5-I-R91150

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5-I-R91150


5-I-R91150 is a radioligand used in neuroscience research, specifically in the study of the serotonin 5-HT2A receptor. It is a selective antagonist for this receptor subtype, meaning it binds to the receptor and blocks its activation by other substances.

Chemistry[edit | edit source]

5-I-R91150 is a derivative of the phenylpiperazine class of compounds. It is structurally related to other 5-HT2A antagonists such as ketanserin and ritanserin, but is distinguished by the presence of an iodine atom at the 5-position of the phenyl ring. This iodine atom allows the compound to be used as a radioligand, as it can be replaced with a radioactive isotope of iodine for imaging studies.

Pharmacology[edit | edit source]

As a 5-HT2A antagonist, 5-I-R91150 inhibits the action of serotonin at this receptor subtype. The 5-HT2A receptor is widely distributed in the brain and is involved in a variety of physiological processes, including mood regulation, cognition, and perception. Antagonists of this receptor have been investigated for their potential in treating psychiatric disorders such as schizophrenia and depression.

Research Use[edit | edit source]

5-I-R91150 is primarily used in Positron Emission Tomography (PET) studies to visualize the distribution of 5-HT2A receptors in the brain. By using a radioactive isotope of iodine to label the compound, researchers can track its binding to the receptor in vivo. This provides valuable information about the density and distribution of 5-HT2A receptors in different brain regions, and how these may be altered in various neurological and psychiatric conditions.

See Also[edit | edit source]

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Contributors: Prab R. Tumpati, MD