57262-94-9
Chemical Structure
Setiptiline
Synonym(s): Org-8282
- CAS No.: 57262-94-9
- Formula:C19H19N
- Molecular Weight:261.37
IUPAC Name: 2-methyl-2,3,4,9-tetrahydro-1H-dibenzo[3,4:6,7]cyclohepta[1,2-c]pyridine
InChIKey: GVPIXRLYKVFFMK-UHFFFAOYSA-N
SMILES: CN1CC2=C(CC1)C3=CC=CC=C3CC4=C2C=CC=C4
Biological Activity: Setiptiline (Org-8282) is a tetracyclic antidepressant and orally active 5-HT1ₑR/5-HT1FR agonist, with an EC50 of 171.0 nM, a Ki of 29.3 nM for human 5-HT1ₑR, and an EC50 of 64.6 nM for human 5-HT1FR. Setiptiline induces the dissociation of G proteins from the heterotrimeric Gαi1/Gβ1/Gγ2 complex and promotes the recruitment of β-arrestin2. Setiptiline is applicable to research related to migraine and schizophrenia[1][2].
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Setiptiline | 98.03% | Setiptiline (Org-8282) is a tetracyclic antidepressant and orally active 5-HT1ₑR/5-HT1FR agonist, with an EC50 of 171.0 nM, a Ki of 29.3 nM for human 5-HT1ₑR, and an EC50 of 64.6 nM for human 5-HT1FR. Setiptiline induces the dissociation of G proteins from the heterotrimeric Gαi1/Gβ1/Gγ2 complex and promotes the recruitment of β-arrestin2. Setiptiline is applicable to research related to migraine and schizophrenia. | ||||||||||||||||||||
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Setiptiline (Standard) | ≥98% | Setiptiline (Standard) is the analytical standard of Setiptiline. This product is intended for research and analytical applications. Setiptiline (Org-8282) is a serotonin receptor antagonist. 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. | ||||||||||||||||||||
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Setiptiline-d3 | Setiptiline-d3 is the deuterium labeled Setiptiline. Setiptiline (Org-8282) is a serotonin receptor antagonist. 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. | |||||||||||||||||||||
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Similarity Score 0.82
HY-32329ARSetiptiline maleate (Standard) -
Similarity Score 0.60
HY-A0149Phenindamine -
Similarity Score 0.59
HY-W009938Anthrone -
Similarity Score 0.59
HY-105962Erizepine -
Similarity Score 0.58
HY-B1622Cyproheptadine -
Similarity Score 0.56
HY-78509Dibenzosuberone -
Similarity Score 0.56
HY-B0366ACyproheptadine hydrochloride -
Similarity Score 0.56
HY-W683866Piroheptine -
Similarity Score 0.55
HY-B1165Cyproheptadine hydrochloride sesquihydrate -
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References
- [1]. Zilberg G, et al. Structural Insights into the Unexpected Agonism of Tetracyclic Antidepressants at Serotonin Receptors 5-HT1eR and 5-HT1FR. bioRxiv [Preprint]. 2023 Oct 7:2023.10.05.561100.
- [2]. Kuniyoshi M, et al. Effectiveness of concomitant setiptiline maleate (Tecipul) on negative symptoms of schizophrenia. Prog Neuropsychopharmacol Biol Psychiatry. 1994;18(2):339-346. [Content Brief]
