Nolomirole


Nolomirole, also known as 5,6-diisobutyryloxy-N-methyl-2-aminotetralin, is a dual dopamine D2 and α2-adrenergic receptor agonist which was under development for the treatment of heart failure but was never marketed. It is taken orally.

Pharmacology

The drug acts as an agonist of the dopamine D2 receptor, with an affinity of 120nM for the - enantiomer and 2,400nM for the - enantiomer, and as an agonist of the α2-adrenergic receptor, with an affinity of 130nM for the - enantiomer and 1,600nM for the - enantiomer. It is a prodrug of CHF-1024, to which it is rapidly hydrolyzed by circulating esterase enzymes. The elimination half-life of nolomirole is said to be 3hours and its log P is 1.97.

Chemistry

Nolomirole and its active form CHF-1024 are cyclized phenethylamines and 2-aminotetralin analogues of the catecholamine neurotransmitter dopamine and its N-methyl derivative epinine.

History

Nolomirole was first described in the scientific literature by 1992. It was being developed by the pharmaceutical company Chiesi Farmaceutici in the 1990s and 2000s. Nolomirole reached phase 3 clinical trials prior to the discontinuation of its development.