Search results for "Azepine"

1-Methyl-?-carboline (Harmane), a potent endogenous inhibitor of benzodiazepine receptor binding

1980

The interaction of several beta-carbolines with specific [3H]-flunitrazepam binding to benzodiazepine receptors in rat brain membranes was investigated. Out of the investigated compounds, harmane and norharmane were the most potent inhibitors of specific [3H]-flunitrazepam binding, with IC50-values in the micromolar range. All other derivatives, including harmine, harmaline, and several tetrahydroderivatives were at least ten times less potent. Harmane has been previously found in rat brain and human urine, so it is the most potent endogenous inhibitor of specific [3H]-flunitrazepam binding known so far, with a several fold higher affinity for the benzodiazepine receptor than inosine and hy…

Epoxides metabolically produced from some known carcinogens and from some clinically used drugs. I. Differences in mutagenicity.

1975

The epoxide metabolites of two clinically used drugs and an experimental psychotropic agent, carbamazepine 10,11-oxide, cyproheptadine 10,11-oxide and cyclobenzaprine 10,11-oxide, were fully devoid of any mutagenic activity under conditions where K-region-epoxide metabolites of some known carcinogens, such as benzo (a)pyrene, proved to be potent frameshift mutational agents for Salmonella typhimurium TA 1537 and TA 1538. All epoxides tested were non-mutagenic for TA 1535, designed to detect substitution mutations. The 10,11-epoxides of the three drugs, carbamazepine, cyproheptadine and cyclobenzaprine, were not cytotoxic to any of the bacterial tester strains used, precluding that mutagenic…

Isoindolo[1,5]benzoxazepine as Potential Antitumor and/or Antiviral Agents

2013

Cerium(IV)-Catalyzed Single Electron Transfer(SET) on Acenaphthene and 1,4-Dihydronaphtho-[1,8-d,e][1,2]diazepine: Chemical Evidence for Distinct Rad…

1987

The influence of Span®20 on stratum corneum lipids in Langmuir monolayers: comparison with Azone®

2000

Recently we have proved that Span 20 has the same enhancer effect as Azone on in vitro percutaneous penetration of lipophilic compounds (logP(oct) from 1.34 to 2.33). The purpose of this work is to study the interactions of Span 20 with stratum corneum lipids monolayers and to compare them with Azone. The surface pressure-area characteristics of Span 20 in mixed monolayers with different model lipids (ceramides, cholesterol, free fatty acids and two mixtures of ceramides+cholesterol, and ceramides+cholesterol+free fatty acids) in similar proportions to that which exists in human stratum corneum lipids were recorded as compression isotherms at 25 degrees C. Azone was also investigated on mon…

Combination strategies for enhancing transdermal absorption of sumatriptan through skin

2006

The aim of the present work was to characterize in vitro sumatriptan transdermal absorption through human skin and to investigate the effect of chemical enhancers and iontophoresis applied both individually and in combination. A secondary objective was to compare the results obtained with those in porcine skin under the same conditions, in order to characterize the relationship between the two skin models and validate the porcine model for further research use. Transdermal flux of sumatriptan was determined in different situations: (a) after pre-treatment of human skin with ethanol, Azone (1-dodecyl-azacycloheptan-2-one), polyethylene glycol 600 and R-(+)-limonene, (b) under iontophoresis a…

CCDC 1847752: Experimental Crystal Structure Determination

2018

Related Article: Carles Lluna‐Galán, Gonzalo Blay, Isabel Fernández, M. Carmen Muñoz, José R. Pedro, Carlos Vila|2018|Adv.Synth.Catal.|360|3662|doi:10.1002/adsc.201800754

CCDC 2069303: Experimental Crystal Structure Determination

2021

Related Article: Renè Hommelsheim, Heliana Michaela Núñez Ponce, Khai-Nghi Truong, Kari Rissanen, Carsten Bolm|2021|Org.Lett.|23|3415|doi:10.1021/acs.orglett.1c00874

CCDC 2069304: Experimental Crystal Structure Determination

2021

Related Article: Renè Hommelsheim, Heliana Michaela Núñez Ponce, Khai-Nghi Truong, Kari Rissanen, Carsten Bolm|2021|Org.Lett.|23|3415|doi:10.1021/acs.orglett.1c00874

CCDC 1413502: Experimental Crystal Structure Determination

2016

Related Article: Lei Wang, Sun Li, Marcus Blümel, Arne R. Philipps, Ai Wang, Rakesh Puttreddy, Kari Rissanen, Dieter Enders|2016|Angew.Chem.,Int.Ed.|55|11110|doi:10.1002/anie.201604819