Rapid desensitization and down-regulation of 5-HT2 receptors by DOM treatment.
J E Leysen, P F Janssen, C J Niemegeers
European Journal of Pharmacology April 12, 1989 DOI: 10.1016/0014-2999(89)90409-3 (opens in new tab)
Study at a glance
AI-extracted from the abstract| Characteristics | Animal experimental study Peer reviewed |
|---|---|
| Population | Rats |
| Dose | 2.5 mg/kg, s.c. |
| Measures | head twitch response, [3H]ketanserin binding (Bmax, KD) |
| Key findings | Repeated DOM administration in rats produced a near-maximal reduction in head twitch behavior (-70%) and in frontal cortex [3H]ketanserin binding Bmax (-41%), with receptors reappearing at half-lives of 5.5 to 3 days. The authors propose a refinement of receptor regulation theory in light of anomalous antagonist effects and regular agonist effects. |
Abstract
The regulation of the 5-HT2 receptor-mediated head twitch response and of 5-HT2 receptor binding in the frontal cortex was studied in rats treated repeatedly with the 5-HT2 agonist 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane (DOM) (2.5 mg/kg, s.c.). Four injections in 24 h produced a near maximal reduction in the behaviour (-70%) and in the Bmax for [3H]ketanserin binding (-41%). The KD values tended to increase slightly. 5-HT2 receptors reappeared, with half-lives of 5.5 to 3 days. In view of the reported anomalous 5-HT2 receptor regulation by antagonists and the regular regulation by agonists, we propose a refinement in the receptor regulation theory.
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