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[Binding of dicyclohexylamide derivatives of N-substituted aminocarboxylic acids with muscarinic cholinoreceptors and beta-adrenoreceptors]. / Sviazyvanie proizvodnykh ditsiklogeksilamidov N-zameshchennykh aminokarbonovykh kislot s muskarinovymi kholinoretseptorami i beta-adrenoretseptorami.
Brusova, E G; Kaverina, N V; Likhosherstov, A M.
Afiliación
  • Brusova EG; Laboratory of Circulation System Pharmacology, Institute of Pharmacology, Russian Academy of Medical Sciences, Baltiiskaya ul. 8, Moscow, 125315 Russia.
Eksp Klin Farmakol ; 65(5): 39-41, 2002.
Article en Ru | MEDLINE | ID: mdl-12596513
The binding of N-substituted aminocarboxylic acid dicyclohexylamide (NACA-DCHA) derivatives to M-1 muscarinic cholinoreceptors (MRs) in rat brain cortex and and beta-1 adrenoreceptors (ARs) in rat heart was studied. The maximum MR affinity was observed for AL-275 (IC50, 2.8 microM) and AL-315 (IC 50, 3.2 microM) preparations. The other compounds (except AL-310 with IC50 > 100 microM) interacted with MR at a lower affinity. The binding to beta-1 AR in rat heart was observed for a single preparation AL-298 (IC50, 38 microM). The antimuscarinic activity of some NACA-DCHA derivatives, especially AL-275 and AL-315) may play a significant role in realization of the antiarrhythmic activity.
Asunto(s)
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Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Receptores Adrenérgicos beta / Receptores Muscarínicos / Ciclohexilaminas / Aminoácidos Límite: Animals Idioma: Ru Revista: Eksp Klin Farmakol Asunto de la revista: FARMACOLOGIA Año: 2002 Tipo del documento: Article Pais de publicación: Rusia
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Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Receptores Adrenérgicos beta / Receptores Muscarínicos / Ciclohexilaminas / Aminoácidos Límite: Animals Idioma: Ru Revista: Eksp Klin Farmakol Asunto de la revista: FARMACOLOGIA Año: 2002 Tipo del documento: Article Pais de publicación: Rusia