Comparison of bicyclic phosphorous esters with bicuculline and picrotoxin as antagonists of presynaptic inhibition in the rat cuneate nucleus. 1977

N Davidson, and E I Macfarlane, and D L Michie

The effects of 2 of a series of bicyclic phosphorous esters, the ethyl (EPTBO) and isopropyl (IPTBO) compounds, were compared with those of the GABA antagonists, picrotoxin and bicuculline, on presynaptic inhibition in the rat cunneate nucleus. Both EPTBO and IPTBO were found to be effective, reversible antagonists of presynaptic inhibition, with IPTBO approximately 10 times more potent than EPTBO and equipotent with bicuculline, EPTBO equipotent with picrotoxin.

UI MeSH Term Description Entries
D007546 Isoquinolines A group of compounds with the heterocyclic ring structure of benzo(c)pyridine. The ring structure is characteristic of the group of opium alkaloids such as papaverine. (From Stedman, 25th ed)
D008526 Medulla Oblongata The lower portion of the BRAIN STEM. It is inferior to the PONS and anterior to the CEREBELLUM. Medulla oblongata serves as a relay station between the brain and the spinal cord, and contains centers for regulating respiratory, vasomotor, cardiac, and reflex activities. Accessory Cuneate Nucleus,Ambiguous Nucleus,Arcuate Nucleus of the Medulla,Arcuate Nucleus-1,External Cuneate Nucleus,Lateral Cuneate Nucleus,Nucleus Ambiguus,Ambiguus, Nucleus,Arcuate Nucleus 1,Arcuate Nucleus-1s,Cuneate Nucleus, Accessory,Cuneate Nucleus, External,Cuneate Nucleus, Lateral,Medulla Oblongatas,Nucleus, Accessory Cuneate,Nucleus, Ambiguous,Nucleus, External Cuneate,Nucleus, Lateral Cuneate
D009943 Organophosphorus Compounds Organic compounds that contain phosphorus as an integral part of the molecule. Included under this heading is broad array of synthetic compounds that are used as PESTICIDES and DRUGS. Organophosphorus Compound,Organopyrophosphorus Compound,Organopyrophosphorus Compounds,Compound, Organophosphorus,Compound, Organopyrophosphorus,Compounds, Organophosphorus,Compounds, Organopyrophosphorus
D010852 Picrotoxin A mixture of PICROTOXININ and PICROTIN that is a noncompetitive antagonist at GABA-A receptors acting as a convulsant. Picrotoxin blocks the GAMMA-AMINOBUTYRIC ACID-activated chloride ionophore. Although it is most often used as a research tool, it has been used as a CNS stimulant and an antidote in poisoning by CNS depressants, especially the barbiturates. 3,6-Methano-8H-1,5,7-trioxacyclopenta(ij)cycloprop(a)azulene-4,8(3H)-dione, hexahydro-2a-hydroxy-9-(1-hydroxy-1-methylethyl)-8b-methyl-, (1aR-(1aalpha,2abeta,3beta,6beta,6abeta,8aS*,8bbeta,9S*))-, compd. with (1aR-(1aalpha,2abeta,3beta,6beta,6abeta,8,Cocculin
D001952 Bridged-Ring Compounds Cyclic hydrocarbons that contain multiple rings which share one or more bridgehead connections. Bridged Compounds,Bridged Ring Compounds
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
D001640 Bicuculline An isoquinoline alkaloid obtained from Dicentra cucullaria and other plants. It is a competitive antagonist for GABA-A receptors. 6-(5,6,7,8-Tetrahydro-6-methyl-1,3-dioxolo(4,5-g)isoquinolin-5-yl)furo(3,4-e)1,3-benzodioxol-8(6H)one
D001643 Bridged Bicyclo Compounds Saturated alicyclic hydrocarbon molecules consisting of two rings that have two non-adjacent atoms in common. Bicyclo Compounds,Bicyclo Compounds, Bridged
D013569 Synapses Specialized junctions at which a neuron communicates with a target cell. At classical synapses, a neuron's presynaptic terminal releases a chemical transmitter stored in synaptic vesicles which diffuses across a narrow synaptic cleft and activates receptors on the postsynaptic membrane of the target cell. The target may be a dendrite, cell body, or axon of another neuron, or a specialized region of a muscle or secretory cell. Neurons may also communicate via direct electrical coupling with ELECTRICAL SYNAPSES. Several other non-synaptic chemical or electric signal transmitting processes occur via extracellular mediated interactions. Synapse
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

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