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合成大麻素AKB48对大鼠的药理和行为学影响。

Pharmacological and Behavioral Effects of the Synthetic Cannabinoid AKB48 in Rats.

作者信息

Bilel Sabrine, Tirri Micaela, Arfè Raffaella, Stopponi Serena, Soverchia Laura, Ciccocioppo Roberto, Frisoni Paolo, Strano-Rossi Sabina, Miliano Cristina, De-Giorgio Fabio, Serpelloni Giovanni, Fantinati Anna, De Luca Maria Antonietta, Neri Margherita, Marti Matteo

机构信息

Department of Morphology, Experimental Medicine and Surgery, Section of Legal Medicine and Laboratory for Technologies of Advanced Therapies (LTTA) Centre, University of Ferrara, Ferrara, Italy.

Section of Legal Medicine, Institute of Public Health, Università Cattolica del Sacro Cuore, Rome, Italy.

出版信息

Front Neurosci. 2019 Oct 30;13:1163. doi: 10.3389/fnins.2019.01163. eCollection 2019.

DOI:10.3389/fnins.2019.01163
PMID:31736697
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6831561/
Abstract

AKB48 is a designer drug belonging to the indazole synthetic cannabinoids class, illegally sold as herbal blend, incense, or research chemicals for their psychoactive cannabis-like effects. In the present study, we investigated the pharmacological and behavioral effects of AKB48 in male rats and measured the pharmacodynamic effects of AKB48 and simultaneously determined its plasma pharmacokinetic. AKB48 at low doses preferentially stimulated dopamine release in the nucleus accumbens shell (0.25 mg/kg) and impaired visual sensorimotor responses (0.3 mg/kg) without affecting acoustic and tactile reflexes, which are reduced only to the highest dose tested (3 mg/kg). Increasing doses (0.5 mg/kg) of AKB48 impaired place preference and induced hypolocomotion in rats. At the highest dose (3 mg/kg), AKB48 induced hypothermia, analgesia, and catalepsy; inhibited the startle/pre-pulse inhibition test; and caused cardiorespiratory changes characterized by bradycardia and mild bradipnea and SpO2 reduction. All behavioral and neurochemical effects were fully prevented by the selective CB receptor antagonist/inverse agonist AM251. AKB48 plasma concentrations rose linearly with increasing dose and were correlated with changes in the somatosensory, hypothermic, analgesic, and cataleptic responses in rats. For the first time, this study shows the pharmacological and behavioral effects of AKB48 in rats, correlating them to the plasma levels of the synthetic cannabinoid. AKB48 (PubChem CID: 57404063); AM251 (PubChem CID: 2125).

摘要

AKB48是一种属于吲唑合成大麻素类的设计药物，作为草药混合物、熏香或研究化学品非法销售，因其具有类似大麻的精神活性作用。在本研究中，我们研究了AKB48对雄性大鼠的药理和行为影响，测量了AKB48的药效学作用，并同时测定了其血浆药代动力学。低剂量的AKB48优先刺激伏隔核壳中的多巴胺释放（0.25毫克/千克），并损害视觉感觉运动反应（0.3毫克/千克），而不影响听觉和触觉反射，只有在测试的最高剂量（3毫克/千克）时这些反射才会减弱。增加剂量（0.5毫克/千克）的AKB48会损害大鼠的位置偏好并导致运动减少。在最高剂量（3毫克/千克）时，AKB48会引起体温过低、镇痛和僵住症；抑制惊吓/前脉冲抑制试验；并导致以心动过缓、轻度呼吸减慢和血氧饱和度降低为特征的心肺变化。所有行为和神经化学效应均被选择性CB受体拮抗剂/反向激动剂AM251完全阻断。AKB48的血浆浓度随剂量增加呈线性上升，并与大鼠体感、体温过低、镇痛和僵住症反应的变化相关。本研究首次展示了AKB48对大鼠的药理和行为影响，并将其与合成大麻素的血浆水平相关联。AKB48（PubChem CID：57404063）；AM251（PubChem CID：2125）。

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