Setiptiline

Setiptiline
Clinical data
Trade names	Tecipul
Other names	Teciptiline; delta(13b,4a),4a-Carba-mianserin; MO-8282; ORG-8282
AHFS/Drugs.com	International Drug Names
Routes of; administration	Oral
ATC code	none;
Legal status
Legal status	In general: ℞ (Prescription only);
Identifiers
	show IUPAC name
CAS Number	57262-94-9 ;
PubChem CID	5205;
DrugBank	DB09304 ;
ChemSpider	5016 ;
UNII	7L38105Z6E;
KEGG	D08511 ;
ChEBI	CHEBI:135076;
CompTox Dashboard (EPA)	DTXSID50205886 ;
ECHA InfoCard	100.055.123
Chemical and physical data
Formula	C19H19N
Molar mass	261.368 g·mol−1
3D model (JSmol)	Interactive image;
	show SMILES
	show InChI
	(what is this?)

Setiptiline (brand name Tecipul), also known as 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.^[1]^[2]

Pharmacology[]

Pharmacodynamics[]

Setiptiline^[3]
Site	K_i (nM)	Species	Ref
SERT	>10,000 (IC₅₀)	Rat	^[4]
NET	220 (IC₅₀)	Rat	^[4]
DAT	>10,000 (IC₅₀)	Rat	^[4]
5-HT_1A	ND	ND	ND
5-HT_2A	ND	ND	ND
5-HT_2C	ND	ND	ND
α₁	ND	ND	ND
α₂	24.3 (IC₅₀)	Rat	^[5]
H₁	ND	ND	ND
mACh	ND	ND	ND
Values are K_i (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,^{[citation needed]} as well as an H₁ receptor inverse agonist/antihistamine.^[4]^{[additional citation(s) 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.

References[]

^ Buschmann, H.; Torrens, A.; Vela, J. M. (2007). Antidepressants, Antipsychotics, Anxiolytics: From Chemistry and Pharmacology to Clinical Application. 1. Wiley VCH. p. 248. ISBN 978-3-527-31058-6.
^ Swiss Pharmaceutical Society, ed. (2000). Index Nominum 2000: International Drug Directory. Medpharm Scientific Publishers. p. 942. ISBN 3-88763-075-0.
^ Roth, BL; Driscol, J. "PDSP K_i Database". Psychoactive Drug Screening Program (PDSP). University of North Carolina at Chapel Hill and the United States National Institute of Mental Health. Retrieved 14 August 2017.
^ Jump up to: ^a ^b ^c ^d ^e Niho T, Ito C, Shibutani Y, Hashizume H, Yamaguchi K (1986). "[Pharmacological properties of MO-8282, a novel antidepressant]". Nippon Yakurigaku Zasshi (in Japanese). 88 (4): 309–20. doi:10.1254/fpj.88.309. PMID 3792961.
^ Jump up to: ^a ^b Mizota M, Oikawa Y, Nakayama K, Mizuguchi K, Takarada T, Kojima M, Kanehiro H, Funato H, Kayamoto M, Sato M (1986). "[Pharmacological studies of MO-8282, a new antidepressant]". Nippon Yakurigaku Zasshi (in Japanese). 88 (6): 457–66. doi:10.1254/fpj.88.457. PMID 2881854.
^ Przegaliński E, Baran L, Siwanowicz J, Rawłów A (1986). "The lack of antidepressant properties and a potent central antiserotonin activity of Org 8282". Pol J Pharmacol Pharm. 38 (4): 377–84. PMID 3774630.

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[1] Buschmann, H.; Torrens, A.; Vela, J. M. (2007). Antidepressants, Antipsychotics, Anxiolytics: From Chemistry and Pharmacology to Clinical Application. 1. Wiley VCH. p. 248. ISBN 978-3-527-31058-6.

[IndexNominum-2] Swiss Pharmaceutical Society, ed. (2000). Index Nominum 2000: International Drug Directory. Medpharm Scientific Publishers. p. 942. ISBN 3-88763-075-0.

[PDSP-3] Roth, BL; Driscol, J. "PDSP K_i Database". Psychoactive Drug Screening Program (PDSP). University of North Carolina at Chapel Hill and the United States National Institute of Mental Health. Retrieved 14 August 2017.

[pmid3792961-4] Jump up to: ^a ^b ^c ^d ^e Niho T, Ito C, Shibutani Y, Hashizume H, Yamaguchi K (1986). "[Pharmacological properties of MO-8282, a novel antidepressant]". Nippon Yakurigaku Zasshi (in Japanese). 88 (4): 309–20. doi:10.1254/fpj.88.309. PMID 3792961.

[pmid2881854-5] Jump up to: ^a ^b Mizota M, Oikawa Y, Nakayama K, Mizuguchi K, Takarada T, Kojima M, Kanehiro H, Funato H, Kayamoto M, Sato M (1986). "[Pharmacological studies of MO-8282, a new antidepressant]". Nippon Yakurigaku Zasshi (in Japanese). 88 (6): 457–66. doi:10.1254/fpj.88.457. PMID 2881854.

[pmid3774630-6] Przegaliński E, Baran L, Siwanowicz J, Rawłów A (1986). "The lack of antidepressant properties and a potent central antiserotonin activity of Org 8282". Pol J Pharmacol Pharm. 38 (4): 377–84. PMID 3774630.

[1]

[2]

[3]

[4]

[5]

[6]

show v t Anxiolytics (N05B)
5-HT_1AR agonists	Buspirone Gepirone^† Tandospirone
GABA_AR PAMs	Benzodiazepines: Adinazolam Alprazolam Bromazepam Camazepam Chlordiazepoxide Clobazam Clonazepam Clorazepate Clotiazepam Cloxazolam Diazepam^# Ethyl loflazepate Etizolam Fludiazepam Halazepam Ketazolam Lorazepam^# Medazepam Nordazepam Oxazepam Pinazepam Prazepam; Others: Alpidem^‡ Barbiturates (e.g., phenobarbital) Carisoprodol Carbamates (e.g., meprobamate) Chlormezanone^‡ Ethanol (alcohol) Etifoxine Imepitoin; Herbs: Kava Skullcap Valerian
Gabapentinoids (α₂δ VDCC blockers)	Gabapentin Gabapentin enacarbil Phenibut Pregabalin
Antidepressants	SSRIs (e.g., escitalopram) SNRIs (e.g., duloxetine) SARIs (e.g., trazodone) TCAs (e.g., clomipramine^#) TeCAs (e.g., mirtazapine) MAOIs (e.g., phenelzine); Others: Agomelatine Bupropion Tianeptine Vilazodone Vortioxetine
Sympatholytics (Antiadrenergics)	Alpha-1 blockers (e.g., prazosin) Alpha-2 agonists (e.g., clonidine, dexmedetomidine, guanfacine) Beta blockers (e.g., propranolol)
Others	Benzoctamine Cannabidiol Cycloserine Fabomotizole Hydroxyzine Kanna Lavender Lorpiprazole Mebicar Mepiprazole Nicotine Opipramol Oxaflozane^‡ Phenaglycodol Phenibut Picamilon Selank Tiagabine Tofisopam Validolum
^#WHO-EM ^‡Withdrawn from market Clinical trials: ^†Phase III ^§Never to phase III

show v t Tricyclics
Classes	Acridine Anthracene Dibenzazepine Dibenzocycloheptene Dibenzodiazepine Dibenzothiazepine Dibenzothiepin Dibenzoxazepine Dibenzoxepin Phenothiazine Pyridazinobenzoxazine Pyridinobenzodiazepine Thioxanthene
Antidepressants (TCAs and TeCAs)	7-OH-Amoxapine Amezepine Amineptine Amitriptyline Amitriptylinoxide Amoxapine Aptazapine Azepindole Azipramine Batelapine Butriptyline Cianopramine Ciclazindol Ciclopramine Cidoxepin Clomipramine Cotriptyline Cyanodothiepin Demexiptiline Depramine (balipramine) Desipramine (desmethylimipramine) Desmethylclomipramine Dibenzepin Dimetacrine Dosulepin (dothiepin) Doxepin Enprazepine Esmirtazapine Fluotracen Hepzidine Homopipramol Imipramine Imipraminoxide Intriptyline Iprindole Ketipramine Litracen Lofepramine Losindole Loxapine Maprotiline Mariptiline Mazindol Melitracen Metapramine Mezepine Mianserin Mirtazapine Naranol Nitroxazepine Nordoxepin Northiaden (nordosulepin) Nortriptyline (noramitriptyline) Noxiptiline Octriptyline Opipramol Oxaprotiline Pipofezine Pirandamine Propizepine Protriptyline Quinupramine Setiptiline (teciptiline) Tandamine Tampramine Tianeptine Tienopramine Trimipramine
Antihistamines	Azatadine Bisulepin Clobenzepam Cyproheptadine Dacemazine Deptropine Desloratadine Epinastine Etymemazine Fenethazine Hydroxyethylpromethazine Isopromethazine Isothipendyl Ketotifen Latrepirdine Loratadine Mebhydrolin Mequitazine Methdilazine Olopatadine Oxomemazine Phenindamine Pimethixene Promethazine Propiomazine Rupatadine Thiazinamium
Antipsychotics	Acetophenazine Alimemazine Amoxapine Asenapine Butaclamol Butaperazine Carfenazine (carphenazine) Carpipramine Chlorpromazine Chlorprothixene Ciclindole Clocapramine Clorotepine Clotiapine Clozapine Flucindole Flumezapine Fluotracen Flupentixol Fluphenazine Gevotroline Homopipramol Levomepromazine/Methotrimeprazine Loxapine Lurasidone Mesoridazine Metiapine Metitepine Mosapramine Naranol Olanzapine Oxyprothepin Perathiepin Perazine Perphenazine Periciazine Pinoxepin Piperacetazine Pipotiazine Piquindone Prochlorperazine Promazine Prothipendyl Quetiapine Sulforidazine Tenilapine Thiethylperazine Thiopropazate Thioridazine Thiothixene Trifluoperazine Triflupromazine Zotepine Zuclopenthixol
Anticonvulsants	Carbamazepine Dizocilpine Eslicarbazepine Eslicarbazepine acetate Etazepine Licarbazepine Oxcarbazepine Oxitriptyline
Others	Adosopine Atiprosin Benzoctamine Carvedilol Cidoxepin Cyclobenzaprine Methylene blue Monatepil Oxetorone Perlapine Pipazethate P7C3 Pirenzepine Pirolate Pitrazepin Pizotifen Profenamine Serazapine Telenzepine Tropatepine

Setiptiline

Contents

Pharmacology[]

Pharmacodynamics[]

Chemistry[]

See also[]

References[]