G-36 (drug)

G-36_structure.png

G-36 is a synthetic compound that acts as a selective antagonist of 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-36 functions by binding to the GPER, thereby inhibiting its activation by endogenous estrogens such as estradiol. This blockade prevents the downstream signaling pathways that are typically activated by GPER, which include the activation of adenylate cyclase, modulation of intracellular calcium levels, and activation of various kinases such as ERK1/2.

Pharmacological Effects

In preclinical studies, G-36 has been shown to:

• Inhibit estrogen-induced proliferation of certain cancer cell lines, suggesting a potential role in breast cancer research.
• Modulate cardiovascular function, indicating its utility in studying estrogen's effects on the cardiovascular system.
• Affect metabolic processes, providing insights into estrogen's role in metabolism and obesity.

Research Applications

G-36 is widely used in laboratory settings to:

• Investigate the non-genomic actions of estrogens mediated by GPER.
• Differentiate between the effects mediated by classical estrogen receptors (ERα and ERβ) and GPER.
• Explore potential therapeutic targets for diseases influenced by estrogen signaling, such as cancer, cardiovascular disease, and metabolic disorders.

Safety and Toxicology

As G-36 is primarily used in research, detailed safety and toxicology profiles are not fully established. However, standard laboratory safety protocols should be followed when handling this compound.

Also see

• G protein-coupled estrogen receptor
• Estrogen receptor
• Selective estrogen receptor modulator
• Breast cancer
• Cardiovascular system