GR-127935

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GR-127935[edit | edit source]

Chemical structure of GR-127935

GR-127935 is a chemical compound that acts as a selective antagonist of the 5-HT1B receptor and 5-HT1D receptor. It is primarily used in scientific research to study the role of these receptors in various physiological and pathological processes.

Pharmacology[edit | edit source]

GR-127935 is known for its high affinity and selectivity for the serotonin receptor subtypes 5-HT1B and 5-HT1D. These receptors are part of the larger family of G protein-coupled receptors (GPCRs) and are involved in the modulation of neurotransmitter release, particularly serotonin.

Mechanism of Action[edit | edit source]

As an antagonist, GR-127935 binds to the 5-HT1B and 5-HT1D receptors, preventing the action of endogenous serotonin. This blockade can help elucidate the physiological roles of these receptors, such as their involvement in migraine pathophysiology and vasoconstriction.

Research Applications[edit | edit source]

GR-127935 is widely used in neuroscience research to investigate the function of 5-HT1B and 5-HT1D receptors. Studies have utilized this compound to explore its effects on behavioral neuroscience, pain management, and psychiatric disorders.

Migraine Studies[edit | edit source]

Research has shown that GR-127935 can be used to study the mechanisms underlying migraine headaches. By blocking the 5-HT1B and 5-HT1D receptors, researchers can better understand the role of serotonin in migraine attacks and develop potential therapeutic strategies.

Behavioral Studies[edit | edit source]

In behavioral studies, GR-127935 has been used to assess the role of serotonin in anxiety, depression, and aggression. The compound's ability to selectively block specific serotonin receptors makes it a valuable tool for dissecting the complex serotonergic pathways involved in these behaviors.

Chemical Properties[edit | edit source]

GR-127935 is a small molecule with a specific chemical structure that allows it to interact selectively with its target receptors. The structure of GR-127935 is depicted in the image to the right, highlighting its key functional groups responsible for receptor binding.

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Contributors: Prab R. Tumpati, MD