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Pharmacological and molecular characterization of a dorsal root ganglion cell line expressing cannabinoid CB(1) and CB(2) receptors.
Eur J Pharmacol. 2011 Jun 01; 659(2-3):161-8.EJ

Abstract

The behavioral effects evoked by cannabinoids are primarily mediated by the CB(1) and CB(2) cannabinoid receptor subtypes. In vitro pharmacology of cannabinoid receptors has been elucidated using recombinant expression systems expressing either CB(1) or CB(2) receptors, with limited characterization in native cell lines endogenously expressing both CB(1) and CB(2) receptors. In the current study, we report the molecular and pharmacological characterization of the F-11 cell line, a hybridoma of rat dorsal root ganglion neurons and mouse neuroblastoma (N18TG2) cells, reported to endogenously express both cannabinoid receptors. The present study revealed that both receptors are of mouse origin in F-11 cells, and describes the relative gene expression levels between the two receptors. Pharmacological characterization of the F-11 cell line using cannabinoid agonists and antagonists indicated that the functional responses to these cannabinoid ligands are mainly mediated by CB(1) receptors. The non-selective cannabinoid ligands CP 55,940 and WIN 55212-2 are potent agonists and their efficacies in adenylate cyclase and MAPK assays are inhibited by the CB(1) selective antagonist SR141716A (SR1), but not by the CB(2) selective antagonist SR144528 (SR2). The endocannabinoid ligand 2AG, although not active in adenylate cyclase assays, was a potent activator of MAPK signaling in F-11 cells. The analysis of CB(1) and CB(2) receptor gene expression and the characterization of cannabinoid receptor pharmacology in the F-11 cell line demonstrate that it can be used as a tool for interrogating the endogenous signal transduction of cannabinoid receptor subtypes.

Authors+Show Affiliations

Neurological Diseases Research, Global Pharmaceutical Research & Development, Abbott Laboratories, R47W, AP9A, 100 Abbott Park Road, Abbott Park, IL 60064, USA. yihong.fan@abbott.comNo 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

21458448

Citation

Fan, Yihong, et al. "Pharmacological and Molecular Characterization of a Dorsal Root Ganglion Cell Line Expressing Cannabinoid CB(1) and CB(2) Receptors." European Journal of Pharmacology, vol. 659, no. 2-3, 2011, pp. 161-8.
Fan Y, Hooker BA, Garrison TR, et al. Pharmacological and molecular characterization of a dorsal root ganglion cell line expressing cannabinoid CB(1) and CB(2) receptors. Eur J Pharmacol. 2011;659(2-3):161-8.
Fan, Y., Hooker, B. A., Garrison, T. R., El-Kouhen, O. F., Idler, K. B., Holley-Shanks, R. R., Meyer, M. D., & Yao, B. B. (2011). Pharmacological and molecular characterization of a dorsal root ganglion cell line expressing cannabinoid CB(1) and CB(2) receptors. European Journal of Pharmacology, 659(2-3), 161-8. https://doi.org/10.1016/j.ejphar.2011.03.020
Fan Y, et al. Pharmacological and Molecular Characterization of a Dorsal Root Ganglion Cell Line Expressing Cannabinoid CB(1) and CB(2) Receptors. Eur J Pharmacol. 2011 Jun 1;659(2-3):161-8. PubMed PMID: 21458448.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Pharmacological and molecular characterization of a dorsal root ganglion cell line expressing cannabinoid CB(1) and CB(2) receptors. AU - Fan,Yihong, AU - Hooker,Bradley A, AU - Garrison,Tiffany Runyan, AU - El-Kouhen,Odile F, AU - Idler,Kenneth B, AU - Holley-Shanks,Rhonda R, AU - Meyer,Michael D, AU - Yao,Betty Bei, Y1 - 2011/03/31/ PY - 2010/10/15/received PY - 2011/01/19/revised PY - 2011/03/08/accepted PY - 2011/4/5/entrez PY - 2011/4/5/pubmed PY - 2011/9/10/medline SP - 161 EP - 8 JF - European journal of pharmacology JO - Eur J Pharmacol VL - 659 IS - 2-3 N2 - The behavioral effects evoked by cannabinoids are primarily mediated by the CB(1) and CB(2) cannabinoid receptor subtypes. In vitro pharmacology of cannabinoid receptors has been elucidated using recombinant expression systems expressing either CB(1) or CB(2) receptors, with limited characterization in native cell lines endogenously expressing both CB(1) and CB(2) receptors. In the current study, we report the molecular and pharmacological characterization of the F-11 cell line, a hybridoma of rat dorsal root ganglion neurons and mouse neuroblastoma (N18TG2) cells, reported to endogenously express both cannabinoid receptors. The present study revealed that both receptors are of mouse origin in F-11 cells, and describes the relative gene expression levels between the two receptors. Pharmacological characterization of the F-11 cell line using cannabinoid agonists and antagonists indicated that the functional responses to these cannabinoid ligands are mainly mediated by CB(1) receptors. The non-selective cannabinoid ligands CP 55,940 and WIN 55212-2 are potent agonists and their efficacies in adenylate cyclase and MAPK assays are inhibited by the CB(1) selective antagonist SR141716A (SR1), but not by the CB(2) selective antagonist SR144528 (SR2). The endocannabinoid ligand 2AG, although not active in adenylate cyclase assays, was a potent activator of MAPK signaling in F-11 cells. The analysis of CB(1) and CB(2) receptor gene expression and the characterization of cannabinoid receptor pharmacology in the F-11 cell line demonstrate that it can be used as a tool for interrogating the endogenous signal transduction of cannabinoid receptor subtypes. SN - 1879-0712 UR - https://www.unboundmedicine.com/medline/citation/21458448/Pharmacological_and_molecular_characterization_of_a_dorsal_root_ganglion_cell_line_expressing_cannabinoid_CB_1__and_CB_2__receptors_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0014-2999(11)00292-5 DB - PRIME DP - Unbound Medicine ER -