Setiptiline

Names

[ Name ]:
Setiptiline

[Synonym ]:
ORG 8282
Setiptilina [Spanish]
EINECS 260-653-4
MO 8282
Setiptilinum [Latin]
2,3,4,9-tetrahydro-2-methyl-1H-dibenzo[3,4:6,7]cyclohepta[1,2-c]pyridine
Teciptiline

Biological Activity

[Description]:

Setiptiline(Org-8282) is a serotonin receptor antagonist.IC 50 value:Target: 5-HT receptorSetiptiline 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.

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

Research Areas >> Neurological Disease

[References]

[1]. Yamada K, Furukawa T. [Behavioral effects of a new antidepressant, setiptiline]. Nihon Yakurigaku Zasshi. 1991 Jan;97(1):31-9.

[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.

[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.

[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.

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.15

[ Boiling Point ]:
421.7ºC at 760mmHg

[ Molecular Formula ]:
C₁₉H₁₉N

[ Molecular Weight ]:
261.36100

[ Flash Point ]:
185.5ºC

[ Exact Mass ]:
261.15200

[ PSA ]:
3.24000

[ LogP ]:
3.77500

[ Index of Refraction ]:
1.656

[ Storage condition ]:
2-8℃

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :: HO7578000

CAS REGISTRY NUMBER :: 57262-94-9

LAST UPDATED :: 199612

DATA ITEMS CITED :: 2

MOLECULAR FORMULA :: C19-H19-N

MOLECULAR WEIGHT :: 261.39

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 554 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #4447437

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 423 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: JKXXAF Japanese Kokai Tokyo Koho Patents. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #81-65825