Yohimbine

An α2-adrenoceptor antagonist

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1g

￥600.00

480.00

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Background

Yohimbine is a natural alkaloid that has highest affinity for α₂-adrenergic receptors (pK_is = 8.2, 8.7, and 9.6 for human α_2A, α_2B, and α_2C, respectively), with antagonist activity at these receptors.^1,2 It less potently antagonizes serotonin 5-HT₁ receptors (pK_is = 7.3, 6.8, and 7.6 for human HT_1A, HT_1B, and HT_1D, respectively) and α₁-adrenergic receptors (pK_is = 6.7, 6.8, and 6.8 for human α_1A, α_1B, and α_1D, respectively).¹ Yohimbine is used in veterinary medicine to reverse the sedative effects of α₂-agonists.

1.Millan, M.J., Newman-Tancredi, A., Audinot, V., et al.Agonist and antagonist actions of yohimbine as compared to fluparoxan at α2-adrenergic receptors (AR)s, serotonin (5-HT)1A, 5-HT1B, 5-HT1D and dopamine D2 and D3 receptors. Significance for the modulation of frontocortical monoaminergic transmission and depressive statesSynapse35(2)79-95(2000) 2.Schwartz, D.D., and Clark, T.P.Selectivity of atipamezole, yohimbine and tolazoline for alpha-2 adrenergic receptor subtypes: Implications for clinical reversal of alpha-2 adrenergic receptor mediated sedation in sheepJ. Vet. Pharmacol. Ther.21(5)342-347(1998)