Nolomirole (; developmental code name CHF-1035), also known as 5,6-diisobutyryloxy-N-methyl-2-aminotetralin, is a dual dopamine D<sub>2</sub> and ñ<sub>2</sub>-adrenergic receptor agonist which was under development for the treatment of heart failure but was never marketed. It is taken orally.
The drug acts as an agonist of the dopamine D<sub>2</sub> receptor, with an affinity (K<sub>i</sub>) of 120nM for the (âÂÂ)- enantiomer and 2,400nM for the (+)- enantiomer, and as an agonist of the ñ<sub>2</sub>-adrenergic receptor, with an affinity (K<sub>i</sub>) of 130nM for the (âÂÂ)- enantiomer and 1,600nM for the (+)- enantiomer. It is a prodrug of CHF-1024 (5,6-dihydroxy-N-methyl-2-aminotetralin), 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.
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 (deoxyepinephrine, N-methyldopamine).
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.