Buy Nolomirole (CHF-1035) Cas 90060-42-7
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.[1][2][3][4] It is taken orally.[1][2]
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.[1][2] It is a prodrug of CHF-1024 (5,6-dihydroxy-N-methyl-2-aminotetralin), to which it is rapidly hydrolyzed by circulating esterase enzymes.[1] The elimination half-life of nolomirole is said to be 3 hours and its log P is 1.97.[3]
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).[1][2]
History
Nolomirole was first described in the scientific literature by 1992.[1][5] It was being developed by the pharmaceutical company Chiesi Farmaceutici in the 1990s and 2000s.[1][4] Nolomirole reached phase 3 clinical trials prior to the discontinuation of its development
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