GR-135,531

GR-135,531

GR-135,531 is a synthetic compound that acts as a selective antagonist of the 5-HT_1B receptor, a subtype of the serotonin receptor. This compound has been utilized in scientific research to better understand the role of 5-HT_1B receptors in various physiological and neurological processes.

Chemical Structure and Properties

GR-135,531 is chemically classified as a piperazine derivative. Its molecular formula is C₂₀H₂₅ClN₂O, and it has a molecular weight of 344.88 g/mol. The compound is characterized by its high affinity for the 5-HT_1B receptor, where it acts as a competitive antagonist.

Mechanism of Action

The primary action of GR-135,531 is to block the 5-HT_1B receptor, which is a G protein-coupled receptor (GPCR) involved in the modulation of neurotransmitter release. By inhibiting this receptor, GR-135,531 can alter the release of serotonin and other neurotransmitters, thereby affecting mood, cognition, and various other central nervous system functions.

Research Applications

GR-135,531 has been extensively used in preclinical studies to investigate the role of 5-HT_1B receptors in:

• Migraine: The compound has been used to study the pathophysiology of migraines, as 5-HT_1B receptors are implicated in the vasoconstriction of cranial blood vessels.
• Depression and Anxiety: Research has explored how 5-HT_1B receptor antagonism affects mood disorders, providing insights into potential therapeutic targets.
• Substance Abuse: Studies have examined the role of 5-HT_1B receptors in addiction and reward pathways, particularly in relation to drugs such as cocaine and alcohol.

Pharmacokinetics

The pharmacokinetic profile of GR-135,531 includes its absorption, distribution, metabolism, and excretion. The compound is typically administered in experimental settings via intravenous or intraperitoneal routes. It is metabolized primarily in the liver and excreted through the kidneys.

Safety and Toxicology

As with many research chemicals, the safety profile of GR-135,531 is not fully established in humans. However, animal studies have provided some data on its potential toxicological effects, which include alterations in cardiovascular and central nervous system functions at high doses.

Also see

• 5-HT1B receptor
• Serotonin receptor
• Migraine pathophysiology
• Neurotransmitter release
• G protein-coupled receptor