Azemiopsin, a Selective Peptide Antagonist of Muscle Nicotinic Acetylcholine Receptor: Preclinical Evaluation as a Local Muscle Relaxant.

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作者： Irina V,Shelukhina ^[1] ; Maxim N,Zhmak ^[2] ; Alexander V,Lobanov ^[3] ; Igor A,Ivanov ^[4] ; Alexandra I,Garifulina ^[5] ; Irina N,Kravchenko ^[6] ; Ekaterina A,Rasskazova ^[7] ; Margarita A,Salmova ^[8] ; Elena A,Tukhovskaya ^[9] ; Vladimir A,Rykov ^[10] ; Gulsara A,Slashcheva ^[11] ; Natalya S,Egorova ^[12] ; Inessa S,Muzyka ^[13] ; Victor I,Tsetlin ^[14] ; Yuri N,Utkin ^[15]

作者单位： Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, ul. Miklukho-Maklaya 16/10, Moscow 117997, Russia. shelukhina.iv@yandex.ru. ^[1] Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, ul. Miklukho-Maklaya 16/10, Moscow 117997, Russia. mzhmak@gmail.com. ^[2] Branch of the Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, Pushchino 142290, Moscow Region, Russia. ^[3] Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, ul. Miklukho-Maklaya 16/10, Moscow 117997, Russia. chai.mail0@gmail.com. ^[4] Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, ul. Miklukho-Maklaya 16/10, Moscow 117997, Russia. garifulinaai@gmail.com. ^[5] Branch of the Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, Pushchino 142290, Moscow Region, Russia. ikravchenko@bibch.ru. ^[6] Branch of the Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, Pushchino 142290, Moscow Region, Russia. katyarass@mail.ru. ^[7] Branch of the Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, Pushchino 142290, Moscow Region, Russia. mak401@gmail.com. ^[8] Branch of the Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, Pushchino 142290, Moscow Region, Russia. elentuk@mail.ru. ^[9] Branch of the Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, Pushchino 142290, Moscow Region, Russia. vladimirrykov@email.su. ^[10] Branch of the Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, Pushchino 142290, Moscow Region, Russia. slashcheva_ga@mail.ru. ^[11] Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, ul. Miklukho-Maklaya 16/10, Moscow 117997, Russia. natalyegorov@yandex.ru. ^[12] Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, ul. Miklukho-Maklaya 16/10, Moscow 117997, Russia. mis_kou@mail.ru. ^[13] Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, ul. Miklukho-Maklaya 16/10, Moscow 117997, Russia. vits@mx.ibch.ru. ^[14] Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, ul. Miklukho-Maklaya 16/10, Moscow 117997, Russia. Yutkin@yandex.ru. ^[15]

关键词 Investigation of the preclinical profile of azemiopsin demonstrated its high affinity and specificity for muscle type nicotinic acetylcholine receptor as well as good muscle relaxant capacity. Toxicology studies in mice indicated that azemiopsin was well tolerated during chronic dosing and showed no immunotoxicity, allergenic or mutagenic activity, which made it a good candidate for application as a local muscle relaxant.Key Contribution azemiopsin myorelaxant nicotinic acetylcholine receptor pharmacokinetics preclinical studies toxicity