Setiptiline maleate | teciptiline | MO 8282 | CAS#85650-57-3 | 57262-94-9 | serotonin receptor antagonist

MedKoo Cat#: 326697 | Name: Setiptiline maleate

Description:

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

Setiptiline, also known as MO 8282 and teciptiline, is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). It was launched in 1989 for the treatment of depression in Japan by Mochida. Setiptiline acts as a norepinephrine reuptake inhibitor,[3] α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine.

Chemical Structure

Setiptiline maleate

CAS#85650-57-3 (maleate); 57262-94-9 (free base)

Theoretical Analysis

MedKoo Cat#: 326697

Name: Setiptiline maleate

CAS#: 85650-57-3 (maleate); 57262-94-9 (free base)

Chemical Formula: C23H23NO4

Exact Mass:

Molecular Weight: 377.44

Elemental Analysis: C, 73.19; H, 6.14; N, 3.71; O, 16.96

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.

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Related CAS #

No Data

Synonym

MO 8282; MO8282; MO-8282; BRN 1650422; BRN-1650422; BRN1650422; teciptiline; Setiptiline maleate; trade name Tecipul.

IUPAC/Chemical Name

2,3,4,9-Tetrahydro-2-methyl-1H-dibenzo(3,4:6,7)cyclohepta(1,2-c)pyridine maleate

InChi Key

AVPIBVPBCWBXIU-BTJKTKAUSA-N

InChi Code

InChI=1S/C19H19N.C4H4O4/c1-20-11-10-18-16-8-4-2-6-14(16)12-15-7-3-5-9-17(15)19(18)13-20;5-3(6)1-2-4(7)8/h2-9H,10-13H2,1H3;1-2H,(H,5,6)(H,7,8)/b;2-1-

SMILES Code

CN1CCC(C2=CC=CC=C2CC3=CC=CC=C34)=C4C1.O=C(O)/C=C\C(O)=O

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, not in water

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

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 377.44 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

1: Shinozuka T, Terada M, Tanaka E. Solid-phase extraction and analysis of 20 antidepressant drugs in human plasma by LC/MS with SSI method. Forensic Sci Int. 2006 Oct 16;162(1-3):108-12. Epub 2006 Jul 20. PubMed PMID: 16859851. 2: Ishii A, Kurihara R, Kojima T, Sano T, Mizuno Y, Yamakawa Y, Katsumata Y. Sensitive determination of mianserin and setiptiline in body fluids by gas chromatography with surface ionization detection (GC-SID). Leg Med (Tokyo). 2000 Aug;2(2):115-8. PubMed PMID: 12935454. 3: Namera A. [Practical analysis of toxic substances useful of clinical toxicology -2- tricyclic and tetracyclic antidepressants]. Chudoku Kenkyu. 2002 Apr;15(2):187-90. Review. Japanese. PubMed PMID: 12108019. 4: Namera A, Watanabe T, Yashiki M, Iwasaki Y, Kojima T. Simple analysis of tetracyclic antidepressants in blood using headspace-solid-phase microextraction and GC-MS. J Anal Toxicol. 1998 Sep;22(5):396-400. PubMed PMID: 9737336. 5: Shimizu M, Nishida A, Zensho H, Yamawaki S. Chronic antidepressant exposure enhances 5-hydroxytryptamine7 receptor-mediated cyclic adenosine monophosphate accumulation in rat frontocortical astrocytes. J Pharmacol Exp Ther. 1996 Dec;279(3):1551-8. PubMed PMID: 8968382. 6: Nisijima K, Oyafuso K, Shimada T, Hosino H, Ishiguro T. Cerebrospinal fluid monoamine metabolism in a case of neuroleptic malignant syndrome improved by electroconvulsive therapy. Biol Psychiatry. 1996 Mar 1;39(5):383-4. PubMed PMID: 8704073. 7: Tohda M, Urushihara H, Nomura Y. Inhibitory effects of antidepressants on NMDA-induced currents in Xenopus oocytes injected with rat brain RNA. Neurochem Int. 1995 Jan;26(1):53-8. PubMed PMID: 7787763. 8: Kamimura M, Aoba A, Yamaguchi N, Tsuneizumi T, Takagi H, Chishima T, Sakai T, Negishi K, Morokawa Y, Takeshita T, et al. The effect of age on plasma level of setiptiline maleate in depressed patients. Prog Neuropsychopharmacol Biol Psychiatry. 1994 Oct;18(6):1015-26. PubMed PMID: 7824756. 9: Kuniyoshi M, Nakamura J, Miura C, Inanaga K. Effectiveness of concomitant setiptiline maleate (Tecipul) on negative symptoms of schizophrenia. Prog Neuropsychopharmacol Biol Psychiatry. 1994 Mar;18(2):339-46. PubMed PMID: 7516085. 10: Kodama H. [Effect of lithium, carbamazepine, and setiptiline on diacylglycerol in rat brain ex vivo]. Nihon Shinkei Seishin Yakurigaku Zasshi. 1994 Feb;14(1):33-8. Japanese. PubMed PMID: 8048280. 11: Sato T, Sakado K, Sato S. Is there any specific personality disorder or personality disorder cluster that worsens the short-term treatment outcome of major depression? Acta Psychiatr Scand. 1993 Nov;88(5):342-9. PubMed PMID: 7905225. 12: Aoba A. [Depression in late life]. Nihon Ronen Igakkai Zasshi. 1991 Jul;28(4):470-4. Japanese. PubMed PMID: 1942625. 13: Yamada K, Furukawa T. [Behavioral effects of a new antidepressant, setiptiline]. Nihon Yakurigaku Zasshi. 1991 Jan;97(1):31-9. Japanese. PubMed PMID: 2045013. 14: Mizota M, Oikawa Y, Nakayama K, Mizuguchi K, Takarada T, Kojima M, Kanehiro H, Funato H, Kayamoto M, Sato M, et al. [Pharmacological studies of MO-8282, a new antidepressant]. Nihon Yakurigaku Zasshi. 1986 Dec;88(6):457-66. Japanese. PubMed PMID: 2881854. 15: Niho T, Ito C, Shibutani Y, Hashizume H, Yamaguchi K. [Pharmacological properties of MO-8282, a novel antidepressant]. Nihon Yakurigaku Zasshi. 1986 Oct;88(4):309-20. Japanese. PubMed PMID: 3792961. 16: Przegaliński E, Baran L, Siwanowicz J, Rawłów A. The lack of antidepressant properties and a potent central antiserotonin activity of Org 8282. Pol J Pharmacol Pharm. 1986 Jul-Aug;38(4):377-84. PubMed PMID: 3774630.