RESUMEN
Inhibition of monoamine oxidase A (MAO A) is believed to cause antidepressant and possibly antianxiety effects. The previous paper had developed structure-activity relationships (SAR) for in vitro MAO A inhibition by tricyclic N-arylamides. It is shown in this paper that the same in vitro SAR can be carried over to tricyclics whose potentially toxic amide function is replaced by an appropriately substituted imidazoline, a 1,2,4- or 1,3,4-oxadiazole, or an alkylated tetrazole moiety. Dialysis of the inhibitor from the enzyme was used as a measure of reversibility which correlates with a low ability to cause a blood pressure rise with ingested tyramine ("cheese effect").
Asunto(s)
Imidazoles/análisis , Inhibidores de la Monoaminooxidasa/farmacología , Oxadiazoles/análisis , Tetrazoles/análisis , Inhibidores de la Monoaminooxidasa/química , Relación Estructura-ActividadRESUMEN
2-Ethoxy-6-(5-tetrazolyl)xanthone reduces the oxygen affinity of blood by two mechanisms; firstly, by a direct effect on the haemoglobin molecule and secondly by maintaining levels of 2,3-diphosphoglycerate (DPG) in stored blood. This compound thus has potential as a blood storage additive which will improve the oxygen delivery of stored blood.
Asunto(s)
Ácidos Difosfoglicéricos/sangre , Eritrocitos/metabolismo , Hemoglobinas/metabolismo , Oxígeno/sangre , Xantenos/farmacología , Xantonas , 2,3-Difosfoglicerato , Adenosina Trifosfato/sangre , Conservación de la Sangre , Eritrocitos/efectos de los fármacos , Humanos , Concentración de Iones de HidrógenoAsunto(s)
Antivirales , Flavonoides/farmacología , Rhinovirus/efectos de los fármacos , Tejido Adiposo/metabolismo , Animales , Encéfalo/metabolismo , Evaluación Preclínica de Medicamentos , Células HeLa/metabolismo , Humanos , Cinética , Hígado/metabolismo , Pulmón/metabolismo , Ratas , Distribución TisularRESUMEN
In-vivo studies have demonstrated antiallergic properties in doxantrazole when given orally to rats. These properties were confirmed in work with in-vitro preparations. No significant animal toxicity has been detected. 200 mg. given by mouth inhibited the immediate-type asthmatic response in volunteer patients challenged with specific antigen.