ABSTRACT
As an important member of metabotropic glutamate receptors (mGluR), metabotropic glutamate receptor 1 (mGluR1) plays an important role in the signal transduction of central nervous system. Selective mGluR1 antagonists can block the signaling pathway activated by mGluR1 and exert a series of physiological actions including analgesia, antianxiety, antidepression, etc. Currently, the discovery and modification of selective mGluR1 antagonists have become a hot research focus. This paper reviews the structural catalogs of selective mGluR1 antagonists and their structure-activity relationships in the last decade.
Subject(s)
Animals , Analgesics , Chemistry , Pharmacokinetics , Pharmacology , Benzimidazoles , Chemistry , Pharmacokinetics , Pharmacology , Blood-Brain Barrier , Cycloheptanes , Chemistry , Pharmacokinetics , Pharmacology , Heterocyclic Compounds, 3-Ring , Chemistry , Pharmacokinetics , Pharmacology , Pain Measurement , Pyrimidines , Chemistry , Pharmacokinetics , Pharmacology , Receptors, Metabotropic Glutamate , Chemistry , Signal Transduction , Structure-Activity Relationship , Thiazoles , Chemistry , Pharmacokinetics , PharmacologyABSTRACT
Decent research on azulene compounds has indicated wide-spread interest in large ring compounds containing aromatic and heteroaromatic structures, In extension to our studies in arenotropones, arenotropilidenes, and their metal complexes, we examine in this investigation the reactivity of the carbonyl group in the seven membered ting towards some organolithium reagents as an avenue for the preparation of Cycloheptatriene derivatives
Subject(s)
CycloheptanesABSTRACT
Se investigo la eficacia y tolerancia del fumarato de benciclan en 25 enfermos con padecimiento vascular obstructivo arterial de las extremidades inferiores. El estado de los enfermos al cabo de 4 a 6 meses de tratamiento mostro la utilidad del medicamento cuando se desea un efecto vasodilatador; su tolerancia fue excelente, ya que no se observo ningun efecto colateral. Aunque el numero de enfermos valorados es reducido, podemos concluir que el fumarato de benciclan es un vasodilatador activo y util cuando se complementa con el adecuado manejo de factores de riesgo y el cumplimiento de las medidas higienicas clasicamente aceptadas