Some dipeptides reverse the inhibitory effect of GABA on /sup 35/S-TBPS binding
All known GABA-A receptor blocker reverse the inhibitory effect of GABA on /sup 35/S-t-butylphosphorothionate (TBPS) binding to rat brain membranes in vitro. This system has already been used to identify several novel GABA antagonists. The authors now report that 12 out of 52 dipeptides tested (all containing L-amino acids), at 1 mM, significantly reverse the inhibitory effect of 1 ..mu..M GABA, which inhibits specific /sup 35/S-TBPS binding about 60%. Most of the active dipeptides contain an aromatic and a basic amino acid. Tryptophan usually conferred greater activity than phe or tyr, while arg usually conferred greater activity than lys or his. Several larger peptides containing the HFRW sequence found in ACTH were also GABA antagonists; ACTH(1-24), ACTH(1-18), ACTH(1-13), ACTH(4-10) and ..gamma..-MSH while ACTH(11-24) was inactive. The excitatory effects of these later peptides may be in part due to blockade of GABA-A receptors.
- Research Organization:
- Nathan Kline Institute, Orangeburg, NY
- OSTI ID:
- 6023895
- Report Number(s):
- CONF-870644-; TRN: 87-034017
- Journal Information:
- Fed. Proc., Fed. Am. Soc. Exp. Biol.; (United States), Vol. 46:6; Conference: 78. annual meeting of the American Society of Biological Chemists conference, Philadelphia, PA, USA, 7 Jun 1987
- Country of Publication:
- United States
- Language:
- English
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AMINOBUTYRIC ACID
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THIONATES
BIOCHEMICAL REACTION KINETICS
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SULFUR 35
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AMINO ACIDS
AUTONOMIC NERVOUS SYSTEM AGENTS
BETA DECAY RADIOISOTOPES
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DAYS LIVING RADIOISOTOPES
DRUGS
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ORGANIC COMPOUNDS
ORGANIC SULFUR COMPOUNDS
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550201* - Biochemistry- Tracer Techniques