Apholate

In high-dose animal studies, causes hepatitis and kidney injury; Causes ataxia and paralysis in birds; [RTECS] Mechanism appears to be as alkylating agent on genetic material; Causes marked leukopenia in mammals within 24 hours of injection; Mutagenic in Neurospora crassa; [HSDB]

Apholate

Group 3: Not classifiable as to its carcinogenicity to humans

Volume 9: (1975) Some Aziridines, N-, S- and O-Mustards and Selenium

1987

1987

SIXTY WEANLING MALE & FEMALE FISCHER RATS RECEIVED APHOLATE IN STEROID-SUSPENDING VEHICLE, BY GAVAGE, ON 5 DAYS/WK IN DAILY DOSES/ANIMAL OF 0.003-0.1 MG (12 MALES & 12 FEMALES), 0.3 MG (15 MALES & 15 FEMALES) OR 1 MG (MAX TOLERATED DOSE, GIVEN TO 3 MALES & 3 FEMALES) FOR UP TO 1 YR. AVG SURVIVAL TIMES RANGED FROM 340 DAYS IN MALES GIVEN THE HIGHEST DOSE TO 565 DAYS IN FEMALES GIVEN THE LOWEST DOSE. THE TUMOR INCIDENCE WAS REPORTED TO BE SIMILAR TO THAT IN CONTROLS; NO TUMORS WERE REPORTED TO HAVE OCCURRED IN ANIMALS GIVEN THE HIGHEST DOSE LEVEL. (THE SMALL NUMBER OF ANIMALS USED SHOULD BE NOTED).

THE LD50 BY SKIN APPLICATION WAS 400-800 MG/KG FOR RATS OF BOTH SEXES.

TREATMENT OF NEUROSPORA CONIDIA WITH APHOLATE INDUCED AN INCR IN THE FREQUENCY OF RECESSIVE LETHAL MUTATIONS. AFTER IP INJECTION OF 1.5 MG/KG BODY WT APHOLATE IN MICE, A PEAK OF CHROMOSOME & CHROMATID ABERRATIONS WAS FOUND IN THE BONE MARROW 24 HR LATER.

Used as an insect chemosterilant (prevents reproduction in certain insects); [HSDB]

Farming (Pesticides) [Category: Industry]

EXPTL INSECT CHEMOSTERILANT

...BY ADDN OF AZIRIDINE TO 2,2,4,4,6,6-HEXACHLORO-2,2,4,4,5,5-HEXAHYDROTRIAZATRIPHOSPHORINE; HOWEVER, IT HAS BEEN PRODUCED FOR RESEARCH PURPOSES ONLY.

RATZ GRUNDMANN, US PATENT 2,858,306 (1958 TO OLIN MATHIESON).

WHEN A COLONY OF AEDES AEGYPTI WAS EXPOSED IN THE LARVAL STAGE TO THE CHEMOSTERILANT APHOLATE FOR GENERATION AFTER GENERATION, IT BECAME MORE TOLERANT TO THE STERILIZING EFFECT OF THE CHEMICAL.

APHOLATE HAS BEEN TESTED AS ANTINEOPLASTIC AGENT, BUT IT DOES NOT APPEAR TO HAVE BEEN USED FOR THIS PURPOSE IN HUMAN MEDICINE. IT HAS BEEN SHOWN TO BE AN EFFECTIVE CHEMOSTERILANT FOR VARIOUS INSECTS, BUT PROBLEMS ASSOC WITH ITS APPLICATION TO INSECTS, ITS TOXICITY & POSSIBLE ENVIRONMENTAL EFFECTS HAVE PREVENTED ITS USE IN THIS WAY ON A COMMERCIAL BASIS.

...EXPTL INSECT CHEMOSTERILANT ACTIVE AGAINST BOTH SEXES OF THE COMMON HOUSE FLY & OTHER ECONOMICALLY IMPORTANT SPECIES. ... HIGH TOXICITY LIMITS...PRESENT USE TO LAB IN WHICH STERILE POPULATIONS OF INSECTS ARE RAISED & RELEASED TO COMPETE FOR FERTILE MATES. SAID TO BE ALKYLATING AGENT WITH EFFECTS ON GENETIC MATERIAL SIMILAR TO IONIZING RADIATION.