(R)-3,N-Dimethyl-N-[1-methyl-3-(4-methylpiperidin-1-yl)propyl]benzenesulfonamide:  The First Selective 5-HT7 Receptor Antagonist

IT Forbes, S Dabbs, DM Duckworth… - Journal of medicinal …, 1998 - ACS Publications
5-HT1A< 5.1 5-HT2C< 4.8 5-HT1B< 5.3 5-HT4< 5.0 5-HT1D 5.5 5-HT6< 4.8 5-HT1E< 4.8 5-
HT7 7.5 (0.04 (n) 6) 5-HT1F< 5.2 adrenergic R1B< 4.8 5-HT2A< 4.8 dopaminergic D2 5.4 5 …

Structure−Activity Relationship Study on N-(1,2,3,4-Tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides, a Class of 5-HT7 Receptor Agents. 2

M Leopoldo, E Lacivita, M Contino… - Journal of medicinal …, 2007 - ACS Publications
Here we report the synthesis of N-(1, 2, 3, 4-tetrahydronaphthalen-1-yl)-4-aryl-1-
piperazinealkylamides 16− 29 that were designed to elucidate both structure− affinity and …

5-Chloro-N-(4-methoxy-3-piperazin-1-yl- phenyl)-3-methyl-2-benzothiophenesulfon- amide (SB-271046):  A Potent, Selective, and Orally Bioavailable 5-HT6 …

SM Bromidge, AM Brown, SE Clarke… - Journal of medicinal …, 1999 - ACS Publications
The 5-hydroxytryptamine (5-HT, serotonin) superfamily of receptors currently consists of 7
classes (5-HT1-5-HT7) that embrace 14 human subclasses. 1 The most recent addition is …

A Novel, Potent, and Selective 5-HT7 Antagonist:  (R)-3-(2-(2-(4-Methylpiperidin-1-yl)ethyl)pyrrolidine-1-sulfonyl)phenol (SB-269970)

PJ Lovell, SM Bromidge, S Dabbs… - Journal of medicinal …, 2000 - ACS Publications
Introduction. The human 5-HT7 receptor is a recently discovered member of the seven-
transmembrane G-protein-coupled receptor superfamily. 2 The most abundant isoform 5 …

Characterization of [125I]‐SB‐258585 binding to human recombinant and native 5‐HT6 receptors in rat, pig and human brain tissue

WD Hirst, JAL Minton, SM Bromidge… - British journal of …, 2000 - Wiley Online Library
SB‐258585 (4‐Iodo‐N‐[4‐methoxy‐3‐(4‐methyl‐piperazin‐1‐yl)‐phenyl]‐
benzenesulphonamide) is a high affinity ligand at 5‐HT6 receptors. It displays over 100 fold …

[3H]-SB-269970 radiolabels 5-HT7 receptors in rodent, pig and primate brain tissues

DR Thomas, PJ Atkinson, PG Hastie, JC Roberts… - …, 2002 - Elsevier
The selective 5-HT7 receptor antagonist radioligand,[3H]-SB-269970, has been reported to
radiolabel the human cloned 5-HT7 (a) receptor and 5-HT7 receptors in guinea pig cortex …

Phenyl benzenesulfonamides are novel and selective 5-HT6 antagonists: identification of N-(2, 5-dibromo-3-fluorophenyl)-4-methoxy-3-piperazin-1 …

SM Bromidge, SE Clarke, T Gager, K Griffith… - Bioorganic & medicinal …, 2001 - Elsevier
Substituted N-phenyl-4-methoxy-3-piperazin-1-ylbenzenesulfonamides and
conformationally restricted analogues have been identified as high affinity and selective 5 …

The medicinal chemistry of 5-HT6 receptor ligands with a focus on arylsulfonyltryptamine analogs

RA Glennon, U Siripurapu, BL Roth… - Current topics in …, 2010 - ingentaconnect.com
Arylsulfonyl analogs of aminopyrimidines (eg Ro 04-6790; 2), aminopyridines (eg Ro 63-
0563; 3), 1-phenylpiperazines (eg SB-271046; 4), and tryptamines (eg MS-245; 5) were …

(Phenylpiperazinyl-butyl)oxindoles as Selective 5-HT7 Receptor Antagonists

B Volk, J Barkóczy, E Hegedus, S Udvari… - Journal of medicinal …, 2008 - ACS Publications
A series of potent 5-hydroxytryptamine7 (5-HT7) ligands has been synthesized that contain
a 1, 3-dihydro-2 H-indol-2-one (oxindole) skeleton. The binding of these compounds to the 5 …

[N-methyl-3H3] AZ10419369 binding to the 5-HT1B receptor: in vitro characterization and in vivo receptor occupancy

DL Maier, C Sobotka-Briner, M Ding, ME Powell… - … of Pharmacology and …, 2009 - ASPET
Radiotracers suitable for positron emission tomography studies often serve as preclinical
tools for in vivo receptor occupancy. The serotonin 1B receptor (5-HT1B) subtype is a …