Leteprinim

Leteprinim
Clinical data
ATC code	none;
Identifiers
	IUPAC name 4-{[3-(6-oxo-3,6-dihydro-9H-purin-9-yl)propanoyl]amino}benzoic acid;
CAS Number	138117-50-7 ;
PubChem CID	132123;
ChemSpider	116710;
UNII	NBY3IU407M;
CompTox Dashboard (EPA)	DTXSID00160496 ;
Chemical and physical data
Formula	C15H13N5O4
Molar mass	327.295 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C1=CC(=CC=C1C(=O)O)NC(=O)CCN2C=NC3=C2NC=NC3=O;
	InChI 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

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.
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.
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.
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.
Ramirez JJ, Parakh T, George MN, Freeman L, Thomas AA, White CC, Becton A (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.
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.
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.
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.
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.
Johnston TH, Brotchie JM (July 2004). "Drugs in development for Parkinson's disease". Current Opinion in Investigational Drugs. 5 (7): 720–6. PMID 15298067.

External links

Leteprinim potassium - AdisInsight

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[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, Becton A (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.

[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.