SB-357134
SB-357134 is a drug that is used in scientific research. It acts as a potent and selective antagonist for the 5-HT6 receptor. It has been used to investigate the role of this receptor in the release of acetylcholine in the brain, and its potential role in the treatment of cognitive disorders such as Alzheimer's disease.
Pharmacology
SB-357134 is a potent and selective antagonist for the 5-HT6 receptor. It has a high affinity for this receptor, with a Ki of 8.9 nM. It has over 200-fold selectivity for the 5-HT6 receptor over other serotonin receptors and other neurotransmitter receptors.
The 5-HT6 receptor is a subtype of the serotonin receptor that is primarily found in the central nervous system. It is involved in the release of neurotransmitters such as acetylcholine, dopamine, and glutamate. Antagonism of this receptor by SB-357134 has been shown to increase the release of acetylcholine in the brain, which is thought to improve cognitive function.
Clinical significance
The 5-HT6 receptor has been implicated in a number of neurological and psychiatric disorders, including Alzheimer's disease, schizophrenia, and depression. As such, SB-357134 and other 5-HT6 receptor antagonists are being investigated for their potential therapeutic effects in these conditions.
In preclinical studies, SB-357134 has been shown to improve cognitive function in animal models of Alzheimer's disease. It has also been shown to have antidepressant-like effects in animal models of depression.
See also
References
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