Fananserin - CAS 127625-29-0
Category: Inhibitor
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5-HT Receptor | Dopamine Receptor
Fananserin is a 5-HT2A receptor and a dopamine D4 receptor antagonist (Ki = 0.26, 2.93, 25, 38, 70 and 726 nM for 5-HT2A, D4, H1, α1, 5-HT1A and D2 receptors, respectively). Fananserin inhibits 5-HT-induced inositol phosphate formation in vitro (IC50 = 7.76 nM), and antagonizes mescaline-induced head twitches in vivo.
Brife Description:
5-HT2A receptor antagonist, dopamine D4 receptor antagonist
≥99% by HPLC
Fananserin; RP 62203; RP-62203; RP62203; 2-[3-[4-(4-Fluorophenyl)-1-piperazinyl]propyl]-2H-naphthyl[1,8-cd]isothiazole-1,1-dioxide
Canonical SMILES:
1.Naphthosultam derivatives: a new class of potent and selective 5-HT2 antagonists.
Malleron JL;Comte MT;Gueremy C;Peyronel JF;Truchon A;Blanchard JC;Doble A;Piot O;Zundel JL;Huon C J Med Chem. 1991 Aug;34(8):2477-83.
A series of 2-(aminoalkyl)naphth[1,8-cd]isothiazole 1,1-dioxides was synthesized and examined in various receptor binding tests. Most compounds demonstrated high affinity for the 5-HT2 receptor with moderate to high selectivity. A member of this series, compound 24 (RP 62203), displays high 5-HT2 receptor affinity (Ki = 0.26 nM), which is respectively more than 100 and 1000 times higher than its affinity for alpha 1 (Ki = 38 nM) and D2 (Ki greater than 1000 nM) receptors. This compound is a potent orally effective and long lasting 5-HT2 antagonist in the mescaline-induced head-twitches test in mice and rats.
2.[35S]Guanosine-5'-O-(3-thio)triphosphate binding as a measure of efficacy at human recombinant dopamine D4.4 receptors: actions of antiparkinsonian and antipsychotic agents.
Newman-Tancredi A;Audinot V;Chaput C;Verrièle L;Millan MJ J Pharmacol Exp Ther. 1997 Jul;282(1):181-91.
Recombinant human dopamine D4.4 receptor-mediated G protein activation was characterized in membranes of transfected mammalian (Chinese hamster ovary) cells by the use of [35S]guanosine-5'-O-(3-thio)triphosphate ([35S]GTPgammaS) binding. An initial series of experiments defined the conditions (3 microM GDP, 100 mM NaCl, 3 mM MgCl2) under which optimal stimulation (2.2-fold increase in specific [35S]GTPgammaS binding) was achieved with the endogenous agonist dopamine. The number of dopamine-activated G proteins in Chinese hamster ovary-D4.4 membranes was determined through [35S]GTPgammaS isotopic dilution saturation binding, yielding a Bmax value of 2.29 pmol/mg. This compared with a D4.4 receptor Bmax value of 1.40 pmol/mg determined by [3H]spiperone saturation binding, indicating that 1 or 2 G proteins were activated per D4.4 receptor and that there were few or no "spare receptors" in this cell line. Under these conditions, the efficacy for stimulation of [35S]GTPgammaS binding at D4.4 receptors of 12 dopaminergic agonists was determined. Several antiparkinsonian drugs, including ropinirole, quinerolane and lisuride, exhibited agonist activity at D4.4 receptors (Emax = 74.3%, 72.4% and 32.
3.[3H]MDL 100,907 labels 5-HT2A serotonin receptors selectively in primate brain.
López-Giménez JF;Vilaró MT;Palacios JM;Mengod G Neuropharmacology. 1998 Sep;37(9):1147-58.
The selective antagonist for the 5-HT2A serotonin receptor MDL 100,907, recently characterized autoradiographically in rat brain, has been characterized as a radioligand for the visualization of this receptor in human and monkey brain. In both species [3H]MDL 100,907 binding to brain sections was saturable, had sub-nanomolar affinity (Kd = 0.14-0.19 nM in human brain; Kd= 0.16-0.19 nM in monkey brain) and presented a pharmacological profile consistent with its binding to 5-HT2A receptors (rank order of affinity for [3H]MDL 100,907-labeled receptors: MDL 100,907 > spiperone > ketanserin > mesulergine). The autoradiographical signal obtained with [3H]MDL 100,907 was compared to the signal obtained with [3H]ketanserin, [3H]RP62203 and [3H]mesulergine in both species, and to the distribution of 5-HT2A receptor mRNA as determined by in situ hybridization in monkey brain. At variance with the other radioligands, [3H]MDL 100,907 showed a single population of binding sites with extremely low levels of non-specific binding. As expected, mesulergine showed low affinity for [3H]MDL 100,907-labeled receptors and the autoradiographic pattern shown by [3H]mesulergine confirmed the lack of labeling of the 5-HT2A receptor by this radioligand in primate brain.
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CAS 127625-29-0 Fananserin

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