SB-258719

SB-258719 is a serotonin 5-HT4 receptor antagonist developed by SmithKline Beecham. It has been used in scientific research to explore the role of 5-HT4 receptors in the brain and gut, and has been shown to produce anxiolytic effects in animal studies.

Chemistry

SB-258719 is a quinuclidine derivative. It is chemically described as 1-(4-amino-5-chloro-2-methoxyphenyl)-3-[1-(2-methylsulphonylamino)ethyl]-4- piperidinyl-1-propanone hydrochloride. Its molecular formula is C19H28ClN3O4S and it has a molecular weight of 429.96 g/mol.

Pharmacology

SB-258719 is a potent and selective antagonist of the serotonin 5-HT4 receptor. It has a high affinity for this receptor subtype, with a Ki value of 0.16 nM. It has been shown to block the effects of 5-HT4 receptor agonists in various in vitro and in vivo assays.

Clinical significance

The 5-HT4 receptor is thought to play a role in various physiological and pathological processes, including the regulation of gastrointestinal motility, the modulation of neurotransmitter release in the brain, and the pathophysiology of irritable bowel syndrome and depression. Therefore, SB-258719 has been used in scientific research to explore these roles.

In animal studies, SB-258719 has been shown to produce anxiolytic effects. It has been suggested that these effects may be due to the blockade of 5-HT4 receptors in the brain, which may inhibit the release of stress-related neurotransmitters.

See also

• 5-HT4 receptor
• Serotonin
• SmithKline Beecham
• Quinuclidine