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MedKoo Cat#: 563093 | Name: Diclofensine HCl
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Diclofensine (Ro 8-4650) is a antidepressant. It was found that the (S)-isomer was responsible for activity. Diclofensine is a stimulant drug which acts as a triple monoamine reuptake inhibitor, primarily inhibiting the reuptake of dopamine and norepinephrine, with affinities (Ki) of 16.8 nM, 15.7 nM, and 51 nM for DAT, NET, and SERT (dopamine, norepinephrine and serotonin transporters), respectively.

Chemical Structure

Diclofensine HCl
CAS#34041-84-4 (HCl)

Theoretical Analysis

MedKoo Cat#: 563093

Name: Diclofensine HCl

CAS#: 34041-84-4 (HCl)

Chemical Formula: C17H18Cl3NO

Exact Mass: 357.0454

Molecular Weight: 358.68

Elemental Analysis: C, 56.93; H, 5.06; Cl, 29.65; N, 3.91; O, 4.46

Price and Availability

Size Price Availability Quantity
5mg USD 250.00 2 Weeks
10mg USD 450.00 2 Weeks
50mg USD 950.00 2 Weeks
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Related CAS #
34041-84-4 (HCl) 67165-56-4 (free base)
Synonym
Diclofensine HCl; Moxifensine hydrochloride; Diclofensine; Ro 8-4650; Ro-8-4650; Ro8-4650; Ro 84650; Ro-84650; Ro84650;
IUPAC/Chemical Name
4-(3,4-Dichlorophenyl)-7-methoxy-2-methyl-3,4-dihydro-1H-isoquinoline hydrochloride
InChi Key
PEHOXCSPLOXNOK-UHFFFAOYSA-N
InChi Code
InChI=1S/C17H17Cl2NO.ClH/c1-20-9-12-7-13(21-2)4-5-14(12)15(10-20)11-3-6-16(18)17(19)8-11;/h3-8,15H,9-10H2,1-2H3;1H
SMILES Code
CN1CC2=C(C=CC(OC)=C2)C(C3=CC=C(Cl)C(Cl)=C3)C1.[H]Cl
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 358.68 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Capponi R, Hormazabal L, Schmid-Burgk W. Diclofensine and imipramine. A double-blind comparative trial in depressive out-patients. Neuropsychobiology. 1985;14(4):173-80. doi: 10.1159/000118224. PMID: 3915058. 2: Gasić S, Korn A, Eichler HG. Effect of diclofensine, a novel antidepressant, on peripheral adrenergic function. Clin Pharmacol Ther. 1986 May;39(5):582-5. doi: 10.1038/clpt.1986.100. PMID: 3698467. 3: Luethi D, Hoener MC, Liechti ME. Effects of the new psychoactive substances diclofensine, diphenidine, and methoxphenidine on monoaminergic systems. Eur J Pharmacol. 2018 Jan 15;819:242-247. doi: 10.1016/j.ejphar.2017.12.012. Epub 2017 Dec 7. PMID: 29225192. 4: Cherpillod C, Omer LM. A controlled trial with diclofensine, a new psychoactive drug, in the treatment of depression. J Int Med Res. 1981;9(5):324-9. doi: 10.1177/030006058100900505. PMID: 7028532. 5: Jansen W, Brückner GW, Henauer S, Omer LM. Klinischer Doppelblindvergleich von Diclofensin und Plazebo bei geriatrischen Patienten mit depressiven Verstimmungszuständen [Clinical double blind comparison of diclofensine and placebo in geriatric patients with depressive syndromes]. Pharmacopsychiatria. 1982 Nov;15(6):205-9. German. doi: 10.1055/s-2007-1019539. PMID: 6760217. 6: Keller HH, Schaffner R, Carruba MO, Burkard WP, Pieri M, Bonetti EP, Scherschlicht R, Da Prada M, Haefely WE. Diclofensine (Ro 8-4650)--a potent inhibitor of monoamine uptake: biochemical and behavioural effects in comparison with nomifensine. Adv Biochem Psychopharmacol. 1982;31:249-63. PMID: 6979165. 7: Di Renzo G, Amoroso S, Taglialatela M, Canzoniero LM, Maida P, Lombardi G, Annunziato L. Pure uptake blockers of dopamine can reduce prolactin secretion: studies with diclofensine. Life Sci. 1988;42(21):2161-9. doi: 10.1016/0024-3205(88)90131-2. PMID: 2968488. 8: Culig J, Ehsanullah RS, Hallett C, Iliopoulou A, Matheson I, Turner P. A clinical pharmacological comparison of diclofensine (Ro 8-4650) with nomifensine and amitriptyline in normal human volunteers. Br J Clin Pharmacol. 1983 May;15(5):537-43. doi: 10.1111/j.1365-2125.1983.tb02087.x. PMID: 6860528; PMCID: PMC1427714. 9: Lamb RJ, Griffiths RR. Self-administration in baboons and the discriminative stimulus effects in rats of bupropion, nomifensine, diclofensine and imipramine. Psychopharmacology (Berl). 1990;102(2):183-90. doi: 10.1007/BF02245920. PMID: 2125734. 10: Omer OL, Díaz-Olivera M, Ismail S. Therapeutic efficacy and tolerance of diclofensine in psychoreactive depression--a double-blind comparison with placebo. Methods Find Exp Clin Pharmacol. 1984 Mar;6(3):147-51. PMID: 6379345. 11: Omer LM. Pilot trials with diclofensine, a new psychoactive drug in depressed patients. Int J Clin Pharmacol Ther Toxicol. 1982 Jul;20(7):320-6. PMID: 7107085. 12: Jackson SH, Turner P, Ehsanullah RS. A comparison of diclofensine and desmethylimipramine using tyramine pressor tests in normal subjects. Br J Clin Pharmacol. 1983 Oct;16(4):427-9. doi: 10.1111/j.1365-2125.1983.tb02189.x. PMID: 6626436; PMCID: PMC1428037. 13: Funke HJ, Holtmann W, Ismail S, Jansen W, Leonhardt KF, Muth H, Omer LM, O'Connolly M, Ramm H. Double-blind comparison of diclofensine with nomifensine in outpatients with dysphoric mood. Pharmacopsychiatry. 1986 May;19(3):120-3. doi: 10.1055/s-2007-1017168. PMID: 3725890. 14: Strojny N, de Silva JA. Determination of diclofensine, an antidepressant agent, and its major metabolites in human plasma by high-performance liquid chromatography with fluorometric detection. J Chromatogr. 1985 Jun 14;341(2):313-31. doi: 10.1016/s0378-4347(00)84045-1. PMID: 4030982. 15: Manna SK, Panda G. Synthesis of enantiomerically enriched indolines and tetrahydroisoquinolines from (S)-amino acid-derived chiral carbocations: an easy access to (3S,4R)-demethoxy-3-isopropyl diclofensine. Org Biomol Chem. 2014 Nov 7;12(41):8318-24. doi: 10.1039/c4ob00922c. Epub 2014 Sep 11. PMID: 25208820. 16: Hojabri H, Dadgar D, Glennon JD. Gas-liquid chromatographic analysis with electron-capture detection of diclofensine in human plasma following derivatization. J Chromatogr. 1984 Nov 9;311(1):189-93. doi: 10.1016/s0378-4347(00)84708-8. PMID: 6520163. 17: Meyer MR, Wagmann L, Schneider-Daum N, Loretz B, de Souza Carvalho C, Lehr CM, Maurer HH. P-glycoprotein interactions of novel psychoactive substances - stimulation of ATP consumption and transport across Caco-2 monolayers. Biochem Pharmacol. 2015 Apr 1;94(3):220-6. doi: 10.1016/j.bcp.2015.01.008. Epub 2015 Jan 28. PMID: 25637762. 18: Tian D, Li C, Gu G, Peng H, Zhang X, Tang W. Stereospecific Nucleophilic Substitution with Arylboronic Acids as Nucleophiles in the Presence of a CONH Group. Angew Chem Int Ed Engl. 2018 Jun 11;57(24):7176-7180. doi: 10.1002/anie.201712829. Epub 2018 May 9. PMID: 29687594. 19: Nakachi N, Kiuchi Y, Inagaki M, Inazu M, Yamazaki Y, Oguchi K. Effects of various dopamine uptake inhibitors on striatal extracellular dopamine levels and behaviours in rats. Eur J Pharmacol. 1995 Aug 4;281(2):195-203. doi: 10.1016/0014-2999(95)00246-h. PMID: 7589207. 20: Hyttel J, Larsen JJ. Neurochemical profile of Lu 19-005, a potent inhibitor of uptake of dopamine, noradrenaline, and serotonin. J Neurochem. 1985 May;44(5):1615-22. doi: 10.1111/j.1471-4159.1985.tb08803.x. PMID: 2580950.

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