H13N5O4
Molar mass327.300 g·mol−1
3D model (JSmol)
  • C1=CC(=CC=C1C(=O)O)NC(=O)CCN2C=NC3=C2NC=NC3=O
  • InChI=1S/C15H13N5O4/c21-11(19-10-3-1-9(2-4-10)15(23)24)5-6-20-8-18-12-13(20)16-7-17-14(12)22/h1-4,7-8H,5-6H2,(H,19,21)(H,23,24)(H,16,17,22)
  • Key:JMPOIZCOJJMTHI-UHFFFAOYSA-N
  (verify)

Leteprinim (Neotrofin, AIT-082) is a hypoxanthine derivative drug with neuroprotective and nootropic effects.[1][2][3] It stimulates release of nerve growth factors and enhances survival of neurons in the brain,[4][5][6][7][8] and is under development as a potential treatment for neurodegenerative disorders such as Alzheimer's disease, Parkinson's disease and stroke.[9][10]

References

  1. ^ Di Iorio P, Virgilio A, Giuliani P, Ballerini P, Vianale G, Middlemiss PJ, et al. (June 2001). "AIT-082 is neuroprotective against kainate-induced neuronal injury in rats". Experimental Neurology. 169 (2): 392–9. doi:10.1006/exnr.2001.7654. PMID 11358452. S2CID 43094767.
  2. ^ Lahiri DK, Ge YW, Farlow MR (April 2000). "Effect of a memory-enhancing drug, AIT-082, on the level of synaptophysin". Annals of the New York Academy of Sciences. 903 (1): 387–93. Bibcode:2000NYASA.903..387L. doi:10.1111/j.1749-6632.2000.tb06390.x. PMID 10818529. S2CID 33710679.
  3. ^ Yan R, Nguyen Q, Gonzaga J, Johnson M, Ritzmann RF, Taylor EM (April 2003). "Reversal of cycloheximide-induced memory disruption by AIT-082 (Neotrofin) is modulated by, but not dependent on, adrenal hormones". Psychopharmacology. 166 (4): 400–7. doi:10.1007/s00213-002-1350-5. PMID 12605287. S2CID 25028981.
  4. ^ Rathbone MP, Middlemiss PJ, Crocker CE, Glasky MS, Juurlink BH, Ramirez JJ, et al. (August 1999). "AIT-082 as a potential neuroprotective and regenerative agent in stroke and central nervous system injury". Expert Opinion on Investigational Drugs. 8 (8): 1255–62. doi:10.1517/13543784.8.8.1255. PMID 15992149.
  5. ^ Ramirez JJ, Parakh T, George MN, Freeman L, Thomas AA, White CC, et al. (2002). "The effects of Neotrofin on septodentate sprouting after unilateral entorhinal cortex lesions in rats". Restorative Neurology and Neuroscience. 20 (1–2): 51–9. PMID 12237496.
  6. ^ Holmes M, Maysinger D, Foerster A, Pertens E, Barlas C, Diamond J (November 2003). "Neotrofin, a novel purine that induces NGF-dependent nociceptive nerve sprouting but not hyperalgesia in adult rat skin". Molecular and Cellular Neurosciences. 24 (3): 568–80. doi:10.1016/s1044-7431(03)00217-3. PMID 14664808. S2CID 13359687.
  7. ^ Jiang S, Khan MI, Middlemiss PJ, Lu Y, Werstiuk ES, Crocker CE, et al. (2004). "AIT-082 and methylprednisolone singly, but not in combination, enhance functional and histological improvement after acute spinal cord injury in rats". International Journal of Immunopathology and Pharmacology. 17 (3): 353–66. doi:10.1177/039463200401700315. PMID 15461869. S2CID 26045848.
  8. ^ Calcutt NA, Freshwater JD, Hauptmann N, Taylor EM, Mizisin AP (March 2006). "Protection of sensory function in diabetic rats by Neotrofin". European Journal of Pharmacology. 534 (1–3): 187–93. doi:10.1016/j.ejphar.2006.01.047. PMID 16507305.
  9. ^ Potkin SG, Alva G, Keator D, Carreon D, Fleming K, Fallon JH (September 2002). "Brain metabolic effects of Neotrofin in patients with Alzheimer's disease". Brain Research. 951 (1): 87–95. doi:10.1016/s0006-8993(02)03140-2. PMID 12231461. S2CID 23021393.
  10. ^ Johnston TH, Brotchie JM (July 2004). "Drugs in development for Parkinson's disease". Current Opinion in Investigational Drugs. 5 (7): 720–6. PMID 15298067.