PMID- 30820175
OWN - NLM
STAT- PubMed-not-MEDLINE
LR  - 20201001
IS  - 1348-589X (Print)
IS  - 1349-0923 (Electronic)
IS  - 1348-589X (Linking)
VI  - 44
IP  - 1
DP  - 2019 Feb 20
TI  - Studies on the metabolism, mode of action, and development of insecticides acting 
      on the GABA receptor.
PG  - 71-86
LID - 10.1584/jpestics.J18-04 [doi]
AB  - gamma-BHC and dieldrin are legacy insecticides that were extensively used after the 
      second World War. When they were banned, their modes of action and metabolism 
      were not known. This article aims at providing a picture of the metabolism of 
      gamma-BHC and the modes of action of gamma -BHC and dieldrin. gamma-BHC is metabolized via 
      two independent metabolic pathways. One is a glutathione conjugation pathway 
      resulting in the formation of dichlorophenyl mercapturic acid and the other is an 
      oxidative metabolism catalyzed by microsomes to mainly 2,4,6-trichlorophenol 
      (TCP) and (36/45)-1,2,3,4,5,6-hexachlorocyclohex-1-ene (HCCHE). Other metabolites 
      of this pathway are 2,4,5-TCP, 2,3,4,6-tetrachlorophenol (TeCP), (36/45)- and 
      (346/5)-1,3,4,5,6-pentachlorocyclohex-1-enes (PCCHE). Nowadays, gamma-BHC and 
      dieldrin are very important reagents which are used to study the GABA receptor in 
      insects and mammals. They were found to be noncompetitive GABA antagonists 
      blocking the chloride ion selective pores in the GABA-gated chloride channels and 
      leading to inhibition of chloride ion conductance. [(3)H]EBOB binding data showed 
      that gamma-BHC, its analogs, dieldrin, and other cyclodiene insecticides interact 
      with the same site on GABA receptor as picrotoxinin. Only gamma-BHC, among other BHC 
      isomers, exhibits this binding characteristic. Milbemycin, currently widely used 
      as an insecticide, acaricide and nematicide, has been found to open the 
      GABA-gated chloride channel.
FAU - Tanaka, Keiji
AU  - Tanaka K
AD  - Kindai University, Faculty of Agriculture, Naka-machi, Nara, Nara 631-8505, 
      Japan.
LA  - eng
PT  - Journal Article
PL  - Japan
TA  - J Pestic Sci
JT  - Journal of pesticide science
JID - 101580833
PMC - PMC6389834
OTO - NOTNLM
OT  - GABA receptor chloride ion channel
OT  - deuterium isotope effect
OT  - dieldrin
OT  - milbemycin
OT  - picrotoxinin
OT  - gamma-BHC
EDAT- 2019/03/02 06:00
MHDA- 2019/03/02 06:01
PMCR- 2019/02/20
CRDT- 2019/03/02 06:00
PHST- 2019/03/02 06:00 [entrez]
PHST- 2019/03/02 06:00 [pubmed]
PHST- 2019/03/02 06:01 [medline]
PHST- 2019/02/20 00:00 [pmc-release]
AID - 10.1584/jpestics.J18-04 [doi]
PST - ppublish
SO  - J Pestic Sci. 2019 Feb 20;44(1):71-86. doi: 10.1584/jpestics.J18-04.