Angiostrongylus cantonensis: paralysis due to avermectin B1a and ivermectin. 1984

M Terada, and A I Ishii, and H Kino, and M Sano

Paralysis due to avermectin B1a and ivermectin of Angiostrongylus cantonensis was compared to that of phenylephrine (an alpha-adrenergic agonist) and strychnine (a cholinergic inhibitor). The paralyzing action of ivermectin (2.5 X 10(-9) g/ml) was inhibited by the single, simultaneous addition of picrotoxin (3 X 10(-5) M), whereas the effect of the drug (2.5 X 10(-7) g/ml) was reversed only when picrotoxin was given with cholinergic spasmogens such as pyrantel and eserine. Bicuculline (3 X 10(-5) M) had a similar antagonistic effect for picrotoxin, but bicuculline was less effective. The paralyzing action of avermectin B1a (3.6 X 10(-14) M, 3.0 X 10(-14) g/ml) was antagonized only when picrotoxin was given with cholinergic spasmogens such as pyrantel, eserine, and N-methylcytisine (N-MC), or alpha-adrenergic antagonists such as phentolamine and dibenamine. On the other hand, the paralyzing action of strychnine (3 X 10(-6) M) or phenylephrine (3 X 10(-5) M) was relatively uninfluenced by picrotoxin, but was antagonized by pyrantel and N-MC or dibenamine. These results suggest that a gabergic mechanism is involved in the paralyzing action of ivermectin, as well as avermectin B1a, in A. cantonensis.

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
D008681 Metastrongyloidea A superfamily of nematodes of the order STRONGYLIDA. Characteristics include a fluid-filled outer layer of cuticle and a reduced mouth and bursa. Metastrongyloideas
D009068 Movement The act, process, or result of passing from one place or position to another. It differs from LOCOMOTION in that locomotion is restricted to the passing of the whole body from one place to another, while movement encompasses both locomotion but also a change of the position of the whole body or any of its parts. Movement may be used with reference to humans, vertebrate and invertebrate animals, and microorganisms. Differentiate also from MOTOR ACTIVITY, movement associated with behavior. Movements
D009119 Muscle Contraction A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments. Inotropism,Muscular Contraction,Contraction, Muscle,Contraction, Muscular,Contractions, Muscle,Contractions, Muscular,Inotropisms,Muscle Contractions,Muscular Contractions
D010656 Phenylephrine An alpha-1 adrenergic agonist used as a mydriatic, nasal decongestant, and cardiotonic agent. (R)-3-Hydroxy-alpha-((methylamino)methyl)benzenemethanol,Metaoxedrin,Metasympatol,Mezaton,Neo-Synephrine,Neosynephrine,Phenylephrine Hydrochloride,Phenylephrine Tannate,Neo Synephrine,Tannate, Phenylephrine
D010830 Physostigmine A cholinesterase inhibitor that is rapidly absorbed through membranes. It can be applied topically to the conjunctiva. It also can cross the blood-brain barrier and is used when central nervous system effects are desired, as in the treatment of severe anticholinergic toxicity. Eserine
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
D011715 Pyrantel A depolarizing neuromuscular-blocking agent, that causes persistent nicotinic activation resulting in spastic paralysis of susceptible nematodes. It is a drug of second-choice after benzimidazoles for treatment of ascariasis, hookworm, and pinworm infections, being effective after a single dose. (From Smith and Reynard, Textbook of Pharmacology, 1992, p920)
D011807 Quinolizines

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