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Category:
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7TM Receptors 5-HT Receptors5-HT2 Receptors5-HT2A
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Cat.No.
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Product Name
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2645 |
Fananserin
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| Alternative name(s): |
RP
62203 |
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Price and Availability
Click here for full price details of
Fananserin
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Chemical Name:
2-[3-[4-(4-Fluorophenyl)-1-piperazinyl]propyl]-2H-napht
hyl[1,8-cd]isothiazole-1,1-dioxide |
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Biological Activity:
5-HT2A receptor antagonist that also
displays high affinity at D4 receptors (Ki values are
0.26, 2.93, 25, 38, 70 and 726 nM for 5-HT2A, D4, H1,
α1,
5-HT1A and D2 receptors respectively). Inhibits inositol
phosphate formation evoked by 5-HT in vitro (IC50 = 7.76 nM) and
antagonises mescaline-induced head twitches in vivo.
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Technical Data:
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Resources:
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Certificate of Analysis / MSDS:
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References:
Malleron et al
(1991) Naphthosultam derivatives: a new class of potent and selective 5-HT2
antagonists. J.Med.Chem. 34 2477. Doble et al
(1992) Pharmacological characterization of RP 62203, a novel
5-hydroxytryptamine 5-HT2 receptor antagonist. Br.J.Pharmacol. 105
27. Heuillet et al (1996) The naphtosultam derivative RP 62203
(fananserin) has high affinity for the dopamine D4 receptor. Eur.J.Pharmacol.
314 229.
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Keywords: Fananserin, 5-HT Receptors, 5-HT2A Antagonist. Also D4 Antagonist, RP 62203, Tocris Bioscience
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