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Effects of delta 9-tetrahydrocannabinol on glucagon receptor coupling to adenylate cyclase in rat liver plasma membranes.
Biochem Pharmacol. 1986 Aug 15; 35(16):2797-803.BP

Abstract

Delta-Tetrahydrocannabinol (delta 9-THC), the principal psychoactive constituent of Cannabis sativa, was found to increase glucagon activation of liver plasma membrane adenylate cyclase. In the presence of 30 microM delta 9-THC, the EC50 for glucagon was decreased by 60% from 7.6nM to 3.1 nM. 11-OH-delta 9-THC, a psychoactive metabolite of delta 9-THC, also increased glucagon activation of adenylate cyclase while two cannabinoids without marihuana-like psychoactive potency, cannabinol and cannabidiol, did not. At 30 microM, delta 9-THC either slightly decreased or had no effect on the activation of adenylate cyclase by GTP, Gpp(NH)p, fluoride ion, forskolin or ATP alone. Delta 9-THC had no effect on the binding of [125I] glucagon to liver plasma membranes. Arrhenius plots demonstrated that delta 9-THC and 11-OH-delta 9-THC, but not CBD, decreased the activation energy above the break temperature. Therefore, delta 9-THC increased the coupling of the glucagon receptor to adenylate cyclase apparently by removing a constraint on receptor-Ns coupling.

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Publisher Full Text

Authors

Hillard CJ
No affiliation info available
Bloom AS
No affiliation info available
Houslay MD
No affiliation info available

MeSH

Adenylyl CyclasesAnimalsCannabinoidsCell MembraneColforsinDronabinolGlucagonGuanosine TriphosphateGuanylyl ImidodiphosphateKineticsLiverMaleRatsRats, Inbred StrainsReceptors, Cell SurfaceReceptors, GlucagonSodium Fluoride

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't
Research Support, U.S. Gov't, P.H.S.

Language

eng

PubMed ID

3017362

Citation

Hillard, C J., et al. "Effects of Delta 9-tetrahydrocannabinol On Glucagon Receptor Coupling to Adenylate Cyclase in Rat Liver Plasma Membranes." Biochemical Pharmacology, vol. 35, no. 16, 1986, pp. 2797-803.
Hillard CJ, Bloom AS, Houslay MD. Effects of delta 9-tetrahydrocannabinol on glucagon receptor coupling to adenylate cyclase in rat liver plasma membranes. Biochem Pharmacol. 1986;35(16):2797-803.
Hillard, C. J., Bloom, A. S., & Houslay, M. D. (1986). Effects of delta 9-tetrahydrocannabinol on glucagon receptor coupling to adenylate cyclase in rat liver plasma membranes. Biochemical Pharmacology, 35(16), 2797-803.
Hillard CJ, Bloom AS, Houslay MD. Effects of Delta 9-tetrahydrocannabinol On Glucagon Receptor Coupling to Adenylate Cyclase in Rat Liver Plasma Membranes. Biochem Pharmacol. 1986 Aug 15;35(16):2797-803. PubMed PMID: 3017362.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Effects of delta 9-tetrahydrocannabinol on glucagon receptor coupling to adenylate cyclase in rat liver plasma membranes. AU - Hillard,C J, AU - Bloom,A S, AU - Houslay,M D, PY - 1986/8/15/pubmed PY - 1986/8/15/medline PY - 1986/8/15/entrez SP - 2797 EP - 803 JF - Biochemical pharmacology JO - Biochem Pharmacol VL - 35 IS - 16 N2 - Delta-Tetrahydrocannabinol (delta 9-THC), the principal psychoactive constituent of Cannabis sativa, was found to increase glucagon activation of liver plasma membrane adenylate cyclase. In the presence of 30 microM delta 9-THC, the EC50 for glucagon was decreased by 60% from 7.6nM to 3.1 nM. 11-OH-delta 9-THC, a psychoactive metabolite of delta 9-THC, also increased glucagon activation of adenylate cyclase while two cannabinoids without marihuana-like psychoactive potency, cannabinol and cannabidiol, did not. At 30 microM, delta 9-THC either slightly decreased or had no effect on the activation of adenylate cyclase by GTP, Gpp(NH)p, fluoride ion, forskolin or ATP alone. Delta 9-THC had no effect on the binding of [125I] glucagon to liver plasma membranes. Arrhenius plots demonstrated that delta 9-THC and 11-OH-delta 9-THC, but not CBD, decreased the activation energy above the break temperature. Therefore, delta 9-THC increased the coupling of the glucagon receptor to adenylate cyclase apparently by removing a constraint on receptor-Ns coupling. SN - 0006-2952 UR - https://www.unboundmedicine.com/medline/citation/3017362/Effects_of_delta_9_tetrahydrocannabinol_on_glucagon_receptor_coupling_to_adenylate_cyclase_in_rat_liver_plasma_membranes_ L2 - https://linkinghub.elsevier.com/retrieve/pii/0006-2952(86)90192-9 DB - PRIME DP - Unbound Medicine ER -