Fananserin Explained

Fananserin (RP-62203) is a drug which acts as a potent antagonist at both the 5HT2A receptor,[1] and the Dopamine D4 receptor,[2] but without blocking other dopamine receptors such as D2.[3] It has sedative[4] and antipsychotic effects, and has been researched for the treatment of schizophrenia,[5] although efficacy was less than expected and results were disappointing.[6]

Notes and References

  1. Malleron JL, Comte MT, Gueremy C, Peyronel JF, Truchon A, Blanchard JC, Doble A, Piot O, Zundel JL, Huon C . 6 . Naphthosultam derivatives: a new class of potent and selective 5-HT2 antagonists . Journal of Medicinal Chemistry . 34 . 8 . 2477–83 . August 1991 . 1908521 . 10.1021/jm00112a025 .
  2. Heuillet E, Petitet F, Mignani S, Malleron JL, Lavayre J, Néliat G, Doble A, Blanchard JC . 6 . The naphtosultam derivative RP 62203 (fananserin) has high affinity for the dopamine D4 receptor . European Journal of Pharmacology . 314 . 1–2 . 229–33 . October 1996 . 8957240 . 10.1016/s0014-2999(96)00554-7 .
  3. Doble A, Girdlestone D, Piot O, Allam D, Betschart J, Boireau A, Dupuy A, Guérémy C, Ménager J, Zundel JL . 6 . Pharmacological characterization of RP 62203, a novel 5-hydroxytryptamine 5-HT2 receptor antagonist . British Journal of Pharmacology . 105 . 1 . 27–36 . January 1992 . 1596688 . 10.1111/j.1476-5381.1992.tb14206.x . 1908636 .
  4. Stutzmann JM, Eon B, Lucas M, Blanchard JC, Laduron PM . RP 62203, a 5-hydroxytryptamine2 antagonist, enhances deep NREM sleep in rats . Sleep . 15 . 2 . 119–24 . April 1992 . 1579785 . 10.1093/sleep/15.2.119 . free .
  5. Sramek JJ, Kirkesseli S, Paccaly-Moulin A, Davidson J, Jhee SS, Hourani J, Sémiond D, Cutler NR . 6 . A bridging study of fananserin in schizophrenic patients . Psychopharmacology Bulletin . 1998 . 34 . 4 . 811–8 . 10513457 .
  6. Truffinet P, Tamminga CA, Fabre LF, Meltzer HY, Rivière ME, Papillon-Downey C . Placebo-controlled study of the D4/5-HT2A antagonist fananserin in the treatment of schizophrenia . The American Journal of Psychiatry . 156 . 3 . 419–25 . March 1999 . 10080558 . 10.1176/ajp.156.3.419 . 41422352 .

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