Wy 27127 is a potent and selective α 2 -adrenergic receptor antagonist. Wy 27127 competitively blocks α 2 -adrenergic receptors, interrupts the negative feedback loop of sympathetic nerve endings, enhances stimulus-evoked norepinephrine release, and blocks agonist-induced inhibition of vas deferens contraction. Wy 27127 shows weak antagonistic effects on α 1 receptors, and exhibits no significant antagonistic activity against 5-hydroxytryptamine, muscarinic, presynaptic dopamine, histamine or β 1 -adrenergic receptors in vitro. Wy 27127 blocks saphenous vein contraction mediated by postsynaptic α 2 -adrenergic receptor agonists. Wy 27127 is applicable to studies related to sympathetic neurotransmission and vascular adrenergic responses.
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