Search results for "relationship"

Structure-activity relationship of histamine H2-receptor agonists

1978

As demonstrated by the results the active C-5(4) substituted histamines and Nα-methyl-histamines are to various extents selective H2-receptor agonists.

Arachidonic acid relaxes human pulmonary arteries through K+ channels and nitric oxide pathways.

2004

We aimed to investigate the role of K(+) channels and nitric oxide (NO) on the relaxant effects of arachidonic acid in the human intralobar pulmonary arteries. Arachidonic acid produced a concentration-dependent relaxation (E(max)=93+/-3% of maximal relaxation induced by papaverine 0.1 mM;-log EC(30)=7.03+/-0.09) that was antagonized by the cyclooxygenase inhibitor indomethacin (1 microM), by the combination of cyclooxygenase blockade and cytochrome P450 (CYP) blockade with 17-octadecynoic acid (17-ODYA, 10 microM), by the combination of cyclooxygenase inhibition and NO synthase (NOS) inhibition with N(omega)-nitro-l-arginine (l-NOARG, 100 microM), by the simultaneous inhibition of CYP and …

Drugs and Nondrugs:  An Effective Discrimination with Topological Methods and Artificial Neural Networks

2003

A set of topological and structural descriptors has been used to discriminate general pharmacological activity. To that end, we selected a group of molecules with proven pharmacological activity including different therapeutic categories, and another molecule group without any activity. As a method for pharmacological activity discrimination, an artificial neural network was used, dividing molecules into active and inactive, to train the network and externally validate it. The following plot frequency distribution diagrams were used: a function of the number of drugs within a value interval, and the output value of the neural network versus these values. Pharmacological distribution diagram…

Synthesis of Bioactive 2-Aza-Analogues of Ipecac and Alangium Alkaloids

2010

Interactions of benzodiazepines with human serum albumin. Circular dichroism studies.

1973

The circular dichroism spectra of 12 benzodiazepine derivatives studied in presence of human serum albumin are presented. Nearly all substances give biphasic extrinsic Cotton effects. At the CD maxima the molar ellipticities and the anisotropy factors are calculated. The influence of the chemical structure of the benzodiazepines on the induced Cotton effect is discussed. There is a linear correlation between the anisotropy factors and the logarithms of the partition coefficients of the substances. It is suggested that the phenyl ring of the benzodiazepine molecule is one of the essential groups for the binding of these substances to human serum albumin.

Development of [1,2]oxazoloisoindoles tubulin polymerization inhibitors: Further chemical modifications and potential therapeutic effects against lym…

2022

Lymphomas are among the ten most common cancers, and, although progress has been achieved in increasing survival, there is still an unmet need for more effective therapeutic approaches, including better options for patients with refractory tumors that initially respond but then relapse. The lack of effective alternative treatment options highlights the need to develop new therapeutic strategies capable of improving survival prospects for lymphoma patients. Herein, we describe the identification and exploration of the SAR of a series of [1,2]oxazolo[5,4-e]isoindoles as potent small molecules that bind to the colchicine site of tubulin and that have promise for the treatment of refractory lym…

Analyse des akustischen Geschlechtererkennungsmechanismus (Befreiungsrufe) bei Kröten (GenusBufo)

1968

The release calls of male European toads (B. bufo L.,B. calamita Laur.,B. viridis Laur.) have been described and recorded in the form of spectrograms and oscillograms. While only 1 type of release call is uttered byB. bufo, inB. viridis andB. calamita 2 and 3 types respectively were found. The latter 2 species show a close relationship,B. calamita being the most highly developed toad in Europe.

Structure-activity relationship of furosemide-derived compounds as antagonists of cerebellum-specific GABA(A) receptors.

1998

The Na+-K+-2Cl- cotransporter blocker furosemide inhibits gamma-aminobutyric acid (GABA)-gated chloride currents and reverses GABA-mediated inhibition of [35S]-t-butylbicyclophosphorothionate ([35S]TBPS) binding of the cerebellar alpha6 subunit-containing GABA(A) receptors much more potently than the cerebrocortical non-alpha6 subunit-containing receptors. Of the 44 compounds studied, all precursors or derivatives of diuretics, one compound [hydrazinosulfonyl-furosemide (PF 1885)] reversed 5-microM GABA-induced inhibition of [35S]TBPS binding to cerebellar and cerebrocortical receptors. Three other compounds, all of which are structurally closely related to furosemide, were selective antago…

Copper radiopharmaceuticals for theranostic applications

2018

The growing advancement in nuclear medicine challenges researchers from several different fields to integrate imaging and therapeutic modalities in a theranostic radiopharmaceutical, which can be defined as a molecular entity with readily replaceable radioisotope to provide easy switch between diagnostic and therapeutic applications for efficient and patient-friendly treatment of diseases. For such a reason, the diagnostic and therapeutic potential of all five medical radionuclides of copper have thoroughly been investigated as they boost the hope for development of successful radiotheranostics. To facilitate the mutual understanding between all different specialists working on this multidi…

QRAR models for central nervous system drugs using biopartitioning micellar chromatography.

2002

The capability of biopartitioning Micellar Chromatography, BMC, to describe and estimate pharmacokinetic and pharmacodynamic parameters of central nervous system drugs is reviewed in this article. BMC is a mode of micellar liquid chromatography, MLC, that uses micellar mobile phases of Brij35 (polyoxyethilene(23) lauryl ether) prepared in physiological conditions (pH, ionic strength). The retention of a drug in this system depends on its hydrophobic, electronic and steric properties, which also determine its biological activity. The results of BMC studies suggest that this in vitro approach is an attractive useful tool to be implemented into the lead optimization step of drug development sc…