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| Item type: | Article | ||||
|---|---|---|---|---|---|
| Journal or Publication Title: | Neuroscience letters | ||||
| Publisher: | Elsevier | ||||
| Volume: | 447 | ||||
| Number of Issue or Book Chapter: | 1 | ||||
| Page Range: | pp. 68-72 | ||||
| Date: | 2008 | ||||
| Additional Information (public): | CAN 150:48318 2-5 Mammalian Hormones 9059-32-9 (GTPase) Role: BSU (Biological study, unclassified), BIOL (Biological study) (activity regulation; differential coupling of human cannabinoid receptors hCB1R and hCB2R to G-protein Galpha i2beta 1gamma 2 point to distinct functions in central nervous system); 146-91-8 (5'-GDP); 37589-80-3 (GTPgamma S) Role: BSU (Biological study, unclassified), BIOL (Biological study) (binding; differential coupling of human cannabinoid receptors hCB1R and hCB2R to G-protein Galpha i2beta 1gamma 2 point to distinct functions in central nervous system) | ||||
| Institutions: | Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical Biology (Prof. Heilmann) | ||||
| Projects (Historical): | GRK 760, Graduiertenkolleg Medizinische Chemie | ||||
| Identification Number: |
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| Keywords: | G proteins Role: BSU (Biological study, unclassified), BIOL (Biological study) (Gi2 (adenylate cyclase-inhibiting, 2), alpha subunit differential coupling of human cannabinoid receptors hCB1R and hCB2R to G-protein Galpha i2beta 1gamma 2 point to distinct functions in central nervous system) Central nervous system Human (differential coupling of human cannabinoid receptors hCB1R and hCB2R to G-protein Galpha i2beta 1gamma 2 point to distinct functions in central nervous system) Cannabinoid receptors Role: BSU (Biological study, unclassified), BIOL (Biological study) (type CB1 differential coupling of human cannabinoid receptors hCB1R and hCB2R to G-protein Galpha i2beta 1gamma 2 point to distinct functions in central nervous system) Cannabinoid receptors Role: BSU (Biological study, unclassified), BIOL (Biological study) (type CB2 differential coupling of human cannabinoid receptors hCB1R and hCB2R to G-protein Galpha i2beta 1gamma 2 point to distinct functions in central nervous system) G proteins Role: BSU (Biological study, unclassified), BIOL (Biological study) (beta 1gamma 2 subunits differential coupling of human cannabinoid receptors hCB1R and hCB2R to G-protein Galpha i2beta 1gamma 2 point to distinct functions in central nervous system) cannabinoid receptor CB1R CB2R Gi protein GTPase GDP GTP | ||||
| Dewey Decimal Classification: | 500 Science > 570 Life sciences 500 Science > 540 Chemistry & allied sciences | ||||
| Status: | Published | ||||
| Refereed: | Yes, this version has been refereed | ||||
| Created at the University of Regensburg: | Yes | ||||
| Item ID: | 17240 |
Abstract
Human cannabinoid receptors 1 (hCB1R) and 2 (hCB2R) are expressed in the CNS and couple to Gi/Go-proteins. The aim of this study was to compare coupling of hCB1R and hCB2R to Galpha i2beta 1gamma 2 in Sf9 insect cells. High-affinity agonist binding at hCB1R, but not at hCB2R, was resistant to guanine nucleotides. HCB1R activated Galpha i2beta 1gamma 2 much more rapidly than hCB2R in the ...
Abstract
Human cannabinoid receptors 1 (hCB1R) and 2 (hCB2R) are expressed in the CNS and couple to Gi/Go-proteins. The aim of this study was to compare coupling of hCB1R and hCB2R to Galpha i2beta 1gamma 2 in Sf9 insect cells. High-affinity agonist binding at hCB1R, but not at hCB2R, was resistant to guanine nucleotides. HCB1R activated Galpha i2beta 1gamma 2 much more rapidly than hCB2R in the [35S]guanosine 5'-[gamma -thio]triphosphate ([35S]GTPgamma S) binding assay. Moreover, hCB1R exhibited a higher constitutive activity than hCB2R as assessed by the relative inhibitory effects of inverse agonists on [35S]GTPgamma S binding and steady-state high-affinity GTPase activity compared to the stimulatory effects of the hCB1/2R agonist CP 55,940 [(-)-cis-3-[2-hydroxy-4-(1,1-dimethylheptyl)phenyl]-trans-4-(3-hydroxypropyl)cyclohexanol]. Galpha i2beta 1gamma 2 coupled to hCB2R exhibited higher GDP- and GTPgamma S-affinities than Galpha i2beta 1gamma 2 coupled to hCB1R. NaCl effectively reduced constitutive activity of hCB1R but not of hCB2R. Collectively, hCB1R and hCB2R couple differentially to Galpha i2beta 1gamma 2. Moreover, hCB1R exhibits higher constitutive activity than hCB2R. These differences point to distinct functions of hCB1R and hCB2R in the CNS.
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