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| Other names | CHF-1035; CHF1035; 5,6-Diisobutyryloxy-N-methyl-2-aminotetralin; 5,6-Diisobutyryloxy-2-(methylamino)-1,2,3,4-tetrahydronaphthalene; 5,6,7,8-Tetrahydro-6-(methylamino)-1,2-naphthylene diisobutyrate;N-Methyl-2-aminotetralin |
| Routes of administration | Oral[1][2] |
| Drug class | DopamineD2 receptoragonist;α2-Adrenergic receptoragonist |
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| Formula | C19H27NO4 |
| Molar mass | 333.428 g·mol−1 |
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Nolomirole (INNTooltip International Nonproprietary Name; developmental code nameCHF-1035), also known as5,6-diisobutyryloxy-N-methyl-2-aminotetralin, is a dualdopamineD2 andα2-adrenergic receptoragonist which was under development for the treatment ofheart failure but was never marketed.[1][2][3][4] It is takenorally.[1][2]
The drug acts as an agonist of the dopamine D2 receptor, with anaffinity (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 aprodrug ofCHF-1024 (5,6-dihydroxy-N-methyl-2-aminotetralin), to which it is rapidlyhydrolyzed by circulatingesteraseenzymes.[1] Theelimination half-life of nolomirole is said to be 3 hours and itslog P is 1.97.[3]
Nolomirole and its active formCHF-1024 arecyclized phenethylamines and2-aminotetralinanalogues of thecatecholamineneurotransmitterdopamine and itsN-methylderivativeepinine (deoxyepinephrine,N-methyldopamine).[1][2]
Nolomirole was first described in thescientific literature by 1992.[1][5] It was being developed by thepharmaceutical companyChiesi Farmaceutici in the 1990s and 2000s.[1][4] Nolomirole reachedphase 3clinical trials prior to the discontinuation of its development.[1][4]
