Datasheet Inhibitors / Agonists / Screening Libraries a DRUG SCREENING EXPERT

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Datasheet Inhibitors / Agonists / Screening Libraries A DRUG SCREENING EXPERT Product Name : Diclofensine hydrochloride Catalog Number : T7745 CAS Number : 34041-84-4 Molecular Formula : C17H18Cl3NO Molecular Weight : 358.69 Description: Diclofensine hydrochloride is a Novel Antidepressant, on Peripheral Adrenergic Function Storage: 2 years -80°C in solvent; 3 years -20°C powder; H2O 52 mg/mL (144.97 mM) Solubility ( < 1 mg/ml refers to the product slightly soluble or insoluble ) In vitro Activity The action of diclofensine on peripheral neuronal adrenergic function was studied through tests of the blood pressure response to NE, tyramine, and phenylephrine (PE). The blood pressure response to NE was enhanced and that to tyramine was decreased by diclofensine, as a result of its inhibitive action on peripheral neuronal amine uptake. PE sensitivity was also enhanced by diclofensine as well as after a single dose of desmethylimipramine (DMI). In contrast to the common opinion that PE does not interact with the neuronal uptake mechanism, the increase in PE-induced blood pressure response after diclofensine and DMI suggests that PE, a nonbiogenic amine, does indeed enter into the peripheral adrenergic neuron[1]. Reference 1. S Gasić, Korn A , Eichler H G . Effect of diclofensine, a novel antidepressant, on peripheral adrenergic function[J]. Clinical Pharmacology & Therapeutics, 1986, 39. 2. Renzo G D , Amoroso S , Taglialatela M , et al. Pure uptake blockers of dopamine can reduce prolactin secretion: Studies with diclofensine[J]. Life Sciences, 1988, 42(21):2161-2169. FOR RESEARCH PURPOSES ONLY. NOT FOR DIAGNOSTIC OR THERAPEUTIC USE. Information for product storage and handling is indicated on the product datasheet. Targetmol products are stable for long term under the recommended storage conditions. Our products may be shipped under different conditions as many of them are stable in the short-term at higher or even room temperatures. We ensure that the product is shipped under conditions that will maintain the quality of the reagents. Upon receipt of the product, please follow the storage recommendations on the product data sheet. [email protected] | Tel: +1-781-999-4286 | www.targetmol.com.

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(19) United States (12) Patent Application Publication (10) Pub
US 20130289061A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2013/0289061 A1 Bhide et al. (43) Pub. Date: Oct. 31, 2013 (54) METHODS AND COMPOSITIONS TO Publication Classi?cation PREVENT ADDICTION (51) Int. Cl. (71) Applicant: The General Hospital Corporation, A61K 31/485 (2006-01) Boston’ MA (Us) A61K 31/4458 (2006.01) (52) U.S. Cl. (72) Inventors: Pradeep G. Bhide; Peabody, MA (US); CPC """"" " A61K31/485 (201301); ‘4161223011? Jmm‘“ Zhu’ Ansm’ MA. (Us); USPC ......... .. 514/282; 514/317; 514/654; 514/618; Thomas J. Spencer; Carhsle; MA (US); 514/279 Joseph Biederman; Brookline; MA (Us) (57) ABSTRACT Disclosed herein is a method of reducing or preventing the development of aversion to a CNS stimulant in a subject (21) App1_ NO_; 13/924,815 comprising; administering a therapeutic amount of the neu rological stimulant and administering an antagonist of the kappa opioid receptor; to thereby reduce or prevent the devel - . opment of aversion to the CNS stimulant in the subject. Also (22) Flled' Jun‘ 24’ 2013 disclosed is a method of reducing or preventing the develop ment of addiction to a CNS stimulant in a subj ect; comprising; _ _ administering the CNS stimulant and administering a mu Related U‘s‘ Apphcatlon Data opioid receptor antagonist to thereby reduce or prevent the (63) Continuation of application NO 13/389,959, ?led on development of addiction to the CNS stimulant in the subject. Apt 27’ 2012’ ?led as application NO_ PCT/US2010/ Also disclosed are pharmaceutical compositions comprising 045486 on Aug' 13 2010' a central nervous system stimulant and an opioid receptor ’ antagonist.
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Product Information Diclofensine (hydrochloride) Item No. 15355 CAS Registry No.: 34041-84-4 Formal Name: 4- (3, 4- dichlorophenyl) - 1, 2, 3, 4- tetrahydro- 7- methoxy- 2- methyl- N isoquinoline, monohydrochloride • HCl Synonym: Ro 8-4650 Cl MF: C17H17Cl2NO • HCl FW: 358.7 Purity: ≥98% Stability: ≥2 years at -20°C O Cl Supplied as: A crystalline solid Laboratory Procedures For long term storage, we suggest that diclofensine (hydrochloride) be stored as supplied at -20°C. It should be stable for at least two years. Diclofensine (hydrochloride) is supplied as a crystalline solid. A stock solution may be made by dissolving the diclofensine (hydrochloride) in the solvent of choice. Diclofensine (hydrochloride) is soluble in methanol at a concentration of approximately 10 mg/ml. Diclofensine (hydrochloride) is sparingly soluble in aqueous solutions. To enhance aqueous solubility, dilute the organic solvent solution into aqueous buffers or isotonic saline. If performing biological experiments, ensure the residual amount of organic solvent is insignificant, since organic solvents may have physiological effects at low concentrations. We do not recommend storing the aqueous solution for more than one day. Diclofensine is a potent inhibitor of monoamine reuptake, blocking the uptake of dopamine, noradrenaline, and 1 serotonin by rat brain synaptosomes with IC50 values of 0.74, 2.3, and 3.7 nM, respectively. While it has applications as an antidepressant, diclofensine increases locomotor activity, decreases food intake, and has abuse potential.2-5 This product is intended for research and forensic applications. References 1. Hyttel, J. and Larsen, J.J. Neurochemical profile of Lu 19-005, a potent inhibitor of uptake of dopamine, noradrenaline, and serotonin.
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