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Effects of AM1346, a high-affinity CB1 receptor selective

Effects of AM1346, a high-affinity CB1 receptor selective

  1. helikophis
    AM1346 is a cannabinoid receptor type 1 (CB1R) anandamide analog [alkoxyacid amide of N-eicosa-(5Z, 8Z, 11Z, 14Z)-tetraenylamine] with high affinity and selectivity for the CB1 vs. CB2 receptor [Ki (CB1) = 1.5 nmol/l; Ki (CB2) = 152 nmol/l]. The present study characterized the effects of AM1346 (5.6–18 mg/kg) and its interaction with the CB1R antagonist/inverse agonist SR141716 (1–5.6 mg/kg) on open-field behaviors of rats. AM1346 reduced ambulation (horizontal activity), rearing (vertical activity) and increased the degree of circling and the latency to leave the central area of the open-field arena. AM1346 also tended to reduce defecation and to increase vocalization in a dose-dependent manner. In pretreatment studies, SR141716 completely blocked the effects of AM1346 on circling and latency and partially antagonized the effects of 18 mg/kg AM1346 on ambulation and rearing. SR141716 also tended to decrease AM1346- induced vocalization in a dose-dependent manner. Earlier studies have shown that SR141716, given alone, can increase grooming behavior and, as well, produces dose-related increases in scratching. In the present studies, these effects were attenuated in a dose-related manner by AM1346. The present profile of behavioral effects for AM1346 is consistent with its designation as aCB1R agonist. When combined with drug discrimination data (surmountable antagonism of effects of SR141716 by D9-THC and AM1346 but not by methanandamide, i.e. AM356), these data indicate that the anandamide analog AM1346 may be more behaviorally similar to cannabinoids like D9-THC than to other anandamide-based molecules such as methanandamide.
    Behavioural Pharmacology 2007, 18:673–680