Abecarnil

• CAS: 111841-85-1
• Catalog Number: ACM111841851
• Category: Agonists
• Molecular Weight: 404.47
• Molecular Formula: C24H24N2O4
• Description: Abecarnil is a beta carboline and a partial benzodiazepine-receptor agonist that has demonstrated promise as an anxiolytic agent. It may be useful in treating generalized anxiety disorder.
• Synonyms: Abecarnil; ZK 112119; ZK-112119; ZK112119
• IUPAC Name: 6-(Benzyloxy)-4-(methoxymethyl)-9H-pyrido[3,4-b]indole-3-carboxylic acid 1-methylethyl ester
• Canonical SMILES: O=C(C1=C(COC)C2=C(C=N1)NC3=C2C=C(OCC4=CC=CC=C4)C=C3)OC(C)C
• InChI: InChI=1S/C24H24N2O4/c1-15(2)30-24(27)23-19(14-28-3)22-18-11-17(29-13-16-7-5-4-6-8-16)9-10-20(18)26-21(22)12-25-23/h4-12,15,26H,13-14H2,1-3H3
• InChI Key: RLFKILXOLJVUNF-UHFFFAOYSA-N
• Solubility: Soluble in DMSO
• Appearance: Solid powder
• Shelf Life: >2 years if stored properly
• Storage: Dry, dark and at 0-4 °C for short term (days to weeks) or -20 °C for long term (months to years).
• Biological Target: Abecarnil (ZK 112119) is a ligand or a partial agonist for benzodiazepine (BZ) receptor. Abecarnil can act as a positive allosteric modulator of GABAA receptor. Abecarnil inhibits the binding of the BZ [3H]lormetazepam to rat cerebral cortex membranes, with an IC50 of 0.82 nM.
• Drug Formulation: This drug may be formulated in DMSO
• Elemental Analysis: C, 71.27; H, 5.98; N, 6.93; O, 15.82
• Exact Mass: 404.1736
• HS Tariff Code: 2934.99.9001
• In Vitro Activity: In vitro, abecarnil inhibited the binding of the BZ [3H]lormetazepam to rat cerebral cortex membranes with an IC50 value of 0.82 nM in comparison to 56 nM for DZP.; Reference: J Pharmacol Exp Ther. 1990 Apr;253(1):334-43. https://pubmed.ncbi.nlm.nih.gov/1970361/
• In Vivo Activity: Abecarnil, a selective benzodiazepine receptor agonist with marked anticonvulsant activity, was administered together with chronic PTZ to evaluate whether persistent activation of GABAA receptors and suppression of seizures during kindling might affect the sensitivity of septohippocampal cholinergic neurons to a challenge dose of PTZ. Abecarnil (1 mg/kg, i.p.) administered 40 min before each PTZ injection neither antagonized the decrease in basal acetylcholine release (2.26 +/- 0.19 pmol per 20-min sample) nor prevented the development of kindling. In contrast, abecarnil prevented the chronic PTZ-induced increase in the sensitivity of acetylcholine release to a challenge dose of PTZ.; Reference: J Neurochem. 1997 Jan;68(1):313-8. https://pubmed.ncbi.nlm.nih.gov/8978740/
• Shipping: 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.
• Stock Solution Storage: 0-4 °C for short term (days to weeks), or -20 °C for long term (months).