G-1 (drug)

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G-1 is a synthetic, non-steroidal compound that acts as a selective agonist for the G protein-coupled estrogen receptor (GPER), also known as GPR30. It is primarily used in research to study the physiological and pathological roles of GPER in various tissues.

Mechanism of Action

G-1 binds to GPER, a receptor that is distinct from the classical nuclear estrogen receptors, ERα and ERβ. GPER is a member of the G protein-coupled receptor family and is involved in rapid, non-genomic signaling pathways. Upon activation by G-1, GPER can initiate a variety of intracellular signaling cascades, including the activation of adenylate cyclase, phospholipase C, and the release of intracellular calcium.

Pharmacological Effects

Research has shown that G-1 can have diverse effects depending on the tissue and context. Some of the notable effects include:

• Cardiovascular System: G-1 has been shown to exert cardioprotective effects, potentially reducing myocardial infarction size and improving cardiac function.
• Nervous System: G-1 may have neuroprotective effects and has been studied in the context of neurodegenerative diseases.
• Cancer: G-1 has been investigated for its potential anti-cancer properties, particularly in breast cancer and ovarian cancer, where GPER is often overexpressed.

Research Applications

G-1 is widely used in preclinical studies to elucidate the role of GPER in various physiological and pathological processes. It serves as a valuable tool for distinguishing the effects mediated by GPER from those mediated by classical estrogen receptors.

Safety and Toxicity

As G-1 is primarily used in research settings, comprehensive safety and toxicity profiles in humans are not well-established. However, studies in animal models have not reported significant adverse effects at doses typically used in research.

Also see

• G protein-coupled receptor
• Estrogen receptor
• Selective estrogen receptor modulator
• Non-genomic actions of estrogen