Etrabamine
Pharmaceutical compound
From Wikipedia, the free encyclopedia
Etrabamine (INN; developmental code name JL-14839 or 14.839JL), also known as 6-methylamino-4,5,6,7-tetrahydrobenzothiazole, is a dopamine receptor agonist which was under development for the treatment of Parkinson's disease but was never marketed.[1][2][3][4][5] It is taken orally.[1]
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| Other names | JL-14839; JL14839; 14.839JL; 6-Methylamino-4,5,6,7-tetrahydrobenzothiazole |
| Routes of administration | Oral[1] |
| Drug class | Dopamine receptor agonist; Dopamine D2 and D3 receptor agonist |
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| Formula | C8H12N2S |
| Molar mass | 168.26 g·mol−1 |
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The drug shows affinity for the dopamine D2 and D3 receptors (Ki = 2,620 nM and 300 nM, both for L-etrabamine).[6][7][5] It acts as a dopamine D2 and D3 receptor agonist and does not appear to act as an agonist of the dopamine D1 receptor.[5][6][7] Etrabamine produces stereotypy in rodents and to a greater extent than apomorphine.[5][7] This can be blocked by the dopamine D2 and D3 receptor antagonists sulpiride, haloperidol, and pimozide.[5] It reverses the hypolocomotion induced by the dopamine depleting agent reserpine in rodents.[5] The drug reduces levels of dopamine metabolites in the striatum in rodents.[5] It strongly suppresses prolactin levels in rodents.[5]
The chemical synthesis of etrabamine has been described.[7] The chemical structure of etrabamine was unlike that of other dopamine receptor agonists when it was first developed in the 1980s.[3][5] Subsequently, pramipexole, a closely related derivative of etrabamine, was developed and introduced for the treatment of Parkinson's disease.[4][3][6][8] Pramipexole shows 2.7- and 29-fold higher affinity for the dopamine D2 and D3 receptors than etrabamine, respectively.[6][7] Various other analogues and derivatives of etrabamine besides pramipexole have also been developed.[3][6][9]
Etrabamine was first described in the scientific literature in 1987.[3][5] It was under development by Logeais.[1][2] The drug reached phase 2 clinical trials prior to the discontinuation of its development in 1997.[1][2][4] Its close derivative pramipexole was first approved for medical use in 1997.[8]