CGP-39551 explained

CGP-39551 is a drug used in scientific research, it is investigated as an anti-convulsant.^[1]

Mechanism of action

CGP-39551 and some related molecules are competitive antagonists of the N-methyl D-aspartate receptor, an excitatory receptor activated by glutamate.^{[2] [3]}

Potential

As other glutamate antagonists, CGP-39551 possesses anti-convulsant properties. It is able to suppress seizures caused by electroshock, with a duration of action superior to 24 hours.^[4]

It has also been shown to be able to block convulsions caused by vestibular stimulation.^[5]

Additionally, CGP-39551 appears to be better than some other NMDA blockers in terms of side effects, since the dose required for its anti-convulsant action does not have significant impact on memory and learning, unlike certain drugs with a similar mechanism of action such as Dizocilpine.^[6]

Notes and References

1. Web site: CGP 39551 NMDA Receptor Antagonist .
2. Fagg . G. E. . Olpe . H. R. . Pozza . M. F. . Baud . J. . Steinmann . M. . Schmutz . M. . Portet . C. . Baumann . P. . Thedinga . K. . Bittiger . H. . April 1990 . CGP 37849 and CGP 39551: novel and potent competitive N-methyl-D-aspartate receptor antagonists with oral activity . British Journal of Pharmacology . 99 . 4 . 791–797 . 10.1111/j.1476-5381.1990.tb13008.x . 0007-1188 . 1917531 . 1972895.
3. Pozza . M. F. . Olpe . H. R. . Brugger . F. . Fagg . G. E. . 1990-06-21 . Electrophysiological characterization of a novel potent and orally active NMDA receptor antagonist: CGP 37849 and its ethylester CGP 39551 . European Journal of Pharmacology . 182 . 1 . 91–100 . 10.1016/0014-2999(90)90496-s . 0014-2999 . 1976098.
4. Schmutz . M. . Portet . C. . Jeker . A. . Klebs . K. . Vassout . A. . Allgeier . H. . Heckendorn . R. . Fagg . G. E. . Olpe . H. R. . van Riezen . H. . July 1990 . The competitive NMDA receptor antagonists CGP 37849 and CGP 39551 are potent, orally-active anticonvulsants in rodents . Naunyn-Schmiedeberg's Archives of Pharmacology . 342 . 1 . 61–66 . 10.1007/BF00178973 . 0028-1298 . 1976233.
5. D'Hooge . R. . Raes . A. . Hiramatsu . M. . Mori . A. . Van Bogaert . P. P. . De Deyn . P. P. . December 1998 . Effects of the competitive N-methyl-D-aspartate antagonist CGP 37849 and its ethylester CGP 39551 on N-methyl-D-aspartate-evoked whole-cell currents in cultured spinal neurones and on vestibular stimulation-induced seizures in EL mice . Arzneimittel-Forschung . 48 . 12 . 1121–1125 . 0004-4172 . 9893924.
6. Bischoff . C. . Tiedtke . P. I. . 1992-03-24 . Competitive and non-competitive NMDA receptor antagonists in spatial learning tasks . European Journal of Pharmacology . 213 . 2 . 269–273 . 10.1016/0014-2999(92)90691-v . 0014-2999 . 1355738.