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The interaction of several beta-carbolines with specific [3H]-flunitrazepam binding to benzodiazepine receptors in rat brain membranes was investigated. Out of the investigated compounds, harmane and norharmane were the most potent inhibitors of specific [3H]-flunitrazepam binding, with IC50-values in the micromolar range. All other derivatives, including harmine, harmaline, and several tetrahydroderivatives were at least ten times less potent. Harmane has been previously found in rat brain and human urine, so it is the most potent endogenous inhibitor of specific [3H]-flunitrazepam binding known so far, with a several fold higher affinity for the benzodiazepine receptor than inosine and hypoxanthine. Thus, we suggest that harmane or other related beta-carbolines could be potential candidates as endogenous ligands of the benzodiazepine receptor.
H Rommelspacher, and
C Nanz, and
H O Borbe, and
K J Fehske, and
W E Müller, and
U Wollert
April 1982,
Brain research,
H Rommelspacher, and
C Nanz, and
H O Borbe, and
K J Fehske, and
W E Müller, and
U Wollert
August 1984,
No to shinkei = Brain and nerve,
H Rommelspacher, and
C Nanz, and
H O Borbe, and
K J Fehske, and
W E Müller, and
U Wollert
January 1986,
Advances in biochemical psychopharmacology,
H Rommelspacher, and
C Nanz, and
H O Borbe, and
K J Fehske, and
W E Müller, and
U Wollert
September 1989,
Pharmacology, biochemistry, and behavior,
H Rommelspacher, and
C Nanz, and
H O Borbe, and
K J Fehske, and
W E Müller, and
U Wollert
July 1986,
Proceedings of the National Academy of Sciences of the United States of America,
H Rommelspacher, and
C Nanz, and
H O Borbe, and
K J Fehske, and
W E Müller, and
U Wollert
April 1993,
Pharmacology, biochemistry, and behavior,
H Rommelspacher, and
C Nanz, and
H O Borbe, and
K J Fehske, and
W E Müller, and
U Wollert
June 1988,
Pharmacology, biochemistry, and behavior,
H Rommelspacher, and
C Nanz, and
H O Borbe, and
K J Fehske, and
W E Müller, and
U Wollert
January 1986,
Advances in biochemical psychopharmacology,
H Rommelspacher, and
C Nanz, and
H O Borbe, and
K J Fehske, and
W E Müller, and
U Wollert
October 1984,
Brain research,
H Rommelspacher, and
C Nanz, and
H O Borbe, and
K J Fehske, and
W E Müller, and
U Wollert
July 1983,
Biulleten' eksperimental'noi biologii i meditsiny,
