Quantitative in vitro and in vivo pharmacological profile of CE-178253, a potent and selective cannabinoid type 1 (CB1) receptor antagonist [0.03%]
CE-178253的体内外药理学特征研究——一种新型高效的外周CB1受体拮抗剂
John R Hadcock,Philip A Carpino,Philip A Iredale et al.
John R Hadcock et al.
Background: Cannabinoid 1 (CB1) receptor antagonists exhibit pharmacological properties favorable for the treatment of obesity and other related metabolic disorders. CE-178253 (1-[7-(2-Chlorophenyl)-8-(4-chlorophenyl)-2-m...
Prediction of cytochrome P450 isoform responsible for metabolizing a drug molecule [0.03%]
预测药物分子代谢所负责的细胞色素P450同工酶
Nitish K Mishra,Sandhya Agarwal,Gajendra Ps Raghava
Nitish K Mishra
Background: Different isoforms of Cytochrome P450 (CYP) metabolized different types of substrates (or drugs molecule) and make them soluble during biotransformation. Therefore, fate of any drug molecule depends on how the...
Use of silkworms for identification of drug candidates having appropriate pharmacokinetics from plant sources [0.03%]
利用家蚕筛选具有合适药代动力学特性植物源药物候选物
Yukihiro Asami,Ryo Horie,Hiroshi Hamamoto et al.
Yukihiro Asami et al.
Background: We use silkworms to evaluate therapeutic effects of drug candidates. Our previous reports have revealed that there are common mechanisms of pharmacokinetics of chemicals in silkworms and mammals. In this repor...
An evaluation of R2 as an inadequate measure for nonlinear models in pharmacological and biochemical research: a Monte Carlo approach [0.03%]
评估R²作为药理和生物化学研究中非线性模型的不充分度量：一种蒙特卡罗方法
Andrej-Nikolai Spiess,Natalie Neumeyer
Andrej-Nikolai Spiess
Background: It is long known within the mathematical literature that the coefficient of determination R(2) is an inadequate measure for the goodness of fit in nonlinear models. Nevertheless, it is still frequently used wi...
Amphetamine dependence and co-morbid alcohol abuse: associations to brain cortical thickness [0.03%]
安非他命依赖及其共病酒精滥用与大脑皮层厚度的关系
Glenn Lawyer,Petr S Bjerkan,Anders Hammarberg et al.
Glenn Lawyer et al.
Background: Long-term amphetamine and methamphetamine dependence has been linked to cerebral blood perfusion, metabolic, and white matter abnormalities. Several studies have linked methamphetamine abuse to cortical grey m...
Deepak Singla,Arun Sharma,Jasjit Kaur et al.
Deepak Singla et al.
Background: Benzylisoquinoline is the structural backbone of many alkaloids with a wide variety of structures including papaverine, noscapine, codeine, morphine, apomorphine, berberine, protopine and tubocurarine. Many be...
Targeting ligand-gated ion channels in neurology and psychiatry: is pharmacological promiscuity an obstacle or an opportunity? [0.03%]
针对神经学和精神病学中的配体门控离子通道的靶向治疗：药理学多重性是障碍还是机会？
Matt T Bianchi,Emmanuel J Botzolakis
Matt T Bianchi
Background: The traditional emphasis on developing high specificity pharmaceuticals ("magic bullets") for the treatment of Neurological and Psychiatric disorders is being challenged by emerging pathophysiology concepts th...
Giulia Ferrari-Toninelli,Giuseppina Maccarinelli,Daniela Uberti et al.
Giulia Ferrari-Toninelli et al.
Background: Pramipexole exists as two isomers. The S(-) enantiomer is a potent D3/D2 receptor agonist and is extensively used in the management of PD. In contrast, the R(+) enantiomer is virtually devoid of any of the DA ...
Antinociceptive effect of geranylgeraniol and 6alpha,7beta-dihydroxyvouacapan-17beta-oate methyl ester isolated from Pterodon pubescens Benth [0.03%]
Pterodon pubescens Benth.抗痛觉物质牻牛儿基牻牛儿醇和6α,7β-二羟基葫芦巴坦-17β-O甲酸乙酯的抗痛觉效果研究
Humberto M Spindola,Leila Servat,Carina Denny et al.
Humberto M Spindola et al.
Background: Pterodon pubescens Benth seeds are commercially available in the Brazilian medicinal plant street market. The crude alcoholic extracts of this plant are used in folk medicine as anti-inflammatory, analgesic, a...
Divergence of allosteric effects of rapacuronium on binding and function of muscarinic receptors [0.03%]
瑞派庫尼翁對膽鹼能受體結合和功能的別構效應的分歧
Jan Jakubík,Alena Randáková,Esam E El-Fakahany et al.
Jan Jakubík et al.
Background: Many neuromuscular blockers act as negative allosteric modulators of muscarinic acetylcholine receptors by decreasing affinity and potency of acetylcholine. The neuromuscular blocker rapacuronium has been show...