Wy 27127
Wy 27127 is a potent and selective α2-adrenergic receptor antagonist. Wy 27127 competitively blocks α2-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 α1 receptors, and exhibits no significant antagonistic activity against 5-hydroxytryptamine, muscarinic, presynaptic dopamine, histamine or β1-adrenergic receptors in vitro. Wy 27127 blocks saphenous vein contraction mediated by postsynaptic α2-adrenergic receptor agonists. Wy 27127 is applicable to studies related to sympathetic neurotransmission and vascular adrenergic responses.
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- CAS 番号: 95669-35-5
- 分子式: C17H27N3O4S2
- 分子量:401.54
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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生物活性
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α2-adrenergic receptor |
Wy 27127 (10-7-10-6 M; 30 min) acts as a competitive α2-adrenergic receptor antagonist in the prostatic segment of isolated rat vas deferens. Its potency against clonidine is comparable to that of idazoxan (pA2=7.93), while its potency against B-HT 933 is slightly lower (pA2=7.63)[1].
Wy 27127 (10-5-3×10-5 M; 30 min) acts as a competitive α1-adrenergic receptor antagonist in isolated rat coccygeus muscles, with a pA2 value of 5.32, and its potency is approximately 1/7 that of idazoxan at this receptor subtype[1].
Wy 27127 (10-6-10-5 M; 30 min) shows no antagonistic activity against 5-HT (D), histamine (H1), muscarinic, presynaptic dopamine or β1-adrenergic receptors at the concentration of 10-5 M in relevant ex vivo tissue experiments[1].
Wy 27127 (30 min) acts as a potent antagonist that inhibits B-HT 933-induced contraction of isolated canine saphenous veins, with a pA2 value of 7.4 at post-synaptic α2-adrenergic receptors[2].
Wy 27127 (10-5 M; 30 min) acts as an antagonist against UK-14304-induced contraction of isolated canine saphenous veins, with a pA2 value of 6.9 at post-synaptic α2-adrenergic receptors[2].
Wy 27127 (30 min) acts as an antagonist of methoxamine-induced contraction in isolated canine saphenous veins, with a pA2 value of 6.0 at α1-adrenergic receptors; its potency does not change significantly when combined with catecholamine uptake blockers and propranolol[2].
Wy 27127 (up to 1.2×10-3 M) shows no agonist activity (contractile effect) in isolated female canine saphenous veins at concentrations up to 1.2×10-3 M[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 95669-35-5
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分子量 401.54
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分子式 C17H27N3O4S2
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SMILES
CS(NCCN([C@H]1C[C@@]2([H])C3=CC=CC=C3CCN2CC1)S(C)(=O)=O)(=O)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[1]. Bill SJ et al. Some pharmacological properties of Wy 27127 a more selective alpha 2:alpha 1-adrenoceptor antagonist than idazoxan in vitro. Naunyn Schmiedebergs Arch Pharmacol. 1986 Dec;334(4):418-22. [Content Brief]
[2]. Rhodes KF, et al. The effects of some alpha-adrenoceptor antagonists on the responses of the canine saphenous vein to B-HT 933, UK-14304 and methoxamine. Naunyn-Schmiedeberg's archives of pharmacology. 1987 Mar;335(3):261-8. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Wy 27127 関連分類
HY-183399 関連分類
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