2,3,4,9-tetrahydro-2-methyl-1H-dibenzo[3,4:6,7]cyclohepta[1,2-c]pyridyl maleate Chemical Properties

storage temp. 

Store at -20°C

solubility 

Soluble in DMSO

form 

Powder

color 

White to gray

2,3,4,9-tetrahydro-2-methyl-1H-dibenzo[3,4:6,7]cyclohepta[1,2-c]pyridyl maleate Usage And Synthesis

Uses

Setiptiline maleate (MO-8282 maleate) is a serotonin receptor antagonist. Setiptiline maleate is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline maleate acts as a norepinephrine reuptake inhibitor, 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[1][2][3][4].

Definition

ChEBI: Setiptiline maleate is a maleate salt obtained by reaction of setiptiline with one equivalent of maleic acid. It has a role as an alpha-adrenergic antagonist and a serotonergic antagonist. It is a maleate salt and a tetracyclic antidepressant. It contains a setiptiline(1+).

Biological Activity

setiptiline is a tetracyclic antidepressant (teca) which acts as a noradrenergic and specific serotonergic antidepressant (nassa). setiptiline acts as a norepinephrine reuptake inhibitor, 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. from wikipedia.

IC 50

5-HT_2A Receptor; 5-HT_2C Receptor; 5-HT₃ Receptor

References

[1] Yamada K, Furukawa T. [Behavioral effects of a new antidepressant, setiptiline]. Nihon Yakurigaku Zasshi. 1991 Jan;97(1):31-9. DOI:10.1254/fpj.97.1_31
[2] Kamimura M, Aoba A, Yamaguchi N 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. DOI:10.1016/0278-5846(94)90127-9
[3] 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. DOI:10.1016/0278-5846(94)90065-5
[4] 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. DOI:10.1254/fpj.88.309

2,3,4,9-tetrahydro-2-methyl-1H-dibenzo[3,4:6,7]cyclohepta[1,2-c]pyridyl maleate(85650-57-3)Related Product Information

• MALEIC ACID MONOSODIUM SALT
• Chlorphenamine maleate
• PHENRAMINE MALEATE
• Setiptiline