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Effects of the CB1R agonist WIN-55,212-2 and the CB1R antagonists SR-141716 and AM-1387: open-field examination in rats.
Pharmacol Biochem Behav. 2006 Sep; 85(1):243-52.PB

Abstract

This study examined the open-field (O-F) effects in rats of the cannabinoid 1 receptor (CB1R) agonist WIN-55,212-2 (WIN; 1 to 5.6 mg/kg) and its interaction with the CB1R antagonist/inverse agonist SR-141716 (1 to 5.6 mg/kg). Additionally, separate studies examined the O-F effects of SR-141716 (1 to 10 mg/kg) and a newly synthesized CB1R selective antagonist/inverse agonist AM-1387 (3 and 10 mg/kg) when these ligands were administered alone. Both antagonists are characterized in vitro by decreased of GTPgammaS binding and increased cAMP accumulation (inverse agonism). WIN dose dependently reduced ambulation (horizontal activity) and rearing (vertical activity); SR-141716 completely (WIN 3 mg/kg) or partially (WIN 5.6 mg/kg) normalized these behaviors. WIN alone resulted in circling and in an increased latency to leave the start area of the O-F, effects blocked by all doses of SR-141716. Both the increased scratching and grooming, associated with SR-141716 administration, were attenuated but not abolished by WIN. SR-141716 alone tended to reduce ambulation (significant at 10 mg/kg) and rearing (non-significant), had no effect on latency, and increased scratching and grooming (both frequency and duration), at doses of 3 mg/kg and up. At the doses examined, AM-1387 had no effect on ambulation, rearing, latency but significantly increased scratching (10 mg/kg); there was also a trend for increased grooming (both frequency and duration). The O-F profile of WIN suggests more similarity with the effects of THC rather than methanandamide (and presumably also anandamide). Intrinsic activity (scratching and grooming) by SR-141716 was re-affirmed and seemed to be associated with administration of AM-1387 as well. AM-1387 was less potent than SR-141716.

Authors+Show Affiliations

Temple University, Department of Psychology, 265-67 Weiss Hall, Philadelphia, PA 19122, USA. t.jarbe@neu.eduNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, N.I.H., Extramural

Language

eng

PubMed ID

16996123

Citation

Järbe, T U C., et al. "Effects of the CB1R Agonist WIN-55,212-2 and the CB1R Antagonists SR-141716 and AM-1387: Open-field Examination in Rats." Pharmacology, Biochemistry, and Behavior, vol. 85, no. 1, 2006, pp. 243-52.
Järbe TU, Ross T, DiPatrizio NV, et al. Effects of the CB1R agonist WIN-55,212-2 and the CB1R antagonists SR-141716 and AM-1387: open-field examination in rats. Pharmacol Biochem Behav. 2006;85(1):243-52.
Järbe, T. U., Ross, T., DiPatrizio, N. V., Pandarinathan, L., & Makriyannis, A. (2006). Effects of the CB1R agonist WIN-55,212-2 and the CB1R antagonists SR-141716 and AM-1387: open-field examination in rats. Pharmacology, Biochemistry, and Behavior, 85(1), 243-52.
Järbe TU, et al. Effects of the CB1R Agonist WIN-55,212-2 and the CB1R Antagonists SR-141716 and AM-1387: Open-field Examination in Rats. Pharmacol Biochem Behav. 2006;85(1):243-52. PubMed PMID: 16996123.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Effects of the CB1R agonist WIN-55,212-2 and the CB1R antagonists SR-141716 and AM-1387: open-field examination in rats. AU - Järbe,T U C, AU - Ross,T, AU - DiPatrizio,N V, AU - Pandarinathan,L, AU - Makriyannis,A, Y1 - 2006/09/22/ PY - 2006/04/09/received PY - 2006/08/09/revised PY - 2006/08/09/accepted PY - 2006/9/26/pubmed PY - 2007/2/24/medline PY - 2006/9/26/entrez SP - 243 EP - 52 JF - Pharmacology, biochemistry, and behavior JO - Pharmacol Biochem Behav VL - 85 IS - 1 N2 - This study examined the open-field (O-F) effects in rats of the cannabinoid 1 receptor (CB1R) agonist WIN-55,212-2 (WIN; 1 to 5.6 mg/kg) and its interaction with the CB1R antagonist/inverse agonist SR-141716 (1 to 5.6 mg/kg). Additionally, separate studies examined the O-F effects of SR-141716 (1 to 10 mg/kg) and a newly synthesized CB1R selective antagonist/inverse agonist AM-1387 (3 and 10 mg/kg) when these ligands were administered alone. Both antagonists are characterized in vitro by decreased of GTPgammaS binding and increased cAMP accumulation (inverse agonism). WIN dose dependently reduced ambulation (horizontal activity) and rearing (vertical activity); SR-141716 completely (WIN 3 mg/kg) or partially (WIN 5.6 mg/kg) normalized these behaviors. WIN alone resulted in circling and in an increased latency to leave the start area of the O-F, effects blocked by all doses of SR-141716. Both the increased scratching and grooming, associated with SR-141716 administration, were attenuated but not abolished by WIN. SR-141716 alone tended to reduce ambulation (significant at 10 mg/kg) and rearing (non-significant), had no effect on latency, and increased scratching and grooming (both frequency and duration), at doses of 3 mg/kg and up. At the doses examined, AM-1387 had no effect on ambulation, rearing, latency but significantly increased scratching (10 mg/kg); there was also a trend for increased grooming (both frequency and duration). The O-F profile of WIN suggests more similarity with the effects of THC rather than methanandamide (and presumably also anandamide). Intrinsic activity (scratching and grooming) by SR-141716 was re-affirmed and seemed to be associated with administration of AM-1387 as well. AM-1387 was less potent than SR-141716. SN - 0091-3057 UR - https://www.unboundmedicine.com/medline/citation/16996123/Effects_of_the_CB1R_agonist_WIN_55212_2_and_the_CB1R_antagonists_SR_141716_and_AM_1387:_open_field_examination_in_rats_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0091-3057(06)00263-2 DB - PRIME DP - Unbound Medicine ER -