alpha(2)-adrenoreceptors profile modulation and high antinociceptive activity of (S)-(-)-2-[1-(biphenyl-2-yloxy)ethyl]-4,5-dihydro-1H-imidazole

Gentili F.; Bousquet P.; Brasili L.; Caretto M.; Carrieri A.; Dontenwill M.; Giannella M.; Marucci G.; Perfumi M.; Piergentili A.; Quaglia W. Rascente C.; Pigini M.

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alpha(2)-adrenoreceptors profile modulation and high antinociceptive activity of (S)-(-)-2-[1-(biphenyl-2-yloxy)ethyl]-4,5-dihydro-1H-imidazole

机译：（S）-（-）-2- [1-（联苯-2-基氧基）乙基] -4,5-二氢-1H-咪唑的α（2）-肾上腺素受体谱调节和高镇痛活性

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A number of derivatives structurally related to cirazoline (1) were synthesized and studied with the purpose of modulating alpha(2)-adrenoreceptors selectivity versus both alpha(1)-adrenoreceptors and I-2 imidazoline binding sites. The most potent alpha(2)-agonist was 2-[1-(biphenyl-2-yloxy)ethyl]-4,5-dihydro-1H-imidazole (7), whose key pharmacophoric features closely matched those found in the alpha(2)-agonist 2-(3-exo-(3-phenylprop-1-yl)-2-exo-norborn,I)amino-2-oxazoline (15).(30) (S)-(-)-7 was the most potent of the two enantiomers, confirming the stereospecificity of the interaction with alpha(2)-adrenoreceptors. This eutomer was tested on two algesiometric paradigms and, because of the interaction with alpha(2)-adrenoreceptors, showed a potent and long-lasting antinociceptive activity, since it was abolished by the selective alpha(2)-antagonist RX821002. [References: 42]

机译：合成和研究了许多与cirazoline（1）结构相关的衍生物，目的是相对于alpha（1）-肾上腺素受体和I-2咪唑啉结合位点调节alpha（2）-肾上腺素受体选择性。最有效的alpha（2）激动剂是2- [1-（联苯-2-基氧基）乙基] -4,5-二氢-1H-咪唑（7），其关键药效学特征与alpha（2） 2）激动剂2-（3-exo-（3-phenylprop-1-yl）-2-exo-norborn，I）amino-2-oxazoline（15）。（30）（S）-（-）-7是两种对映体中最有效的，证实了与α（2）-肾上腺素受体相互作用的立体特异性。该eutomer在两个痛觉计量学范式上进行了测试，由于与α（2）-肾上腺素受体的相互作用，显示出有效且持久的抗伤害感受活性，因为它被选择性的alpha（2）-拮抗剂RX821002废除了。 [参考：42]

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《Journal of Medicinal Chemistry》 |2002年第1期|共9页
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Gentili F.; Bousquet P.; Brasili L.; Caretto M.; Carrieri A.; Dontenwill M.; Giannella M.; Marucci G.; Perfumi M.; Piergentili A.; Quaglia W. Rascente C.; Pigini M.;
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1. alpha(2)-adrenoreceptors profile modulation and high antinociceptive activity of (S)-(-)-2-[1-(biphenyl-2-yloxy)ethyl]-4,5-dihydro-1H-imidazole [J] . Gentili F., Bousquet P., Brasili L., Journal of Medicinal Chemistry . 2002,第1期

机译：（S）-（-）-2- [1-（联苯-2-基氧基）乙基] -4,5-二氢-1H-咪唑的α（2）-肾上腺素受体谱调节和高镇痛活性
2. S18327 (1-(2-(4-(6-fluoro-1, 2-benzisoxazol-3-yl)piperid-1-yl)ethyl)3-phenyl imidazolin-2-one), a novel, potential antipsychotic displaying marked antagonist properties at alpha(1)- and alpha(2)-adrenergic receptors: II. Functional profile and a mult [J] . Millan MJ, Brocco M, Rivet JM, The Journal of Pharmacology and Experimental Therapeutics: Official Publication of the American Society for Pharmacology and Experimental Therapeutics . 2000,第1期

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6. Unique profiles of the alpha 1- alpha 2- and beta-adrenergic receptors in the developing cortical plate and transient embryonic zones of the rhesus monkey [O] . MS Lidow, P Rakic 1994

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机译：由（E）-2-（1-（2-（哌嗪-1-基）乙基亚氨基）乙基）苯酚和（E）-4-（1-（2-）衍生的一些锌（II）配合物的合成和胃保护活性（哌嗪-1-基）乙基亚氨基）乙基）苯-1,3-二醇席夫碱对抗阿司匹林诱导的溃疡

alpha(2)-adrenoreceptors profile modulation and high antinociceptive activity of (S)-(-)-2-[1-(biphenyl-2-yloxy)ethyl]-4,5-dihydro-1H-imidazole

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