• Publications
  • Influence
The interaction of RS 25259‐197, a potent and selective antagonist, with 5‐HT3 receptors, in vitro
TLDR
A series of isoquinolines have been identified as 5‐HT3 receptor antagonists and competition studies in NG‐108‐15 cells indicated a pharmacological specificity entirely consistent with labelling a 5‐ HT3 receptor, i.e. RS 25259‐197 > granisetron > (S)‐zacopride > tropisetrons. Expand
Pharmacological characterization of two novel and potent 5‐HT4 receptor agonists, RS 67333 and RS 67506, in vitro and in vivo
TLDR
RS 67333 and RS 67506 acted as potent, partial 5‐HT4 receptor agonists in vitro and in vivo and may have some utility in elucidating the physiological role of 5‐ HT4 receptors. Expand
Discovery and SAR development of 2-(phenylamino) imidazolines as postacyclin receptor antagonists
On the basis of screening hits (1a,b), a series of selective, high affinity prostacyclin receptor antagonists was developed. The optimized lead compound 25dExpand
Pharmacological characterization of RS 25259‐197, a novel and selective 5‐HT3 receptor antagonist, in vivo
TLDR
RS 25259‐197 is a novel, highly potent and orally active 5‐HT3 receptor antagonist in vivo and appears to be a significant improvement over ondansetron in terms of potency and duration of action. Expand
The Effects of Novel, Selective 5-Hydroxytryptamine (5-HT)4 Receptor Ligands in Rat Spatial Navigation
TLDR
It is suggested that RS 67333 reversed the cognitive deficit induced by atropine and support a role of 5-HT4 receptors in rat spatial learning and memory. Expand
Discovery and SAR development of 2-(phenylamino) imidazolines as prostacyclin receptor antagonists [corrected].
TLDR
On the basis of screening hits (1a,b), a series of selective, high affinity prostacyclin receptor antagonists was developed and the optimized lead compound 25d had analgesic activity in the rat. Expand
2-(Quinuclidin-3-yl)pyrido[4,3-b]indol-1-ones and isoquinolin-1-ones. Potent conformationally restricted 5-HT3 receptor antagonists.
TLDR
The hexahydro-1H-benz[de]isoquinolinone (S,S)-37 was the highest affinity 5-HT3 receptor ligand prepared and was also potent in blocking cisplatin-induced emesis in both the ferret and the dog. Expand
Glucocorticoid receptor antagonists.
  • R. Clark
  • Medicine, Biology
  • Current topics in medicinal chemistry
  • 31 May 2008
TLDR
Potential therapeutic applications of selective GR antagonists are described including the pharmacological rationale and clinical evidence that underlies these proposed uses, including Cushing's syndrome, psychotic depression, diabetes, obesity, Alzheimer's disease, neuropathic pain, drug abuse, and glaucoma. Expand
Pharmacological properties of 5-Hydroxytryptamine(4) receptor antagonists on constitutively active wild-type and mutated receptors.
We studied the pharmacological properties of twenty-four 5-hydroxytryptamine (5-HT)(4) receptor ligands known to act as antagonists on 5-HT(4) receptors positively coupled to adenylyl cyclaseExpand
RS 23597‐190: a potent and selective 5‐HT4 receptor antagonist
TLDR
In conclusion, RS 23597‐190 acts as a high affinity, selective competitive antagonist at 5‐HT4 receptors and appears to be a useful tool for 5‐ HT4 receptor identification in vitro and in vivo. Expand
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