Pazinaclone

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MedKoo CAT#: 326878

CAS#: 103255-66-9

Description: Pazinaclone, also known as A-77000; DN-2327, is a sedative and anxiolytic drug in the cyclopyrrolone family of drugs. Some other cyclopyrrolone drugs include zopiclone and eszopiclone. Pazinaclone has a very similar pharmacological profile to the benzodiazepines including sedative and anxiolytic properties, but with less amnestic effects, and at low doses it is a relatively selective anxiolytic, with sedative effects only appearing at higher doses. Pazinaclone produces its sedative and anxiolytic effects by acting as a partial agonist at GABAA benzodiazepine receptors, although pazinaclone is more subtype-selective than most benzodiazepines.

Chemical Structure

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Pazinaclone
CAS# 103255-66-9
Instruction

Theoretical Analysis

MedKoo Cat#: 326878
Name: Pazinaclone
CAS#: 103255-66-9
Chemical Formula: C25H23ClN4O4
Exact Mass: 478.14
Molecular Weight: 478.933
Elemental Analysis: C, 62.70; H, 4.84; Cl, 7.40; N, 11.70; O, 13.36

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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Related CAS #: 103255-66-9   147724-27-4    

Synonym: A-77000; A 77000; A77000; DN-2327; DN 2327; DN2327; Pazinaclone

IUPAC/Chemical Name: 2-(7-chloro-1,8-naphthyridin-2-yl)-3-(2-oxo-2-(1,4-dioxa-8-azaspiro[4.5]decan-8-yl)ethyl)isoindolin-1-one

InChi Key: DPGKFACWOCLTCA-UHFFFAOYSA-N

InChi Code: InChI=1S/C25H23ClN4O4/c26-20-7-5-16-6-8-21(28-23(16)27-20)30-19(17-3-1-2-4-18(17)24(30)32)15-22(31)29-11-9-25(10-12-29)33-13-14-34-25/h1-8,19H,9-15H2

SMILES Code: O=C(N(CC1)CCC21OCCO2)CC3N(C4=NC5=NC(Cl)=CC=C5C=C4)C(C6=C3C=CC=C6)=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

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:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 478.93 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
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Pazinaclone. A 77000, DN 2327. Drugs R D. 1999 Jul;2(1):57-9. PubMed PMID: 10610295.

2: Kondo T, Yoshida K, Tanayama S. Absorption of the anxiolytic pazinaclone in animals as a criterion for species selection for toxicity studies. Arzneimittelforschung. 1996 Sep;46(9):839-43. PubMed PMID: 8876929.

3: Kondo T, Yoshida K, Yamamoto M, Tanayama S. Enantiomeric toxicokinetics of the new isoindoline anxiolytic pazinaclone in rats and dogs. Arzneimittelforschung. 1996 Jan;46(1):11-14. PubMed PMID: 8821511.

4: Kondo T, Yoshida K, Yoshimura Y, Tanayama S. Enantioselective pharmacokinetics in animals of pazinaclone, a new isoindoline anxiolytic, and its active metabolite. Biopharm Drug Dispos. 1995 Dec;16(9):755-73. PubMed PMID: 8580400.

5: Kondo T, Hamasaki K, Yamaguchi M, Aoki I, Yoshida K, Yoshimura Y, Tanayama S. Enantioselective determination of pazinaclone, a new isoindoline anxiolytic, and its active metabolite in rat plasma by high-performance liquid chromatography. J Chromatogr B Biomed Appl. 1995 Apr 21;666(2):291-7. PubMed PMID: 7633605.

6: Evans SM, Foltin RW, Levin FR, Fischman MW. Behavioral and subjective effects of DN-2327 (pazinaclone) and alprazolam in normal volunteers. Behav Pharmacol. 1995 Mar;6(2):176-186. PubMed PMID: 11224325.

7: Hussein Z, Mulford DJ, Bopp BA, Granneman GR. Stereoselective pharmacokinetics of pazinaclone, a new non-benzodiazepine anxiolytic, and its active metabolite in healthy subjects. Br J Clin Pharmacol. 1993 Oct;36(4):357-61. PubMed PMID: 12959315; PubMed Central PMCID: PMC1364690.

8: Hussein Z, Mulford DJ, Bopp BA, Granneman GR. Differences in the stereoselective pharmacokinetics of pazinaclone (DN-2327), a new anxiolytic, and its active metabolite after intravenous and oral single doses to dogs. Drug Metab Dispos. 1993 Sep-Oct;21(5):805-10. PubMed PMID: 7902240.