Preliminary pharmacological investigation on 38 aminophosphonic acids and their derivatives.
Central pharmacological properties of 38 aminophosphonic acids and their derivatives, mostly newly synthesized, were investigated on mice and rats. Acute toxicity, neurotoxic activity, influence on spontaneous locomotor activity, body temperature, electrogenic and pentetrazol convulsions, on cerebral GABA level were tested. The most active compounds were (in a decreasing order of activity): 2-amino-7-phosphonoheptanoic, 2-amino-5-phosphonovaleric, 2-amino-8-phosphonooctanoic, 2-amino-2-methyl-3-methylphosphonopropionic, and 3-amino-3-hydroxy-5-phosphonovaleric acid.
D000596:Amino Acids / Q000494:pharmacology* / Q000633:toxicity; D000818:Animals; D000927:Anticonvulsants; D001522:Behavior, Animal / Q000187:drug effects*; D001831:Body Temperature / Q000187:drug effects; D001923:Brain Chemistry / Q000187:drug effects; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D051381:Rats; D011919:Rats, Inbred Strains; D016194:Receptors, N-Methyl-D-Aspartate; D017981:Receptors, Neurotransmitter / Q000187:drug effects*; D012640:Seizures / Q000517:prevention & control; D013045:Species Specificity; D005680:gamma-Aminobutyric Acid / Q000378:metabolism
D000596:Amino Acids; D000927:Anticonvulsants; D016194:Receptors, N-Methyl-D-Aspartate; D017981:Receptors, Neurotransmitter; D005680:gamma-Aminobutyric Acid