Setiptiline

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Setiptiline (brand name Tecipul), also known as teciptiline, is a tetracyclic antidepressant (TeCA) that acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). It was launched in 1989 for the treatment of depression in Japan by Mochida.[1][2]

Pharmacology

Pharmacodynamics

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Setiptiline[3]
Site Ki (nM) Species Ref
SERTTooltip Serotonin transporter >10,000 (IC50) Rat [4]
NETTooltip Norepinephrine transporter 220 (IC50) Rat [4]
DATTooltip Dopamine transporter >10,000 (IC50) Rat [4]
5-HT1A ND ND ND
5-HT2A ND ND ND
5-HT2C ND ND ND
α1 ND ND ND
α2 24.3 (IC50) Rat [5]
H1 ND ND ND
mAChTooltip Muscarinic acetylcholine receptor ND ND ND
Values are Ki (nM), unless otherwise noted. The smaller the value, the more strongly the drug binds to the site.

Setiptiline acts as a norepinephrine reuptake inhibitor,[4] α2-adrenergic receptor antagonist,[5] and serotonin receptor antagonist,[6] likely at the 5-HT2 subtypes,Script error: No such module "Unsubst". as well as an H1 receptor inverse agonist/antihistamine.[4]Template:Additional citation needed

Chemistry

Setiptiline has a tetracyclic structure and is a close analogue of mianserin and mirtazapine, with setiptiline being delta(13b,4a),4a-carba-mianserin, and mirtazapine being 6-azamianserin.

See also

References

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