Diclofensine HCl | CAS#34041-84-4 | antidepressant

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

MedKoo CAT#: 563093

CAS#: 34041-84-4 (HCl)

Description: Diclofensine HCl is an antidepressant with equipotent inhibitive effects on the neuronal uptake of norepinephrine (NE), serotonin, and dopamine.

Chemical Structure

Diclofensine HCl

CAS# 34041-84-4 (HCl)

Instruction

Theoretical Analysis

MedKoo Cat#: 563093
Name: Diclofensine HCl
CAS#: 34041-84-4 (HCl)
Chemical Formula: C17H18Cl3NO
Exact Mass: 357.05
Molecular Weight: 358.680
Elemental Analysis: C, 56.93; H, 5.06; Cl, 29.65; N, 3.91; O, 4.46

Price and Availability

Size	Price	Availability
10mg	USD 315	2 weeks
50mg	USD 785	2 weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Related CAS #: 34041-84-4 (HCl) 67165-56-4 (free base)

Synonym: Diclofensine HCl; Moxifensine hydrochloride; Ro-84650; Moxifensine HCl; Ro 84650; Ro84650; Diclofensine Hydrochloride;

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:

Instruction:

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Biological target:
In vitro activity:
In vivo activity:

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.

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

Formulation protocol:
In vitro protocol:
In vivo protocol:

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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.

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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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Diclofensine HCl featured