In the present review, English literature on the pharmacological effects of Gastrodia elata was summarized. The literature mainly reported the effects of G. elata on central nervous system, including anticonvulsant, neuroprotection, improvement on learning and memory, and so on. These pharmacological effects were closely associated with its phenolic components.
Animals ; Central Nervous System ; drug effects ; Drugs, Chinese Herbal ; pharmacology ; Gastrodia ; chemistry ; Humans ; Memory ; drug effects

Gastrodin(GAS) and p-hydroxybenzyl alcohol(HBA) are extracts of dried tubers of Gastrodia elata, which is the material basis for its efficacy and belongs to phenolic compounds. Modern pharmacology studies have shown that they have significant effects on central nervous system diseases, such as insomnia, convulsions, depression, ischemic stroke, anxiety, and cognitive impairment, and these diseases are closely related to neurotransmitters and cytokines. This paper described various mechanisms of GAS and HBA monomer components on the central nervous system. They alleviate hippocampal neuronal toxicity mainly by regulating a variety of neurotransmitters, such as acetylcholine, glutamic acid(GLU), γ-aminobutyric acid(GABA), serotonin(5-HT), dopamine(DA), norepinephrine(NE), 5-indoleacetic acid(5-HIAA), high vanillic acid(HVA) and dihydroxyphenylacetic acid(DOPAC), pro-inflammatory cell growth factors, such as IL-1β, IL-6 and TNF-α and relevant receptor functions, and exert neuropharmacological effects by effectively increasing mRNA expressions of brain neurotrophic factors, such as BDNF and GDNF, and further inhibiting the apoptosis of damaged neurons. This paper summarized various mechanisms on the central nervous system, which provides a scientific basis for the further research of the neuropharmacological mechanism of GAS and HBA and the development of new drugs and functional food.
Benzyl Alcohols/pharmacology* ; Central Nervous System/drug effects* ; Gastrodia/chemistry* ; Glucosides/pharmacology* ; Humans ; Plant Extracts/pharmacology*

In recent years there have been more widely and deeply studies in investigating melamine toxicity. Generally, it is believed that the main target of melamine is the urinary system. However, previous studies revealed that it also had additional biological actions. Obviously, the toxicity mechanisms of melamine have not been fully clarified. It is well known that fetus and infant periods play the most fundamental role in the brain development. And melamine can pass through the placental and blood-brain barrier, and then exerts toxic effects on the central nervous system. This article reviewed the reports about the topic in recent years, for better understanding the dangers of melamine to infants and providing experimental data for further study.
Animals ; Blood-Brain Barrier ; drug effects ; Brain ; growth & development ; Central Nervous System ; drug effects ; Cognition ; drug effects ; Female ; Humans ; Maternal-Fetal Exchange ; drug effects ; Pregnancy ; Triazines ; pharmacokinetics ; toxicity

The objective of this review is the revision of the Korean practice parameters for the pharmacological treatment of attention-deficit hyperactivity disorder (ADHD) based on the change in the diagnostic system from DSM-IV-TR to DSM-5 and psychopharmacological developments. For the evidence-based approach, the authors conducted a review of the literature, including controlled clinical trials, studies of the side effects of drugs, toxicology and meta-analyses from the United States and Europe, as well as recent research conducted in Korea. The review committee composed of Korean experts on ADHD reviewed the revised parameters. This revised version reveals how to use central nervous system psychostimulants, non-stimulants such as atomoxetine and alpha2 agonists, and other medication for ADHD, and how to manage the adverse effects of such medication. At the end of this revised version, the authors propose recommendations for the pharmacotherapy of ADHD.
Advisory Committees ; Atomoxetine Hydrochloride ; Central Nervous System ; Drug Therapy ; Drug-Related Side Effects and Adverse Reactions ; Europe ; Korea ; Toxicology ; United States

Chlorogenic acid displays several important roles in the therapeutic properties of many herbs, such as antioxidant activity, antibacterial, antiviral, scavenging free radicals and exciting central nervous system. Only about one-third of chlorogenic acid was absorbed in its prototype, therefore, its gut metabolites play a more important role in the therapeutic properties of chlorogenic acid. It is necessary to consider not only the bioactivities of chlorogenic acid but also its gut metabolites. This review focuses on the potential activities and mechanisms of chlorogenic acid and its gut metabolites on central nervous system diseases.
Animals ; Central Nervous System Diseases ; drug therapy ; metabolism ; Chlorogenic Acid ; administration & dosage ; metabolism ; Humans ; Intestines ; drug effects ; metabolism

Recently, the antinociceptive and anti-inflammatory efficacy of bee venom (BV, Apis mellifera) has been confirmed in rodent models of inflammation and arthritis. Interestingly, the antinociceptive and anti-inflammatory effect of whole BV can be reproduced by two water-soluble fractions of BV (>20 kDa:BVAF1 and<10 kDa: BVAF3). Based on these scientific findings, BV and its effective water-soluble fractions have been proposed as potential anti-inflammatory and antinociceptive pharmaceuticals. While BV's anti-inflammatory and antinociceptive properties have been well documented, there have been no careful studies of potential, side effects of BV and its fractions when administered in the therapeutic range (BV, 5 microgram/kg; BVAF1, 0.2 microgram/kg: BVAF3, 3 microgram/kg; subcutaneous or intradermal). Such information is critical for future clinical use of BV in humans. Because of this paucity of information, the present study was designed to determine the general pharmacological/physiological effects of BV and its fractions administration on the rodent central nervous, cardiovascular, respiratory and gastrointestinal system. Subcutaneous BV and its fractions treatment did not produce any significant effects on general physiological functions at the highest dose tested (200-fold and 100-fold doses higher than that used clinically, respectively) except writhing test. These results demonstrate that doses of BV or BV subfractions in the therapeutic range or higher can be used as safe antinociceptive and anti-inflammatory agents.
Analgesics/*pharmacology ; Animals ; Anti-Inflammatory Agents/*pharmacology ; Bee Venoms/*pharmacology ; Cardiovascular System/*drug effects ; Central Nervous System/*drug effects ; Digestive System/*drug effects ; Male ; Mice ; Mice, Inbred ICR ; Rabbits ; Rats ; Rats, Sprague-Dawley ; Respiratory System/*drug effects

The blood-brain barrier (BBB) exerts its central nervous system (CNS) protective function as it hinders the delivery of diagnostic and therapeutic agents to the brain. With the development of nanotechnology during the last thirty years, the nanocarriers for delivering drugs make it possible to transport drugs across the BBB. The brain-targeted drug delivery system usually consists of two parts: nanocarriers and brain-targeted strategies. In this review, several kinds of nanocarriers are introduced for brain-targeted drug delivery. We focus on several possible strategies for brain-targeting and comment on their advantages and disadvantages in application.
Animals ; Biological Transport ; Blood-Brain Barrier ; Brain ; drug effects ; metabolism ; Central Nervous System Agents ; administration & dosage ; therapeutic use ; Central Nervous System Diseases ; diagnosis ; drug therapy ; Drug Carriers ; Drug Delivery Systems ; methods ; Humans ; Nanoparticles

Blood-brain barrier is a natural protection for human body. It protects central nervous system from the interruption and damage of xenobiotics. However, it prevents potential drugs aimed at central nervous system, thus becomes an obstruction for the development of central nervous system drugs. The recent development of blood-brain barrier permeability research and several lead optimization strategies to improve blood-brain barrier permeability are reviewed. These structure optimization methods include increasing lipophilicity, reducing hydrogen bond doners, simplifying molecule, increasing rigidity, lowering polar surface area, avoiding acid group, prodrug strategy, modifying into active transporter's substrates, as well as avoiding P-glycoprotein recognized structures.
ATP-Binding Cassette, Sub-Family B, Member 1 ; metabolism ; Biological Transport ; Blood-Brain Barrier ; Central Nervous System ; drug effects ; Central Nervous System Agents ; pharmacokinetics ; Drug Design ; Humans ; Permeability ; Xenobiotics ; adverse effects

Animals ; Cell Differentiation ; drug effects ; Cell Proliferation ; drug effects ; Central Nervous System ; drug effects ; growth & development ; Female ; Organophosphorus Compounds ; toxicity ; Pesticides ; toxicity ; Pregnancy ; Rats

OBJECTIVETo observe the effects of Herba ephedrae, honey-fried Herba ephedrae and Maxingshigan decoction on pentobabital sodium sleep experiment in mice.

METHODSMale Kunming mice were divided into 11 groups, namely normal saline (NS) group, ephedrine group, 3 Herba ephedrae dose (high, medium, and low) groups, 3 honey-fried Herba ephedrae dose group, and 3 Maxingshigan decoction dose groups. The corresponding drugs were administered intragastrically for 6 consecutive days, and 45 min after the final administration, the mice received intraperitoneal injection of pentobabital sodium, and the latent period and continuous sleeping time were recorded.

RESULTSCompared with high- and low-dose Herba ephedrae groups, Maxinshigan decoction containing equivalent Herba ephedrae significantly increased the sleeping time of the mice (P<0.05). In comparison with NS, the decoction at medium and low doses produced no significant changes in the sleeping time, which, however, was significantly shortened in the other 8 groups (P<0.05). Compared with Herba ephedrae, Maxingshigan decoction and honey-fried Herba ephedrae at equivalent doses showed comparable effects on the sleep latency (P>0.05).

CONCLUSIONUnder the condition of this experiment and with pentobabital sodium-induced sleeping time as the index, honey-fried Herba ephedrae shows no obvious effect in reducing the excitement of the central nervous system, while Maxingshigan decoction can significantly lower the excitement level, the effect of which is inversely correlated to the dose administered.

Animals ; Central Nervous System ; drug effects ; Dose-Response Relationship, Drug ; Drugs, Chinese Herbal ; pharmacology ; Ephedra sinica ; chemistry ; Male ; Mice ; Pentobarbital ; pharmacology ; Random Allocation ; Sleep ; drug effects