PMID: 36461Apr 1, 1979

The non-specific membrane binding properties of delta9-tetrahydrocannabinol and the effects of various solubilizers

The Journal of Pharmacy and Pharmacology
S Roth, P J Williams

Abstract

The binding of [3H]delta9-tetrahydrocannabinol to crude and purified synaptosomal membrane suspended in either Krebs solution or 10 mM sodium phosphate buffer was examined. The membrane/buffer partition coefficient was found to be 12,500, and was constant over a free concentration range of 10(-8) to 10(-6)M. Binding was similar in both suspending media, and to both crude and purified synaptosomal membrane. The solubilizing agent Cremophor E.L. (8 microgram ml-1) decreased the partition coefficient by one-half, and by greater than 99% at 0.4 mg ml-1. Similar effects were observed with Tween 80, while ethanol caused a maximum decrease of 60%. Membrane concentrations of THC were calculated at various effective concentrations reported in the literature, and were within the range predicted by the Meyer-Overton rule of anaesthesia. An apparent non-specific interaction with neuronal membranes and effective membrane concentrations of the order 2 x 10(-4) to 1 x 10(-2) mol kg-1 suggests THC may exert some of its effects by a mechanism analogous to the general anaesthetics, and thus may be classified as a partial anaesthetic.

References

Jan 1, 1975·Annual Review of Pharmacology·W D Paton
Jun 1, 1976·Biochemical Pharmacology·D BachR Goldman
Oct 1, 1975·Canadian Journal of Physiology and Pharmacology·J Acosta-Urquidi, R Chase
May 1, 1976·Journal of Medicinal Chemistry·A LeoP Y Jow
Feb 26, 1974·Biochimica Et Biophysica Acta·E Alhanaty, A Livne
Dec 1, 1972·Canadian Journal of Physiology and Pharmacology·P SeemanS Moyyen
Jul 1, 1974·Journal of Pharmaceutical Sciences·E R Garrett, C A Hunt
Jan 17, 1972·Biochimica Et Biophysica Acta·H MachleidtP Seeman
May 1, 1972·Biochemical Pharmacology·J M Mahoney, R A Harris
Jun 1, 1972·Canadian Journal of Biochemistry·A Jakubovic, P L McGeer
Jun 30, 1971·Nature: New Biology·S Roth, P Seeman
Feb 2, 1971·Biochimica Et Biophysica Acta·P SeemanH Schneider
Feb 1, 1971·British Journal of Pharmacology·J M Layman, A S Milton
Feb 1, 1964·The Biochemical Journal·V P WhittakerR J Kirkland

Related Concepts

Brain
Tissue Membrane
Solvents
Synaptosomes
Tetrahydrocannabinol, Trans-(+-)-Isomer

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