Antagonism of meta-chlorophenylpiperazine-induced inhibition of exploratory activity in an emergence procedure, the open field test, in rats

Ethopharmacological analysis of the unstable elevated exposed plus maze, a novel model of extreme anxiety: predictive validity and sensitivity to anxiogenic agents

“…social interaction test: Kennedy et al 1993;elevated plus-maze: Fone et al 1996; canopy stretched attend posture test: Grewal et al 1997). Correspondingly, Meert et al (1997) have found that mCPP treated animals appear to be generally aroused, as evidenced by a doserelated increase in plasma prolactin and ACTH levels, in spite of a decrement in locomotor performance.…”

In vivo Schild regression analyses using nonselective 5-HT2C receptor antagonists in a rat operant behavioral assay

“…The agonists MK212 and mCPP are pharmacological tools that possess nanomolar affinity for 5-HT 2C receptors and approximately five-to 16-fold selectivity for 5-HT 2C receptors over other 5-HT receptors (Hoyer 1988b;Kennett et al 1994a;Porter et al 1999). MK212 is a full agonist, and mCPP is a partial agonist at 5-HT 2C receptors in behavioral assays, and both MK212 and mCPP are used frequently to investigate the functional consequence of the 5-HT 2C receptor activation (Cunningham et al 1986;Fiorella et al 1995a, b;Kennett and Curzon 1988;McCreary et al 2003;Meert et al 1997). Therefore, to further characterize the receptor pharmacology of MK212 and mCPP in rats, the nonselective 5-HT 2C receptor antagonists, metergoline, mianserin, methysergide, cyproheptadine and BOL, the 5HT 2A/2C receptor antagonist ketanserin, the 5HT 2B receptor antagonist SB 204,741, the 5HT 2B/2C receptor antagonist SB 200,646, and the peripherally acting 5-HT 2C receptor antagonist RS102221 were evaluated for their capacity to competitively antagonize MK212 and mCPP in a schedule-controlled responding assay.…”

“…These studies will provide a comparison to the 5-HT 2C receptor antagonist potencies reported in previous studies. Indeed, a characteristic of the 5-HT 2C receptor agonists such as mCPP is a pronounced inhibitory influence on locomotor function, which is blocked by antagonists with an affinity for 5-HT 2C receptors such as SB 200,646, mianserin, and methysergide (Kennett et al 1994b;Meert et al 1997). The characterization of the unique behavioral interaction of drugs with 5HT 2C receptors is a crucial element in the understanding of their pharmacological actions.…”

Synthesis of 2-N,N-Dimethylaminomethyl-2,3,3a,12b-tetrahydrodibenzo-[b,f]furo[2,3-d]oxepin Derivatives as Potential Anxiolytic Agents

“…[6][7][8][9][10][11][12] One enantiomer within this isoxazolidine series, R107500, was selected for clinical evaluation as an anxiolytic agent.…”

“…[1][2][3][4][5] Some of those tetracyclic isoxazolidines/tetrahydrofurans were potent mCPP (m-chlorophenylpiperazine) antagonists as shown in our in vivo mCPP challenge test, [3][4][5] and therefore could be considered as potential anxiolytic/antidepressants. [6][7][8][9][10][11][12] One enantiomer within this isoxazolidine series, R107500, was selected for clinical evaluation as an anxiolytic agent.…”