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Chemical Structure : Trazpiroben
Catalog No.: PC-72281Not For Human Use, Lab Use Only.
Trazpiroben (TAK-906) is a potent, peripherally selective D2/D3 dopamine receptor antagonist, moderate affinity for D4, and minimal for D1 and D5.
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Trazpiroben (TAK-906) is a potent, peripherally selective D2/D3 dopamine receptor antagonist, moderate affinity for D4, and minimal for D1 and D5.
Trazpiroben demonstrated the following receptor affinities: high for D2 and D3, moderate for D4, and minimal for D1 and D5, showed moderate affinity for adrenergic α 1B (α 1B) and 5HT)2A receptors and low potential for off-target adverse events (AEs).
Trazpiroben potently inhibited dopamine-activated D2L receptor activation of cognate G-proteins in human embryonic kidney 293 cell membranes and was a neutral D2L receptor antagonist.
Trazpiroben dose-dependently increased prolactin release in orally dosed rat (0.1-1 mg/kg).
Trazpiroben is a potent D2/D3 receptor antagonist designed to avoid the serious potential AEs associated with current gastroparesis.therapies.
| M.Wt | 633.742 | |
| Formula | C35H43N3O8 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Whiting RL, et al. J Pharmacol Exp Ther. 2021 Oct;379(1):85-95.
2. Whiting RL, et al. Clin Pharmacol Drug Dev. 2021 Aug;10(8):927-939.
3. Kaur Mukker J, et al. Clin Transl Sci. 2022 Feb 26.
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