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Inhibitors Product Data Sheet Nitroxazepine • Agonists Cat. No.: HY-101684 CAS No.: 47439-36-1 Molecular Formula: C₁₈H₁₉N₃O₄ • Molecular Weight: 341.36 Screening Libraries Target: Serotonin Transporter Pathway: Neuronal Signaling Storage: Please store the product under the recommended conditions in the Certificate of Analysis. BIOLOGICAL ACTIVITY Description Nitroxazepine is a tricyclic antidepressant (TCA) for the research of depression. Nitroxazepine acts as a serotonin- norepinephrine reuptake inhibitor. IC₅₀ & Target serotonin-norepinephrine reuptake In Vitro The in vitro effect of Nitroxazepine (Sintamil), as a modulator alone and in combination with hydroxyurea (HU), on cytotoxicity is studied in 16 cases of human chronic myeloid leukemia (CML). The cytotoxicity of the drugs as a function of the exposure dose (HU, 100 μM; Nitroxazepine, 10 μg/mL) and the exposure time (1 h) to the agent is investigated. Cytotoxicity is evaluated as the inhibition of incorporation of [3H-methyl]thymidine in the nucleic acids of CML cells. Cytotoxicity of HU is greatly enhanced (P<0.001) by 1 h exposure of the CML cells to Nitroxazepine. The present data indicate that Nitroxazepine potentiates the cytotoxic activity of HU in CML cells[1]. Nitroxazepine is indicated for the treatment of nocturnal enuresis. Nitroxazepine has similar effects to imipramine, but with certain advantages, such as lower anticholinergic side effects. MCE has not independently confirmed the accuracy of these methods. They are for reference only. REFERENCES [1]. Pradhan SG, et al. Augmentation of hydroxyurea cytotoxicity by sintamil in human chronic myeloid leukemia cells. Tumori. 1986 Oct 31;72(5):507-10. McePdfHeight Caution: Product has not been fully validated for medical applications. For research use only. Tel: 609-228-6898 Fax: 609-228-5909 E-mail: [email protected] Address: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA Page 1 of 1 www.MedChemExpress.com.

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WO 2012/148799 Al 1 November 2012 (01.11.2012) P O P C T
(12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (10) International Publication Number (43) International Publication Date WO 2012/148799 Al 1 November 2012 (01.11.2012) P O P C T (51) International Patent Classification: (81) Designated States (unless otherwise indicated, for every A61K 9/107 (2006.01) A61K 9/00 (2006.01) kind of national protection available): AE, AG, AL, AM, A 61 47/10 (2006.0V) AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, (21) International Application Number: DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, PCT/US2012/034361 HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, (22) International Filing Date: KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, 20 April 2012 (20.04.2012) MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SC, SD, (25) Filing Language: English SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, (26) Publication Language: English TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (30) Priority Data: (84) Designated States (unless otherwise indicated, for every 61/480,259 28 April 201 1 (28.04.201 1) US kind of regional protection available): ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, (71) Applicant (for all designated States except US): BOARD UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, MD, RU, OF REGENTS, THE UNIVERSITY OF TEXAS SYS¬ TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, TEM [US/US]; 201 West 7th St., Austin, TX 78701 (US).
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