ICI-154129

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ICI-154129 is a chemical compound that has been studied for its potential pharmacological effects. It is primarily known for its role as a serotonin receptor antagonist, specifically targeting the 5-HT2 receptor subtype. This compound was developed and studied by the pharmaceutical company ICI Pharmaceuticals, now part of AstraZeneca.

Chemical Structure and Properties

ICI-154129 is classified as an indolinone derivative. Its chemical structure is characterized by a dichlorophenyl group attached to an indolinone moiety. The presence of chlorine atoms in the phenyl ring is significant for its binding affinity and selectivity towards serotonin receptors.

Pharmacology

ICI-154129 functions as a selective antagonist of the 5-HT2 receptor, which is a subtype of the serotonin receptor family. The 5-HT2 receptors are involved in various neurological processes, including mood regulation, perception, and cognition. By blocking these receptors, ICI-154129 can modulate the effects of serotonin in the central nervous system.

Mechanism of Action

The mechanism of action of ICI-154129 involves competitive inhibition of serotonin binding to the 5-HT2 receptors. This inhibition can lead to alterations in neurotransmitter release and neuronal excitability, which may have therapeutic implications for conditions such as depression, anxiety, and schizophrenia.

Research and Development

ICI-154129 was initially developed as part of a research program aimed at discovering new treatments for psychiatric disorders. Preclinical studies demonstrated its efficacy in animal models of anxiety and depression, leading to interest in its potential as a therapeutic agent.

Clinical Trials

Despite promising preclinical results, ICI-154129 did not advance to large-scale clinical trials. The reasons for this may include issues related to its pharmacokinetic properties, side effect profile, or the emergence of more promising compounds.

Potential Applications

While ICI-154129 itself is not used clinically, its study has contributed to the understanding of serotonin receptor pharmacology and the development of other 5-HT2 receptor antagonists that are used in clinical practice.

Also see

• Serotonin receptor antagonists
• 5-HT2 receptor
• Pharmacology of serotonin
• AstraZeneca