PMID- 2444852
OWN - NLM
STAT- MEDLINE
DCOM- 19871211
LR  - 20190701
IS  - 0024-3205 (Print)
IS  - 0024-3205 (Linking)
VI  - 41
IP  - 19
DP  - 1987 Nov 9
TI  - Action of tremorgenic mycotoxins on GABAA receptor.
PG  - 2207-14
AB  - The effects of four tremorgenic and one nontremorgenic mycotoxins were studied on 
      gamma-aminobutyric acid (GABAA) receptor binding and function in rat brain and on 
      binding of a voltage-operated Cl- channel in Torpedo electric organ. None of the 
      mycotoxins had significant effect on [3H]muscimol or [3H]flunitrazepam binding to 
      the GABAA receptor. However, only the four tremorgenic mycotoxins inhibited 
      GABA-induced 36Cl- influx and [35S] t-butylbicyclophosphorothionate [( 35S]TBPS) 
      binding in rat brain membranes, while the nontremorgenic verruculotoxin had no 
      effect. Inhibition of [35S]TBPS binding by paspalinine was non-competitive. This 
      suggests that tremorgenic mycotoxins inhibit GABAA receptor function by binding 
      close to the receptor's Cl- channel. On the voltage-operated Cl- channel, only 
      high concentrations of verruculogen and verruculotoxin caused significant 
      inhibition of the channel's binding of [35S]TBPS. The data suggest that the 
      tremorgenic action of these mycotoxins may be due in part to their inhibition of 
      GABAA receptor function.
FAU - Gant, D B
AU  - Gant DB
AD  - Department of Pharmacology & Experimental Therapeutics, University of Maryland 
      School of Medicine, Baltimore 21201.
FAU - Cole, R J
AU  - Cole RJ
FAU - Valdes, J J
AU  - Valdes JJ
FAU - Eldefrawi, M E
AU  - Eldefrawi ME
FAU - Eldefrawi, A T
AU  - Eldefrawi AT
LA  - eng
GR  - ES 02594/ES/NIEHS NIH HHS/United States
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PT  - Research Support, U.S. Gov't, P.H.S.
PL  - Netherlands
TA  - Life Sci
JT  - Life sciences
JID - 0375521
RN  - 0 (Bridged Bicyclo Compounds)
RN  - 0 (Bridged Bicyclo Compounds, Heterocyclic)
RN  - 0 (Chlorides)
RN  - 0 (Ion Channels)
RN  - 0 (Mycotoxins)
RN  - 0 (Receptors, GABA-A)
RN  - 2763-96-4 (Muscimol)
RN  - 620X0222FQ (Flunitrazepam)
RN  - 70636-86-1 (tert-butylbicyclophosphorothionate)
SB  - IM
MH  - Animals
MH  - Brain/drug effects
MH  - Bridged Bicyclo Compounds/metabolism
MH  - *Bridged Bicyclo Compounds, Heterocyclic
MH  - Chlorides/metabolism
MH  - Electric Organ/metabolism
MH  - Flunitrazepam/metabolism
MH  - In Vitro Techniques
MH  - Ion Channels/metabolism
MH  - Male
MH  - Muscimol/metabolism
MH  - Mycotoxins/*pharmacology
MH  - Rats
MH  - Rats, Inbred Strains
MH  - Receptors, GABA-A/*drug effects/metabolism
MH  - Torpedo
MH  - Tremor/*chemically induced
EDAT- 1987/11/09 00:00
MHDA- 1987/11/09 00:01
CRDT- 1987/11/09 00:00
PHST- 1987/11/09 00:00 [pubmed]
PHST- 1987/11/09 00:01 [medline]
PHST- 1987/11/09 00:00 [entrez]
AID - 0024-3205(87)90517-0 [pii]
AID - 10.1016/0024-3205(87)90517-0 [doi]
PST - ppublish
SO  - Life Sci. 1987 Nov 9;41(19):2207-14. doi: 10.1016/0024-3205(87)90517-0.