ameliorated

Compound PDK0269, as 5-HT3 receptor agonists(3–100 μM, pEC50 5.05±0.06), acutely increased XII (hypoglossal) burst frequency and regularity, and decreased bursts/episode . Phenylbiguanide produced a dose-related (10-500 microM) increase in the release of dopamine (280-2000%). When nomifensine (5 microM) was included in the Ringer solution, the effect of Compound PDK0269 on the release of dopamine was ameliorated or inhibited.

GGTI 2147 decreased Rac1 activity, down-regulated p65 expression, and ameliorated OGD/R-induced neuronal apoptosis.

LI-2242 is a potent inositol hexakisphosphate kinase (IP6K) inhibitor with IC50s of 31 nM, 42 nM, 8.7 nM, and 1944 nM for IP6K1, IP6K2, IP6K3, and IPMK, respectively.LI-2242 ameliorated hepatic steatosis by reducing the expression of genes that enhance lipid uptake, lipid stabilization, and adipogenesis, and enhanced mitochondrial oxygen consumption rate (OCR) and insulin signaling in adipocytes and hepatocytes in vitro. LI-2242 ameliorated diet-induced obesity, hyperglycemia and hepatic steatosis in mice.LI-2242 can be used to study type II diabetes, obesity, metabolic complications, venous thrombosis and psychiatric disorders.

Eprociclovir potassium is a new acyclovir analogue and a potent inhibitor of EHV1 replication and may have potential for the treatment and/or prophylaxis of infections with this virus. Eprociclovir possess potent anti-herpetic activity against most human herpesviruses. A-5021 proved to be about 15-fold more potent than acyclovir in inhibiting viral replication. Eprociclovir inhibits murine herpetic keratitis. A-5021 eyedrops, which are easily applied onto the affected cornea, ameliorated clinical scores and suppressed virus growth. Eprociclovir is a promising alternative treatment of herpetic keratitis.

Valibose An α-glucosidase inhibitor. Valibose ameliorated metabolic disturbance of glucose and lipids. valibose markedly reduced level of serum BUN and NAG, and decreased the weight index of kidney.

Astramembrangenin (Cycloastragenol (Astramembrangenin)) is a triterpenoid saponin compound and a hydrolysis product of the main active ingredient in Astragalus membranaceus. Cycloastragenol (CAG) may have a novel therapeutic role in depression

1. Albiflorin (Alibiflorin) has anticonvulsant effect for pain relief. 2. Albiflorin and paeoniflorin has neuroprotective action against Glu toxicity. 3. Albiflorin and paeoniflorin significantly ameliorated Glu-induced reduction of cell viability, nuclear and mitochondrial apoptotic alteration, reactive oxygen species accumulation and B-cell lymphoma 2 (Bcl-2) Bax ratio. 4. Albiflorin can serve as a new chemical marker for the quality control of Paeoniae Radix and the Chinese Pharmacopoeia can be updated, via has similar anti-inflammatory effects to paeoniflorin.

Eprociclovir Na is the salt form of Eprociclovir, also known as A-5021, a new acyclovir analogue and a potent inhibitor of EHV1 replication and may have potential for the treatment and/or prophylaxis of infections with this virus. Eprociclovir possess potent anti-herpetic activity against most human herpesviruses. A-5021 proved to be about 15-fold more potent than acyclovir in inhibiting viral replication. Eprociclovir inhibits murine herpetic keratitis. A-5021 eyedrops, which are easily applied onto the affected cornea, ameliorated clinical scores and suppressed virus growth. Eprociclovir is a promising alternative treatment of herpetic keratitis.

S-8510 is a GABA-A receptor inverse agonist. S-8510 selectively potentiated pentylenetetrazol-induced convulsion without affecting minimal electroconvulsive shock- or strychnine-induced convulsion in ddY mice. S-8510 ameliorated memory impairment induced

Bixin is isolated from the seeds of Bixa orellana and possesses anti-tumor, anti-inflammatory, and antioxidant activities. Bixin treatment ameliorated cardiac dysfunction through inhibiting fibrosis, inflammation, and ROS generation.

BMP agonist 2 has up-regulated bone morphogenetic protein BMP-2 expression activity in vivo and anti-osteoporosis effects, and also has ameliorated the symptoms of osteoporosis in SAMP6 mice.BMP agonist 2 is an osteoinductive cytokine that promotes the production of bone tissue, and can be used in the study of senile osteoporosis (SOP).

R-130823 is a ighly selective inhibition against mitogen-activated protein kinase p38alpha (IC50=22 nM). The release of tumor necrosis factor-alpha, interleukin-1beta, -6 and -8 was inhibited in lipopolysaccharide-stimulated human blood pretreated by R-130823 , with IC50 values of 0.089, 0.066, 0.95 and 0.16 microM, respectively. R-130823 reduced the established hind paw swelling in rat adjuvant-induced arthritis, while methotrexate showed no suppression. In the same model, R-130823 ameliorated adjuvant-induced hyperalgesia with rapid onset and long duration comparable to a cyclooxygenase-2 inhibitor, celecoxib.

Eprociclovir dihydrate is a new acyclovir analogue and a potent inhibitor of EHV1 replication and may have potential for the treatment and/or prophylaxis of infections with this virus. Eprociclovir possess potent anti-herpetic activity against most human herpesviruses. A-5021 proved to be about 15-fold more potent than acyclovir in inhibiting viral replication. Eprociclovir inhibits murine herpetic keratitis. A-5021 eyedrops, which are easily applied onto the affected cornea, ameliorated clinical scores and suppressed virus growth. Eprociclovir is a promising alternative treatment of herpetic keratitis.

MRGPRX1 agonist 4 is a potent and orally active Mas-related G protein-coupled receptor X1 (MRGPRX1) positive conformation modulator (EC50: 0.1 μM). MRGPRX1 agonist 4 ameliorated the behavioral thermal allergic response in mice, a model of MRGPRX1 neuropathic pain.

SIK1 activator 1 can enhances the SIK1 phosphorylation and ameliorated the hyperglyceamia of type 2 diabetic mice. SIK1 activator 1 exhibited remarkable inhibitory activity on hepatic gluconeogenesis.

1. Spinosin (Flavoayamenin) ameliorated memory impairment induced through AβO, the serotonergic neurotransmitter system, and these effects were regulated, in part, through neuroprotective activity via the anti-inflammatory effects of Spinosin. 2. Spinosin exerts anxiolytic-like effects, and its mechanism of action appears to be modulated by GABAA and 5-HT1A receptors. 3. There was a wide brain regional tissue distribution of Spinosin. The concentrations of Spinosin in corpus striatum and hippocampus were higher than that in other areas.