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Anxiolytic Activity (anxiolytic + activity)

Distribution by Scientific Domains
Medical Sciences75%
Chemistry25%

Selected Abstracts

Synthesis, Structure,Activity Relationships, and Anxiolytic Activity of 7-Aryl-6,7-dihydroimidazoimidazole Corticotropin-Releasing Factor 1 Receptor Antagonists.

CHEMINFORM, Issue 50 2005
Xiaojun Han
Abstract For Abstract see ChemInform Abstract in Full Text. [source]

Early behavioral screening for antidepressants and anxiolytics

DRUG DEVELOPMENT RESEARCH, Issue 9 2006
Vincent Castagné
Abstract Early preclinical behavioral testing is an essential stage during the development of substances with potential antidepressant and/or anxiolytic activity. With the growing cost of drug development, optimal research strategies are needed to detect potential new treatments with high efficacy and minimal side effects and to confirm in vitro pharmacological studies. In the following article, we present simple rodent tests used for early behavioral testing for antidepressant-like and anxiolytic-like activity. Unpublished results from our laboratory are discussed with reference to published data to illustrate the predictive validity of several behavioral screening tests. Drug Dev. Res. 67:729,742, 2006. © 2006 Wiley-Liss, Inc. [source]

Prediction of polymorphic N -acetylation of new drug candidates by correlation with human NAT1 and NAT2

DRUG DEVELOPMENT RESEARCH, Issue 1 2002
Katalin Jemnitz
Abstract Due to interindividual variation in N -acetyltransferase 2 (NAT2) activity, pharmaceutical companies face the problem of polymorphic metabolism in drugs that are metabolized mainly or exclusively by this enzyme. An in vitro method has been developed to predict in vivo polymorphic N -acetylation at an early stage of drug development. Two new type 5H-2,3-benzodiazepine derivatives, Nerisopam (NER) with anxiolytic activity and GYKI47261 with antiepileptic activity, are metabolized mainly by N -acetylation in the rat and human. The selectivity of human N -acetyltransferases (NAT1,2) to form the acetylated metabolites has been investigated by correlation analysis. Twelve human liver samples were characterized for NAT1 and NAT2 phenotype based on their enzyme activity toward two selective NAT1 (p -aminobenzoic acid, PABA; p -aminosalicylic acid, PAS) and two selective NAT2 (sulfamethazine, SMZ; procainamide, PROC) substrates. Significant correlation was found between enzyme activities NAT1PABA/NAT1PAS and NAT2SMZ/NAT2PROC, respectively, and no correlation was observed comparing enzyme activities toward NAT1PABA/NAT2PROC. Enzyme activities using NER and GYKI 47261 as substrates were compared to activities obtained with NAT1 and NAT2 selective substrates, and the correlation coefficients were calculated. Good correlation was established between the rates of acetylation of the two drugs and that of the NAT2 selective substrate (NER/NAT2SMZ, r2=0.91, GYKI 47261/NAT2SMZ, r2=0.91). In contrast, no correlation was found between the rate of conjugation of the drugs and that of NAT1 selective substrate (NER/NAT1PABA, r2=0.022, GYKI 47261/NAT1PABA, r2=0.0004), suggesting polymorphic in vivo metabolism, since both drugs are acetylated preferably by NAT2. According to our results, correlation analysis based on in vitro acetylation activity may be used to predict in vivo polymorphic metabolism. Drug Dev. Res. 56:17,22, 2002. © 2002 Wiley-Liss, Inc. [source]

Relationship between cerebral pharmacokinetics and anxiolytic activity of diazepam and its active metabolites after a single intra-peritoneal administration of diazepam in mice

HUMAN PSYCHOPHARMACOLOGY: CLINICAL AND EXPERIMENTAL, Issue 5 2002
E. Dailly
Abstract The relationship between the cerebral pharmacokinetics of diazepam and its active metabolites (desmethyldiazepam, oxazepam) and the anxiolytic effect evaluated by the four-plates test and the light/dark test were investigated after a single intra-peritoneal injection of diazepam (1,mg/kg or 1.5,mg/kg). For up to 30,min after administration, the sedative effect interfered with the anxiolytic effect, thus the results of the anxiolytic effect were not interpretable. From 30,min to 60,min after administration, this interference disappeared, the cerebral level of benzodiazepines was stable (the brain elimination of diazepam was compensated for by the appearance of desmethyldiazepam followed by oxazepam) but the anxiolytic effect decreased dramatically in all the tests with diazepam 1,mg/kg or 1.5,mg/kg. The acute tolerance to benzodiazepines and the difference of affinity for subtypes of GABA(A) receptors between diazepam, desmethyldiazepam, oxazepam could explain this result. Copyright © 2002 John Wiley & Sons, Ltd. [source]

Synthesis of the anxiolytic agent [14C] 6-hydroxy-buspirone for use in a human ADME study

JOURNAL OF LABELLED COMPOUNDS AND RADIOPHARMACEUTICALS, Issue 2 2007
Samuel J. Bonacorsi Jr
Abstract A reliable synthesis of 14C labeled 6-hydroxy-buspirone is described. The molecule belongs to a unique class of compounds with the potential for anxiolytic activity. A radiolabeled analog was prepared to support the development of 6-hydroxy-buspirone. Specifically, a labeled variant was designed to meet the requirements of a human adsorption-distribution-metabolism-elimination (ADME) study. Multiple 14C labels were needed to fully track the potential metabolic transformation of the molecule. Labeled 6-hydroxy-buspirone was prepared by oxidation of separately labeled versions of [14C]buspirone. The final product was isolated in reasonable yield with a radiochemical purity of 99.8%. Copyright © 2007 John Wiley & Sons, Ltd. [source]

Evaluation of anxiolytic activity of spray dried powders of two South Brazilian Passiflora species

PHYTOTHERAPY RESEARCH, Issue 5 2006
Flávio H. Reginatto
Abstract The Passiflora extracts have been used in folk medicine because of its reputed sedative and anxiolytic properties. The present study aimed to compare the potential anxiolytic activity of two Passiflora spray-dried powders obtained from P. alata and P. edulis, known in Brazil as ,maracujá'. Male adult Swiss rats were treated with 200, 400 and 800 mg/kg of spray-dried powders p.o. and anxiolytic activity was evaluated using the elevated plus-maze test. The spray-dried powders showed anxiolytic activity in doses of 400 and 800 mg/kg. Our results support the potential anxiolytic effect of Passiflora spray-dried powders (P. alata and P. edulis). Copyright © 2006 John Wiley & Sons, Ltd. [source]