Chemistry:Aptazapine

Aptazapine
Clinical data
ATC code	none;
Identifiers
	IUPAC name 2-methyl-1,3,4,14b-tetrahydro-2H,10H-pyrazino[1,2-a]pyrrolo[2,1-c][1,4]benzodiazepine;
CAS Number	71576-40-4 ;
PubChem CID	51355;
ChemSpider	46513 ;
UNII	240J927J1R;
KEGG	D02972 ;
ChEMBL	ChEMBL336712 ;
Chemical and physical data
Formula	C16H19N3
Molar mass	253.349 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES c42c(N3C(c1cccn1C2)CN(CC3)C)cccc4;
	InChI InChI=1S/C16H19N3/c1-17-9-10-19-14-6-3-2-5-13(14)11-18-8-4-7-15(18)16(19)12-17/h2-8,16H,9-12H2,1H3 ; Key:MNHDDERDSNZCCK-UHFFFAOYSA-N ;
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Short description: Chemical compound

Aptazapine (developmental code name CGS-7525A) is a tetracyclic antidepressant (TeCA) that was assayed in clinical trials for the treatment of depression in the 1980s but was never marketed.^[1]^[2]^[3] It is a potent α₂-adrenergic receptor antagonist with ~10x the strength of the related compound mianserin and has also been shown to act as a 5-HT₂ receptor antagonist and H₁ receptor inverse agonist, while having no significant effects on the reuptake of serotonin or norepinephrine.^[1]^[4] Based on its pharmacological profile, aptazapine may be classified as a noradrenergic and specific serotonergic antidepressant (NaSSA).

References

↑ ^1.0 ^1.1 "CGS 7525A, a new, centrally active alpha 2 adrenoceptor antagonist". Life Sciences 32 (4): 355–63. January 1983. doi:10.1016/0024-3205(83)90081-4. PMID 6131367.
↑ Author Unknown (1985). Annual Reports in Medicinal Chemistry (Volume 20). Boston: Academic Press. pp. 352. ISBN 0-12-040520-2. https://books.google.com/books?id=j-3Cd_SWIksC&q=aptazapine&pg=PA33.
↑ David J. Triggle (1997). Dictionary of pharmacological agents. London: Chapman & Hall. ISBN 0-412-46630-9. https://books.google.com/books?id=DeX7jgInYFMC&q=aptazapine&pg=PA167.
↑ "Pharmacological evaluation of in vivo tests for alpha 2-adrenoceptor blockade in the central nervous system and the effects of the enantiomers of mianserin and its aza-analog ORG 3770". Archives Internationales de Pharmacodynamie et de Thérapie 291: 185–201. 1988. PMID 2896489.

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Original source: https://en.wikipedia.org/wiki/Aptazapine. Read more

[pmid6131367-1] 1.0 ^1.1 "CGS 7525A, a new, centrally active alpha 2 adrenoceptor antagonist". Life Sciences 32 (4): 355–63. January 1983. doi:10.1016/0024-3205(83)90081-4. PMID 6131367.

[isbn0-12-040520-2-2] Author Unknown (1985). Annual Reports in Medicinal Chemistry (Volume 20). Boston: Academic Press. pp. 352. ISBN 0-12-040520-2. https://books.google.com/books?id=j-3Cd_SWIksC&q=aptazapine&pg=PA33.

[isbn0-412-46630-9-3] David J. Triggle (1997). Dictionary of pharmacological agents. London: Chapman & Hall. ISBN 0-412-46630-9. https://books.google.com/books?id=DeX7jgInYFMC&q=aptazapine&pg=PA167.

[pmid2896489-4] "Pharmacological evaluation of in vivo tests for alpha 2-adrenoceptor blockade in the central nervous system and the effects of the enantiomers of mianserin and its aza-analog ORG 3770". Archives Internationales de Pharmacodynamie et de Thérapie 291: 185–201. 1988. PMID 2896489.

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[2]

[3]

[4]

v t e 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 Desmethyltrimipramine Dibenzepin Dimetacrine Dosulepin (dothiepin) Doxepin Enprazepine Esmirtazapine Fantridone Fluotracen Hepzidine Homopipramol Imipramine Imipraminoxide Intriptyline Iprindole Ketipramine Litracen Lofepramine Losindole Loxapine Maprotiline Mariptiline Mazindol Melitracen Metapramine Mezepine Mianserin Mirtazapine Monometacrine Naranol Nitroxazepine Norbutriptyline Nordoxepin Northiaden (nordosulepin) Nortriptyline (noramitriptyline) Noxiptiline Octriptyline Opipramol Oxaprotiline Pipofezine Pirandamine Propizepine Protriptyline Quinupramine Setiptiline (teciptiline) Spiroxepin 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 Citatepine Clocapramine Clomacran Clorotepine Clotiapine Clozapine Cyanothepin Doclothepin Docloxythepin Erizepine Flucindole Flumezapine Fluotracen Flupentixol Fluphenazine Gevotroline Homopipramol Isofloxythepin Levomepromazine/Methotrimeprazine Loxapine Lurasidone Maroxepin Meperathiepin Mesoridazine Metiapine Metitepine Metoxepin Mosapramine Naranol Octomethothepin Olanzapine Oxyclothepin Oxyprothepin Pentiapine Peradithiepin Perathiepin Perazine Perphenazine Periciazine Pinoxepin Piperacetazine Pipotiazine Piquindone Prochlorperazine Promazine Prothipendyl Quetiapine Savoxepin/Cipazoxapine Sulforidazine Tenilapine Thiethylperazine Thiopropazate Thioridazine Thiothixene Tilozepine Traboxopine Trifluoperazine Triflupromazine Trifluthepin Zotepine Zuclopenthixol
Anticonvulsants	Carbamazepine Dizocilpine Eslicarbazepine Eslicarbazepine acetate Etazepine Licarbazepine Oxcarbazepine Oxitriptyline Rispenzepine
Others	Adosopine Aminopromazine Atiprosin Beloxepin Benzoctamine Carvedilol Cidoxepin Cyclobenzaprine Damotepine Darenzepine Elanzepine Fluradoline Methylene blue Monatepil Nuvenzepine Oxetorone Perlapine P7C3 Pinadoline Pirenzepine Pirolate Pitrazepin Pizotifen Profenamine Serazapine Siltenzepine Telenzepine Tipindole Tropatepine Zolenzepine

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Clinical data

ATC code	none
Identifiers
IUPAC name 2-methyl-1,3,4,14b-tetrahydro-2H,10H-pyrazino[1,2-a]pyrrolo[2,1-c][1,4]benzodiazepine
CAS Number	71576-40-4^N
PubChem CID	51355
ChemSpider	46513^Y
UNII	240J927J1R
KEGG	D02972^Y
ChEMBL	ChEMBL336712^Y
Chemical and physical data
Formula	C₁₆H₁₉N₃
Molar mass	253.349 g·mol⁻¹
3D model (JSmol)	Interactive image
SMILES c42c(N3C(c1cccn1C2)CN(CC3)C)cccc4
InChI InChI=1S/C16H19N3/c1-17-9-10-19-14-6-3-2-5-13(14)11-18-8-4-7-15(18)16(19)12-17/h2-8,16H,9-12H2,1H3^Y Key:MNHDDERDSNZCCK-UHFFFAOYSA-N^Y
^NY (what is this?) (verify)

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