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SB 242084, a Selective and Brain Penetrant 5-HT2C Receptor Antagonist
5-HT2 receptor subtypes: a family re-united?
In vitro and in vivo profile of SB 206553, a potent 5‐HT2C/5‐HT2B receptor antagonist with anxiolytic‐like properties
The results suggest that SB 206553 is a potent mixed 5‐HT2C/5-HT2B receptor antagonist with selectivity over the 5‐ HT2A and all other sites studied and possesses anxiolytic‐like properties.
Pharmacological characterisation of the agonist radioligand binding site of 5-HT2A, 5-HT2B and 5-HT2C receptors
- A. R. Knight, Anil Misra, M. Bickerdike
- BiologyNaunyn-Schmiedeberg's Archives of Pharmacology
- 30 July 2004
The results indicate the importance of defining the selectivity of pharmacological tools, which may have been over-estimated in the past, and highlights the need to find more selective agonists to investigate 5-HT2 receptor pharmacology.
Preferential effects of the cannabinoid CB1 receptor antagonist, SR 141716, on food intake and body weight gain of obese (fa/fa) compared to lean Zucker rats
- S. Vickers, L. Webster, A. Wyatt, C. Dourish, G. Kennett
- Biology, MedicinePsychopharmacology
- 11 March 2003
It is indicated that chronic oral treatment with SR 141716 significantly reduces the food intake and body weight gain of obese and lean Zucker rats, an effect that is greater in obese animals and reversible upon drug withdrawal.
Modulation of 5-HT2A receptor-mediated head-twitch behaviour in the rat by 5-HT2C receptor agonists
The muscarinic receptor agonist xanomeline has an antipsychotic-like profile in the rat.
- K. Stanhope, N. Mirza, A. Wyatt
- Psychology, BiologyJournal of Pharmacology and Experimental…
- 1 November 2001
Xanomeline attenuated amphetamine-induced hyperactivity at doses that had no effect on spontaneous activity, possibly indicating a separation between attenuation of limbic hyperdopaminergic function and the induction of hypolocomotion.
Evidence that mCPP may have behavioural effects mediated by central 5‐HT1C receptors
As mianserin, cyproheptadine and mesulergine in the absence of mCPP did not increase locomotion but increased the number of feeding scores, the activation of 5‐HT1C‐receptors may be of physiological importance in the control of appetite.
Modulation of 5-HT(2A) receptor-mediated head-twitch behaviour in the rat by 5-HT(2C) receptor agonists.
The in vivo and in vitro data suggest that for some ligands, previous reports have overestimated their in vivo selectivity for the 5-HT(2C) receptor.