Biomaterial Database

Avermectin B1a inhibits the binding of strychnine to the glycine receptor of rat spinal cord. 1982

D Graham, and F Pfeiffer, and H Betz

The anthelmintic drug, avermectin B1a, has been reported to interfere with gamma-aminobutyric acid-mediated chloride conductance. Also, enhancement of diazepam binding to mammalian brain membranes by avermectin B1a has led to the suggestion that avermectin B1a interacts with the 'benzodiazepine receptor-gamma-aminobutyric acid receptor-chloride ionophore' complex. Here we report an interaction of avermectin B1a with the glycine receptor. The binding of the glycine receptor antagonist, strychnine, to both membranes and solubilized receptor from rat spinal cord, was inhibited by avermectin B1a with Ki values of 1.3 microM and 3.6 microM, and Hill coefficients of 0.46 and 0.62, respectively.

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
D011956	Receptors, Cell Surface	Cell surface proteins that bind signalling molecules external to the cell with high affinity and convert this extracellular event into one or more intracellular signals that alter the behavior of the target cell (From Alberts, Molecular Biology of the Cell, 2nd ed, pp693-5). Cell surface receptors, unlike enzymes, do not chemically alter their ligands.	Cell Surface Receptor,Cell Surface Receptors,Hormone Receptors, Cell Surface,Receptors, Endogenous Substances,Cell Surface Hormone Receptors,Endogenous Substances Receptors,Receptor, Cell Surface,Surface Receptor, Cell
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
D013116	Spinal Cord	A cylindrical column of tissue that lies within the vertebral canal. It is composed of WHITE MATTER and GRAY MATTER.	Coccygeal Cord,Conus Medullaris,Conus Terminalis,Lumbar Cord,Medulla Spinalis,Myelon,Sacral Cord,Thoracic Cord,Coccygeal Cords,Conus Medullari,Conus Terminali,Cord, Coccygeal,Cord, Lumbar,Cord, Sacral,Cord, Spinal,Cord, Thoracic,Cords, Coccygeal,Cords, Lumbar,Cords, Sacral,Cords, Spinal,Cords, Thoracic,Lumbar Cords,Medulla Spinali,Medullari, Conus,Medullaris, Conus,Myelons,Sacral Cords,Spinal Cords,Spinali, Medulla,Spinalis, Medulla,Terminali, Conus,Terminalis, Conus,Thoracic Cords
D013331	Strychnine	An alkaloid found in the seeds of STRYCHNOS NUX-VOMICA. It is a competitive antagonist at glycine receptors and thus a convulsant. It has been used as an analeptic, in the treatment of nonketotic hyperglycinemia and sleep apnea, and as a rat poison.	Strychnine Nitrate,Nitrate, Strychnine
D051381	Rats	The common name for the genus Rattus.	Rattus,Rats, Laboratory,Rats, Norway,Rattus norvegicus,Laboratory Rat,Laboratory Rats,Norway Rat,Norway Rats,Rat,Rat, Laboratory,Rat, Norway,norvegicus, Rattus
D018009	Receptors, Glycine	Cell surface receptors that bind GLYCINE with high affinity and trigger intracellular changes which influence the behavior of cells. Glycine receptors in the CENTRAL NERVOUS SYSTEM have an intrinsic chloride channel. GlyA receptor is sensitive to STRYCHNINE and localized in the post-synaptic membrane of inhibitory glycinergic neurons. GlyB receptor is insensitive to strychnine and associated with the excitatory NMDA receptor.	Excitatory Glycine Receptors,GlyA Receptors,GlyB Receptors,Glycine A Receptors,Glycine B Receptors,Glycine Receptor alpha1,Glycine Receptors,Inhibitory Glycine Receptor,SIG Receptor,Strychnine-Insensitive Glycine Receptor,Strychnine-Sensitive Glycine Receptor,Glycine Receptor,Glycine Receptor, Inhibitory,Glycine Receptor, Strychnine-Insensitive,Glycine Receptor, Strychnine-Sensitive,Receptor, Glycine,Receptor, Inhibitory Glycine,Receptor, SIG,Receptor, Strychnine-Insensitive Glycine,Receptor, Strychnine-Sensitive Glycine,Receptors, GlyB,Strychnine Insensitive Glycine Receptor,Strychnine Sensitive Glycine Receptor