Enhancement of in vitro binding and some of the pharmacological properties of diazepam by a novel anthelmintic agent, Avermectin B1a. 1979

M Williams, and G G Yarbrough

A novel macrocyclic lactone disaccharide anthelmintic agent, Avermectin B1a (AVM) has been found to cause a concentration-dependent increase in the in vitro binding of 3H-diazepam to rat and mouse brain membranes. The increase in binding is manifested as both an increase in the affinity and number of bindings sites for 3H-diazepam. Preliminary in vivo studies demonstrate that AVM can also enhance some of the pharmacological actions of diazepam.

UI MeSH Term Description Entries
D007559 Ivermectin A mixture of mostly avermectin H2B1a (RN 71827-03-7) with some avermectin H2B1b (RN 70209-81-3), which are macrolides from STREPTOMYCES avermitilis. It binds glutamate-gated chloride channel to cause increased permeability and hyperpolarization of nerve and muscle cells. It also interacts with other CHLORIDE CHANNELS. It is a broad spectrum antiparasitic that is active against microfilariae of ONCHOCERCA VOLVULUS but not the adult form. Eqvalan,Ivomec,MK-933,Mectizan,Stromectol,MK 933,MK933
D007783 Lactones Cyclic esters of hydroxy carboxylic acids, containing a 1-oxacycloalkan-2-one structure. Large cyclic lactones of over a dozen atoms are MACROLIDES. Lactone
D009043 Motor Activity Body movements of a human or an animal as a behavioral phenomenon. Activities, Motor,Activity, Motor,Motor Activities
D003975 Diazepam A benzodiazepine with anticonvulsant, anxiolytic, sedative, muscle relaxant, and amnesic properties and a long duration of action. Its actions are mediated by enhancement of GAMMA-AMINOBUTYRIC ACID activity. 7-Chloro-1,3-dihydro-1-methyl-5-phenyl-2H-1,4-benzodiazepin-2-one,Apaurin,Diazemuls,Faustan,Relanium,Seduxen,Sibazon,Stesolid,Valium
D004187 Disaccharides Oligosaccharides containing two monosaccharide units linked by a glycosidic bond. Disaccharide
D005260 Female Females
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D000871 Anthelmintics Agents that kill parasitic worms. They are used therapeutically in the treatment of HELMINTHIASIS in man and animal. Anthelmintic,Antihelmintic,Vermifuge,Vermifuges,Antihelmintics
D001665 Binding Sites The parts of a macromolecule that directly participate in its specific combination with another molecule. Combining Site,Binding Site,Combining Sites,Site, Binding,Site, Combining,Sites, Binding,Sites, Combining
D013570 Synaptic Membranes Cell membranes associated with synapses. Both presynaptic and postsynaptic membranes are included along with their integral or tightly associated specializations for the release or reception of transmitters. Membrane, Synaptic,Membranes, Synaptic,Synaptic Membrane

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