Drug intelligence / Profile preview

MK-912

Development stage
Preclinical
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

MK-912 is a **non-specific alpha-2 adrenergic receptor antagonist** with high affinity for the alpha-2A, alpha-2B, and alpha-2C receptor subtypes. It was originally developed by Merck & Co. and has been investigated for its potential therapeutic use in **depression** and **diabetes**, notably non-insulin-dependent (type 2) diabetes. MK-912 has also seen regular use as a molecular probe in research on alpha-2 adrenergic receptors due to its potency and subtype affinity. It is orally active in humans and animal models, and has demonstrated ability to block the effects of adrenergic receptor agonists like clonidine, impacting cardiovascular and metabolic parameters such as blood pressure, growth hormone secretion, and plasma glucose levels[1][2][4][5][6][7][9].

02

Targets

ADRA2C (α2C)ADRA2A (α2A)ADRA2B (α2B)

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