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Quantification of anandamide and 2-arachidonoylglycerol plasma levels to examine potential influences of tetrahydrocannabinol application on the endocannabinoid system in humans.
Drug Test Anal. 2014 Jan-Feb; 6(1-2):17-23.DT

Abstract

The effects of tetrahydrocannabinol (THC) and endogenous cannabinoids (endocannabinoids, ECs) are both mediated by activation of the cannabinoid receptors CB1 and CB2. Exogenous activation of these receptors by THC could therefore alter EC levels. We tested this hypothesis in healthy volunteers (n = 25) who received a large intravenous dose of THC (0.10 mg/kg). Effects on the EC system were quantified by serial measurements of plasma ECs after THC administration. Eleven blood samples were drawn during the first 5 h after THC administration and two more samples after 24 and 48 h. THC, its metabolites THC-OH (biologically active) and THC-COOH (non-active), and the ECs anandamide and 2-arachidonoylglycerol (2-AG) were quantified by liquid chromatography-mass spectrometry. EC-plasma levels showed a biphasic response after THC injection reaching maximal values at 30 min. Anandamide increased slightly from 0.58 ± 0.21 ng/ml at baseline to 0.64 ± 0.24 ng/ml (p < 0.05) and 2-AG from 7.60 ± 4.30 ng/ml to 9.50 ± 5.90 ng/ml (p < 0.05). After reaching maximal concentrations, EC plasma levels decreased markedly to a nadir of 300 min after THC administration (to 0.32 ± 0.15 ng/ml for anandamide and to 5.50 ± 3.01 ng/ml for 2-AG, p < 0.05). EC plasma concentrations returned to near baseline levels until 48 h after the experiment. THC (0.76 ± 0.16 ng/ml) and THC-OH (0.36 ± 0.17 ng/ml) were still measurable at 24 h and remained detectible until 48 h after THC administration. Although the underlying mechanism is not clear, high doses of intravenous THC appear to influence endogenous cannabinoid concentrations and presumably EC-signalling.

Authors+Show Affiliations

Department of Anaesthesiology, Ludwig - Maximilians University of Munich, Germany.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

24424856

Citation

Thieme, Ulrike, et al. "Quantification of Anandamide and 2-arachidonoylglycerol Plasma Levels to Examine Potential Influences of Tetrahydrocannabinol Application On the Endocannabinoid System in Humans." Drug Testing and Analysis, vol. 6, no. 1-2, 2014, pp. 17-23.
Thieme U, Schelling G, Hauer D, et al. Quantification of anandamide and 2-arachidonoylglycerol plasma levels to examine potential influences of tetrahydrocannabinol application on the endocannabinoid system in humans. Drug Test Anal. 2014;6(1-2):17-23.
Thieme, U., Schelling, G., Hauer, D., Greif, R., Dame, T., Laubender, R. P., Bernhard, W., Thieme, D., Campolongo, P., & Theiler, L. (2014). Quantification of anandamide and 2-arachidonoylglycerol plasma levels to examine potential influences of tetrahydrocannabinol application on the endocannabinoid system in humans. Drug Testing and Analysis, 6(1-2), 17-23. https://doi.org/10.1002/dta.1561
Thieme U, et al. Quantification of Anandamide and 2-arachidonoylglycerol Plasma Levels to Examine Potential Influences of Tetrahydrocannabinol Application On the Endocannabinoid System in Humans. Drug Test Anal. 2014 Jan-Feb;6(1-2):17-23. PubMed PMID: 24424856.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Quantification of anandamide and 2-arachidonoylglycerol plasma levels to examine potential influences of tetrahydrocannabinol application on the endocannabinoid system in humans. AU - Thieme,Ulrike, AU - Schelling,Gustav, AU - Hauer,Daniela, AU - Greif,Robert, AU - Dame,Torsten, AU - Laubender,Ruediger Paul, AU - Bernhard,Werner, AU - Thieme,Detlef, AU - Campolongo,Patrizia, AU - Theiler,Lorenz, Y1 - 2013/10/28/ PY - 2013/05/24/received PY - 2013/08/28/revised PY - 2013/09/03/accepted PY - 2014/1/16/entrez PY - 2014/1/16/pubmed PY - 2014/9/16/medline KW - 2-Arachidonoylglycerol KW - Anandamide KW - Endocannabinoids KW - HPLC KW - Mass spectrometry KW - Plasma concentrations KW - Tetrahydrocannabinol SP - 17 EP - 23 JF - Drug testing and analysis JO - Drug Test Anal VL - 6 IS - 1-2 N2 - The effects of tetrahydrocannabinol (THC) and endogenous cannabinoids (endocannabinoids, ECs) are both mediated by activation of the cannabinoid receptors CB1 and CB2. Exogenous activation of these receptors by THC could therefore alter EC levels. We tested this hypothesis in healthy volunteers (n = 25) who received a large intravenous dose of THC (0.10 mg/kg). Effects on the EC system were quantified by serial measurements of plasma ECs after THC administration. Eleven blood samples were drawn during the first 5 h after THC administration and two more samples after 24 and 48 h. THC, its metabolites THC-OH (biologically active) and THC-COOH (non-active), and the ECs anandamide and 2-arachidonoylglycerol (2-AG) were quantified by liquid chromatography-mass spectrometry. EC-plasma levels showed a biphasic response after THC injection reaching maximal values at 30 min. Anandamide increased slightly from 0.58 ± 0.21 ng/ml at baseline to 0.64 ± 0.24 ng/ml (p < 0.05) and 2-AG from 7.60 ± 4.30 ng/ml to 9.50 ± 5.90 ng/ml (p < 0.05). After reaching maximal concentrations, EC plasma levels decreased markedly to a nadir of 300 min after THC administration (to 0.32 ± 0.15 ng/ml for anandamide and to 5.50 ± 3.01 ng/ml for 2-AG, p < 0.05). EC plasma concentrations returned to near baseline levels until 48 h after the experiment. THC (0.76 ± 0.16 ng/ml) and THC-OH (0.36 ± 0.17 ng/ml) were still measurable at 24 h and remained detectible until 48 h after THC administration. Although the underlying mechanism is not clear, high doses of intravenous THC appear to influence endogenous cannabinoid concentrations and presumably EC-signalling. SN - 1942-7611 UR - https://www.unboundmedicine.com/medline/citation/24424856/Quantification_of_anandamide_and_2_arachidonoylglycerol_plasma_levels_to_examine_potential_influences_of_tetrahydrocannabinol_application_on_the_endocannabinoid_system_in_humans_ DB - PRIME DP - Unbound Medicine ER -