Inhibition of high affinity choline uptake by N-allyl-3-quinuclidinol
The peripheral actions of N-allyl-3-quinuclidinol (N-Al-3-OHQ) on high affinity choline uptake (HAChU) on rat phrenic nerve diaphragm are described. Endplate regions (EPA) identified by the Koelle histochemical techniques for acetylcholinesterase, were dissected from adult rat hemidiaphragms and placed in cold Krebs solution (pH-7.35). All measurements of HAChU were at 37/sup 0/C in buffers containing tritium choline (5 ..mu..M 0.124 ..mu..C/mmole) at intervals of 1, 2, 4, 8, 15 and 30 min. Tissues were washed 3x, digested in 1N NaOH and counted for tritium in Chaikoff's solution. All data are expressed as pmole Ch/g wet weight. Comparison between EPA and non-EPA tissue demonstrate HAChU and slow choline diffusion, respectively. Steady state is observed in 15 min. N-Al-3-OHQ produces 15% inhibition at 5 x 10/sup -5/ M compared with 50% inhibition on brain synaptosomes. At 5 x 10/sup -4/ M N-Al-3-OHQ, 30% inhibition is observed. Attempts to deplete ACh by pre-stimulation with high K/sup +/-ion (25 mM) were unsuccessful; tissue /sup 3/H-choline uptake appeared to oscillate over a 30 min period.
- Research Organization:
- Temple Univ. School of Medicine, Philadelphia, PA
- OSTI ID:
- 5417954
- Report Number(s):
- CONF-8604222-; TRN: 86-030424
- Journal Information:
- Fed. Proc., Fed. Am. Soc. Exp. Biol.; (United States), Vol. 45:3; Conference: 70. annual meeting of the Federation of American Society for Experimental Biology, St. Louis, MO, USA, 13 Apr 1986
- Country of Publication:
- United States
- Language:
- English
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ACETATES
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CHOLINE
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AFFINITY
BRAIN
INHIBITION
NERVES
RATS
TRACER TECHNIQUES
TRITIUM COMPOUNDS
ALCOHOLS
AMINES
AMMONIUM COMPOUNDS
ANIMALS
BODY
CARBOXYLIC ACID SALTS
CENTRAL NERVOUS SYSTEM
DRUGS
HYDROXY COMPOUNDS
ISOTOPE APPLICATIONS
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LIPOTROPIC FACTORS
MAMMALS
NERVOUS SYSTEM
ORGANIC COMPOUNDS
ORGANS
QUATERNARY COMPOUNDS
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VERTEBRATES
550201* - Biochemistry- Tracer Techniques