Abstract
The pharmacology of 3-(2-ethylmorpholino)-5,5′-di( p-bromophenyl)-imidazolidinedione (DML20), 3-(1-hydroxypropyl)-5,5′-di( p-bromophenyl)-imidazolidinedione (DML21) and 3-heptyl-5,5′-di( p-bromophenyl)-imidazolidinedione (DML23) was extended by studying affinity and GTP binding modulation on cannabinoid receptor subtypes (CB 1 and CB 2) from rat tissues and human cannabinoid receptors expressed in Chinese Hamster Ovary cells. Competitive binding studies indicated that DML20, DML21 and DML23 are selective ligands for cannabinoid CB 1 receptors. In rat cerebellum homogenates, DML20, DML21 and DML23 were unable to influence [ 35S]GTPγS binding but competitively inhibit HU 210-induced [ 35S]GTPγS binding (p K B of 6.11±0.14, 6.25±0.06 and 5.74±0.09, respectively), indicating that they act as cannabinoid CB 1 receptor neutral antagonists. However, in CHO cells homogenates expressing selectively either human cannabinoid CB 1 or CB 2 receptors, they behaved as inverse agonists decreasing the [ 35S]GTPγS binding, with similar efficacy. In conclusion, these derivatives exhibit different activities (neutral antagonism and inverse agonism) in the different models of cannabinoid receptors studied.
Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
