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MedKoo Cat#: 326698 | Name: Aptazapine maleate

Description:

WARNING: This product is for research use only, not for human or veterinary use.

Aptazapine, also known as CGS 7525A, is a tetracyclic antidepressant (TeCA) which was assayed in clinical trials for the treatment of depression in the 1980s but was never marketed. 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. Based on its pharmacological profile, aptazapine may be classified as a noradrenergic and specific serotonergic antidepressant (NaSSA).

Chemical Structure

Aptazapine maleate
CAS#71576-41-5 (maleate)

Theoretical Analysis

MedKoo Cat#: 326698

Name: Aptazapine maleate

CAS#: 71576-41-5 (maleate)

Chemical Formula: C20H23N3O4

Exact Mass:

Molecular Weight: 369.42

Elemental Analysis: C, 65.03; H, 6.28; N, 11.37; O, 17.32

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
71576-40-4 (free base) 71576-41-5 (maleate)
Synonym
CGS 7525A; CGS-7525A; CGS7525A; Aptazapine maleate
IUPAC/Chemical Name
2-methyl-1,3,4,14b-tetrahydro-2H,10H-benzo[e]pyrazino[2,1-c]pyrrolo[1,2-a][1,4]diazepine maleate
InChi Key
JJTOHZLQMBVMPF-BTJKTKAUSA-N
InChi Code
InChI=1S/C16H19N3.C4H4O4/c1-17-9-10-19-14-6-3-2-5-13(14)11-18-8-4-7-15(18)16(19)12-17;5-3(6)1-2-4(7)8/h2-8,16H,9-12H2,1H3;1-2H,(H,5,6)(H,7,8)/b;2-1-
SMILES Code
CN(CC1)CC2N1C3=CC=CC=C3CN4C2=CC=C4.O=C(O)/C=C\C(O)=O
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Related: 71576-41-5 (Aptazapine maleate) 71576-40-4 (Aptazapine free base).

Preparing Stock Solutions

The following data is based on the product molecular weight 369.42 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Cirilli R, Orlando V, Ferretti R, Turchetto L, Silvestri R, De Martino G, La Torre F. Direct HPLC enantioseparation of chiral aptazepine derivatives on coated and immobilized polysaccharide-based chiral stationary phases. Chirality. 2006 Aug;18(8):621-32. PubMed PMID: 16715514. 2: Nishino S, Haak L, Shepherd H, Guilleminault C, Sakai T, Dement WC, Mignot E. Effects of central alpha-2 adrenergic compounds on canine narcolepsy, a disorder of rapid eye movement sleep. J Pharmacol Exp Ther. 1990 Jun;253(3):1145-52. PubMed PMID: 1972749. 3: Gower AJ, Broekkamp CL, Rijk HW, Van Delft AM. 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. Arch Int Pharmacodyn Ther. 1988 Jan-Feb;291:185-201. PubMed PMID: 2896489. 4: Gerhardt S, Liebman JM. Self-regulation of ICSS duration: effects of anxiogenic substances, benzodiazepine antagonists and antidepressants. Pharmacol Biochem Behav. 1985 Jan;22(1):71-6. PubMed PMID: 2858109. 5: DeHaas Vermeulen J, Thompson TA. Assay for the determination of the tetracyclic antidepressant compound aptazapine in plasma by high-performance liquid chromatography. J Chromatogr. 1984 Mar 9;306:412-6. PubMed PMID: 6715482. 6: Liebman JM, Lovell RA, Braunwalder A, Stone G, Bernard P, Barbaz B, Welch J, Kim HS, Wasley JW, Robson RD. CGS 7525A, a new, centrally active alpha 2 adrenoceptor antagonist. Life Sci. 1983 Jan 24;32(4):355-63. PubMed PMID: 6131367.