E161111 is an ultra-short-acting etomidate analogue with stable haemodynamics that elicits only slight adrenocortical suppression in rats.
E161111 is an ultra-short-acting etomidate analogue with stable haemodynamics that elicits only slight adrenocortical suppression in rats.
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DOI：
10.7717/peerj.13492
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发表时间：
2022
期刊：
影响因子：
2.7
通讯作者：
Zhang, Wen-Sheng
中科院分区：
文献类型：
--
作者：
Wang, Bin;Gong, Deying;Kang, Yi;Liu, Jin;Yang, Jun;Zhang, Wen-Sheng
关键词：
我们报道了一种新的超短效依托咪酯类似物E161111，它与依托咪酯具有相同的初级代谢产物。测定了E161111在大鼠血浆和肝脏匀浆中的代谢率。按Richmond激动-镇静量表（RASS）给大鼠注射30或60分钟以维持轻度镇静，评分为−2至0分。在30 min输注期间监测平均动脉压（MAP）。在输注期间和输注后3小时测定血清皮质酮，作为肾上腺皮质功能的测量。大鼠血浆1 min （t1/2 = 6.69±0.07 s）和肝脏匀浆5 min （t1/2 = 10.20±3.76 s）未检出E161111；其主要代谢产物为依托咪酯酸。注射E161111 1 h后，大鼠转直反射丧失恢复时间为4.3±1.5 min。注射30 min时，E161111未引起MAP变化。注射E161111后1小时的刺激血清皮质酮水平显著高于注射依托咪酯后1小时的刺激血清皮质酮水平。E161111代谢迅速，代谢产物与依托咪酯相同，注射1 h后恢复时间短。与依托咪酯相比，它具有血流动力学稳定性和较轻的皮质酮抑制作用。
We report on a novel ultra-short-acting etomidate analogue, E161111, which has the same primary metabolite as etomidate. The metabolic rate of E161111 was determined in rat plasma and liver homogenate. Rats were infused for 30 or 60 min to maintain light sedation at Richmond Agitation-Sedation Scale (RASS) for −2 to 0 score. Mean arterial pressure (MAP) was monitored during 30 min infusion. The serum corticosterone was determined during and 3 h after infusion as a measure of adrenocortical function. E161111 was not detected in rat plasma at 1 min (t1/2 = 6.69 ± 0.07 s) and in rat liver homogenates at 5 min (t1/2 = 10.20 ± 3.76 s); its main metabolic product was etomidate acid. The recovery time from loss of righting reflex (LORR) was 4.3 ± 1.5 min after 1-h infusion of E161111. During 30 min infusion, E161111 did not cause MAP changes. The stimulated serum corticosterone levels after 1-h infusion of E161111 were significantly higher than that after 1-h infusion of etomidate at all time points tested for the 3 h study. E161111 was metabolised rapidly, the metabolites were same as etomidate, and the recovery time after 1-h infusion was short. It elicited haemodynamic stability and milder suppression of corticosterone than that elicited by etomidate.
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影响因子：
5.7
作者：
Komatsu, Ryu;You, Jing;Turan, Alparslan
通讯作者：
Turan, Alparslan
DOI：
10.1124/jpet.121.000691
发表时间：
2021-12-01
影响因子：
3.5
作者：
Xu, Xiangqing;Wei, Yaqin;Li, Qingeng
通讯作者：
Li, Qingeng
影响因子：
5.7
作者：
Ge R;Pejo E;Gallin H;Jeffrey S;Cotten JF;Raines DE
通讯作者：
Raines DE
影响因子：
--
作者：
Edalatkhah A;Kazemi MR;Samadi Khorshidi F;Akhoundimeybodi Z;Seyedhosseini SM;Rostami S;Hosseini BV;Akhondi Z;Ghelmani Y
通讯作者：
Ghelmani Y
影响因子：
15.1
作者：
Ge, Rile;Pejo, Ervin;Raines, Douglas E.
通讯作者：
Raines, Douglas E.