Nolomirole (INNTooltip International Nonproprietary Name; developmental code name CHF-1035), 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 (Ki) of 120 nM for the (–)- enantiomer and 2,400 nM for the (+)- enantiomer, and as an agonist of the α2-adrenergic receptor, with an affinity (Ki) of 130 nM for the (–)- enantiomer and 1,600 nM 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 3 hours 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 (deoxyepinephrine, N-methyldopamine).
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.
See also Cyclized phenethylamine Rotigotine 5-OH-DPAT 7-OH-DPAT Ibopamine Fosopamine O,O′-Diacetyldopamine Docarpamine Neurotransmitter prodrug Carmoxirole
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