An Overview of the CNS-Pharmacodynamic Profiles of Nonselective and Selective GABA Agonists.
Authors: Chen X, de Haas S, de Kam M, van Gerven J Abstract Various α(2,3) subtype selective partial GABA-A agonists are in development to treat anxiety disorders. These compounds are expected to be anxiolytic with fewer undesirable side effects, compared to nonselective GABA-A agonists like benzodiazepines. Several α(2,3) subtype selective and nonselective GABA-A agonists have been examined in healthy volunteers, using a battery addressing different brain domains. Data from five placebo-controlled double-blind studies were pooled. Lorazepam 2 mg was the comparator in three studies. Three α(2,3)-selec...
Source: Advances in Pharmacological Sciences - November 25, 2014 Category: Drugs & Pharmacology Tags: Adv Pharmacol Sci Source Type: research

Perisynaptic GABA Receptors The Overzealous Protector.
Authors: Clarkson AN Abstract An attempt to find pharmacological therapies to treat stroke patients and minimize the extent of cell death has seen the failure of dozens of clinical trials. As a result, stroke/cerebral ischemia is the leading cause of lasting adult disability. Stroke-induced cell death occurs due to an excess release of glutamate. As a consequence to this, a compensatory increased release of GABA occurs that results in the subsequent internalization of synaptic GABA(A) receptors and spillover onto perisynaptic GABA(A) receptors, resulting in increased tonic inhibition. Recent studies show t...
Source: Advances in Pharmacological Sciences - November 25, 2014 Category: Drugs & Pharmacology Tags: Adv Pharmacol Sci Source Type: research

Allosteric modulation of beta1 integrin function induces lung tissue repair.
Authors: Aljamal-Naylor R, Wilson L, McIntyre S, Rossi F, Harrison B, Marsden M, Harrison DJ Abstract The cellular cytoskeleton, adhesion receptors, extracellular matrix composition, and their spatial distribution are together fundamental in a cell's balanced mechanical sensing of its environment. We show that, in lung injury, extracellular matrix-integrin interactions are altered and this leads to signalling alteration and mechanical missensing. The missensing, secondary to matrix alteration and cell surface receptor alterations, leads to increased cellular stiffness, injury, and death. We have identified...
Source: Advances in Pharmacological Sciences - November 25, 2014 Category: Drugs & Pharmacology Tags: Adv Pharmacol Sci Source Type: research

Mechanisms Underlying Tolerance after Long-Term Benzodiazepine Use: A Future for Subtype-Selective GABA(A) Receptor Modulators?
Authors: Vinkers CH, Olivier B Abstract Despite decades of basic and clinical research, our understanding of how benzodiazepines tend to lose their efficacy over time (tolerance) is at least incomplete. In appears that tolerance develops relatively quickly for the sedative and anticonvulsant actions of benzodiazepines, whereas tolerance to anxiolytic and amnesic effects probably does not develop at all. In light of this evidence, we review the current evidence for the neuroadaptive mechanisms underlying benzodiazepine tolerance, including changes of (i) the GABA(A) receptor (subunit expression and receptor...
Source: Advances in Pharmacological Sciences - November 25, 2014 Category: Drugs & Pharmacology Tags: Adv Pharmacol Sci Source Type: research

GABA(A) Receptor Subtypes: Novel Targets for Novel Medicines.
Authors: Mirza NR, Atack J, Wafford K PMID: 22570647 [PubMed] (Source: Advances in Pharmacological Sciences)
Source: Advances in Pharmacological Sciences - November 25, 2014 Category: Drugs & Pharmacology Tags: Adv Pharmacol Sci Source Type: research

Biomarkers of oxidative stress and personalized treatment of pulmonary tuberculosis: emerging role of gamma-glutamyltransferase.
Conclusion. The initial two months led to significant improvement of oxidative stress. Values of oxidative markers in normal ranges might predict low rate of ADR. PMID: 22611380 [PubMed] (Source: Advances in Pharmacological Sciences)
Source: Advances in Pharmacological Sciences - November 25, 2014 Category: Drugs & Pharmacology Tags: Adv Pharmacol Sci Source Type: research

The Anti-Inflammatory, Phytoestrogenic, and Antioxidative Role of Labisia pumila in Prevention of Postmenopausal Osteoporosis.
Authors: Nadia ME, Nazrun AS, Norazlina M, Isa NM, Norliza M, Ima Nirwana S Abstract Osteoporosis is characterized by skeletal degeneration with low bone mass and destruction of microarchitecture of bone tissue which is attributed to various factors including inflammation. Women are more likely to develop osteoporosis than men due to reduction in estrogen during menopause which leads to decline in bone-formation and increase in bone-resorption activity. Estrogen is able to suppress production of proinflammatory cytokines such as IL-1, IL-6, IL-7, and TNF-α. This is why these cytokines are elevated in post...
Source: Advances in Pharmacological Sciences - November 25, 2014 Category: Drugs & Pharmacology Tags: Adv Pharmacol Sci Source Type: research

Antinociceptive, anti-inflammatory, and antipyretic activity of mangrove plants: a mini review.
Authors: Shilpi JA, Islam ME, Billah M, Islam KM, Sabrin F, Uddin SJ, Nahar L, Sarker SD Abstract Mangrove plants are specialised plants that grow in the tidal coasts of tropic and subtropic regions of the world. Their unique ecology and traditional medicinal uses of mangrove plants have attracted the attention of researchers over the years, and as a result, reports on biological activity of mangrove plants have increased significantly in recent years. This review has been set out to compile and appraise the results on antinociceptive, anti-inflammatory, and antipyretic activity of mangrove plants. While t...
Source: Advances in Pharmacological Sciences - November 25, 2014 Category: Drugs & Pharmacology Tags: Adv Pharmacol Sci Source Type: research

The treatment of inflammation, pain, and Fever using medicinal plants.
Authors: Akkol EK, Das S, Sarker SD, Nahar L PMID: 22693493 [PubMed] (Source: Advances in Pharmacological Sciences)
Source: Advances in Pharmacological Sciences - November 25, 2014 Category: Drugs & Pharmacology Tags: Adv Pharmacol Sci Source Type: research

Effects of Nicotine on Emotional Reactivity in PTSD and Non-PTSD Smokers: Results of a Pilot fMRI Study.
Authors: Froeliger B, Crowell Beckham J, Feldman Dennis M, Victoria Kozink R, Joseph McClernon F Abstract There is evidence that individuals with posttraumatic stress disorder (PTSD) may smoke in part to regulate negative affect. This pilot fMRI study examined the effects of nicotine on emotional information processing in smokers with and without PTSD. Across groups, nicotine increased brain activation in response to fearful/angry faces (compared to neutral faces) in ventral caudate. Patch x Group interactions were observed in brain regions involved in emotional and facial feature processing. These prelimi...
Source: Advances in Pharmacological Sciences - November 25, 2014 Category: Drugs & Pharmacology Tags: Adv Pharmacol Sci Source Type: research

Analgesic and Anti-Inflammatory Activity of Pinus roxburghii Sarg.
Authors: Kaushik D, Kumar A, Kaushik P, Rana AC Abstract The Chir Pine, Pinus roxburghii, named after William Roxburgh, is a pine native to the Himalaya. Pinus roxburghii Sarg. (Pinaceae) is traditionally used for several medicinal purposes in India. As the oil of the plant is extensively used in number of herbal preparation for curing inflammatory disorders, the present study was undertaken to assess analgesic and anti-inflammatory activities of its bark extract. Dried and crushed leaves of Pinus roxburghii Sarg. were defatted with petroleum ether and then extracted with alcohol. The alcoholic extract at ...
Source: Advances in Pharmacological Sciences - November 25, 2014 Category: Drugs & Pharmacology Tags: Adv Pharmacol Sci Source Type: research

Assessment of 5-HT(7) Receptor Agonists Selectivity Using Nociceptive and Thermoregulation Tests in Knockout versus Wild-Type Mice.
Authors: Brenchat A, Rocasalbas M, Zamanillo D, Hamon M, Vela JM, Romero L Abstract No study has ever examined the effect of 5-HT(7) receptor agonists on nociception by using 5-HT(7) receptor knockout mice. Basal sensitivity to noxious heat stimuli and formalin-induced nociception in both phase I and II of the formalin test did not differ in 5-HT(7) receptor knockout mice and paired wild-type controls. Similarly, there was no significant difference in basal body temperature between both genotypes. Subcutaneous administration of 5-HT(7) receptor agonists AS-19 (10 mg/kg), E-57431 (10 mg/kg), and E-55888...
Source: Advances in Pharmacological Sciences - November 25, 2014 Category: Drugs & Pharmacology Tags: Adv Pharmacol Sci Source Type: research

Polysaccharides of St. John's Wort Herb Stimulate NHDF Proliferation and NEHK Differentiation via Influence on Extracellular Structures and Signal Pathways.
In conclusion polysaccharides have been shown as biologically active ingredients of aqueous St. John's Wort extracts with a relation between their structural characteristics and function. PMID: 22848211 [PubMed] (Source: Advances in Pharmacological Sciences)
Source: Advances in Pharmacological Sciences - November 25, 2014 Category: Drugs & Pharmacology Tags: Adv Pharmacol Sci Source Type: research

Molecular Mechanisms Underlying Anti-Inflammatory Actions of 6-(Methylsulfinyl)hexyl Isothiocyanate Derived from Wasabi (Wasabia japonica).
Authors: Uto T, Hou DX, Morinaga O, Shoyama Y Abstract 6-(Methylsulfinyl)hexyl isothiocyanate (6-MSITC) is a major bioactive compound in wasabi (Wasabia japonica), which is a typical Japanese pungent spice. Recently, in vivo and in vitro studies demonstrated that 6-MSITC has several biological properties, including anti-inflammatory, antimicrobial, antiplatelet, and anticancer effects. We previously reported that 6-MSITC strongly suppresses cyclooxygenase-2 (COX-2), inducible nitric oxide synthase (iNOS), and cytokines, which are important factors that mediate inflammatory processes. Moreover, molecular an...
Source: Advances in Pharmacological Sciences - November 25, 2014 Category: Drugs & Pharmacology Tags: Adv Pharmacol Sci Source Type: research

Central dopaminergic system and its implications in stress-mediated neurological disorders and gastric ulcers: short review.
Authors: Rasheed N, Alghasham A Abstract For decades, it has been suggested that dysfunction of dopaminergic pathways and their associated modulations in dopamine levels play a major role in the pathogenesis of neurological disorders. Dopaminergic system is involved in the stress response, and the neural mechanisms involved in stress are important for current research, but the recent and past data on the stress response by dopaminergic system have received little attention. Therefore, we have discussed these data on the stress response and propose a role for dopamine in coping with stress. In addition, we ...
Source: Advances in Pharmacological Sciences - November 25, 2014 Category: Drugs & Pharmacology Tags: Adv Pharmacol Sci Source Type: research