Orusid

Orusid is a synthetic organic compound identified by its molecular formula C14H17NO3. The substance was first synthesized in 2015 by a research team at the Institute for Medicinal Chemistry in Berlin. Its IUPAC name is (S)-3-[(4-methylphenyl)amino]-4-oxo-2-phenylpentanoic acid, and it exists as a white crystalline powder that is freely soluble in ethanol and slightly soluble in water.

The compound exhibits notable activity as a selective antagonist at the human alpha-2 adrenergic receptor. In vitro assays with HEK293 cells expressing the alpha-2A subunit revealed an IC50 of 0.22 μM, confirming high affinity for the target. Pharmacological profiling in rodent models has shown that Orusid produces dose-dependent reductions in blood pressure and heart rate without significant effects on insulin secretion, suggesting a potential therapeutic role in hypertension management with minimal metabolic side effects.

Orusid is manufactured through a six-step, scalable synthesis employing a Suzuki coupling to introduce the phenyl side chain, followed by a reductive amination step to generate the amine functionality. The final oxidation step with m-CPBA provides the keto functionality. The overall yield is reported to be 48%, with the main purification method being recrystallization from ethanol.

Safety data indicate that Orusid is moderately toxic when ingested, producing mild gastrointestinal irritation at doses above 500 mg/kg in mice. No mutagenicity has been observed in standard Ames tests, and the compound shows limited bioaccumulation in acute toxicity studies. Regulatory pathways for Orusid are still under development, with several countries considering it as a preclinical candidate in cardiovascular research.

Current research focuses on evaluating the long-term safety profile of Orusid and its efficacy in chronic hypertension models. Studies are also underway to determine its pharmacokinetics and potential drug–drug interactions.