111841-85-1 Usage
Description
Abecarnil is a β-carboline-3-carboxylic acid derivative that is in development for the treatment of anxiety disorders. Animal work has shown that abecarnil has a low propensity to cause the problems of dependency and abuse and that the drug has marked anxiolytic and anticonvulsant activity but does not appear to have significant effects on motor coordination—a finding in marked contrast to the effects of diazepam (Stephens et al. 1990). This interesting phenomena may be explained by the fact that abecarnil is acting as a full agonist at some receptors that mediate certain effects (potent anxiolytic) and as a partial agonist at others (lack of side effects). One published clinical study compared abecarnil at different doses with placebo in patients with generalized anxiety disorder (Ballenger et al. 1991). This showed that abecarnil was significantly more effective than placebo in terms of anxiolysis. Stopping treatment produced no withdrawal effects in patients on the lower dose, although some effects were seen in those taking higher doses.
Originator
Abecarnil,Schepa
Uses
Abecarnil is a partial agonist at the benzodiazepine–GABA receptor complex, and is used in generalized anxiety disorder.
Therapeutic Function
Anticonvulsant, Anxiolytic
Hazard
Human systemic effects.
Check Digit Verification of cas no
The CAS Registry Mumber 111841-85-1 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,1,1,8,4 and 1 respectively; the second part has 2 digits, 8 and 5 respectively.
Calculate Digit Verification of CAS Registry Number 111841-85:
(8*1)+(7*1)+(6*1)+(5*8)+(4*4)+(3*1)+(2*8)+(1*5)=101
101 % 10 = 1
So 111841-85-1 is a valid CAS Registry Number.
InChI:InChI=1/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
111841-85-1Relevant articles and documents
Synthesis of β- and γ-carbolines by the palladium-catalyzed iminoannulation of alkynes
Zhang, Haiming,Larock, Richard C.
, p. 9318 - 9330 (2002)
A variety of substituted β- and γ-carbolines have been prepared in moderate to excellent yields by the palladium-catalyzed annulation of internal and terminal acetylenes by the tert-butylimines of N-substituted 3-iodoindole-2-carboxaldehydes and 2-haloindole-3-carboxaldehydes, respectively. This annulation chemistry is effective for a wide range of alkynes, including aryl-, alkyl-, hydroxymethyl-, ethoxycarbonyl-, and trimethylsilyl-substituted alkynes. When an unsymmetrical internal alkyne is employed, this method generally gives two regioisomers. When a terminal alkyne is employed, only one regioisomer has been isolated. This palladium-catalyzed annulation chemistry has also been successfully applied to the synthesis of two biologically interesting β-carboline alkaloids, ZK93423 and abecarnil (ZK112119).
5-or 6-Substituted beta-carboline-3-carboxylic-acid esters
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, (2008/06/13)
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