Bifeprunox is a partial dopamine and serotonin agonist potentially for the treatment of schizophrenia. Bifeprunox suppresses in vivo VTA dopaminergic neuronal activity via D2 and not D3 dopamine autoreceptor activation. Bifeprunox influences nicotine-seek
VU6010608 is an effective mGlu7 NAM with excellent CNS permeability and is powerful in electrophysiological studies in blocking long-term enhancement of high-frequency stimuli.
The phospholipases are an extensive family of lipid hydrolases that function in cell signaling, digestion, membrane remodeling, and as venom components. The calcium-independent phospholipases (iPLA2) are a PLA2 subfamily closely associated with the release of arachidonic acid in response to physiologic stimuli. (R)-Bromoenol lactone ((R)-BEL) is an irreversible, chiral, mechanism-based inhibitor of calcium-independent phospholipase γ (iPLA2γ). Unlike (S)-BEL, (R)-BEL does not inhibit iPLA2β except at high doses of 20-30 μM. (R)-BEL inhibits human recombinant iPLA2γ with an IC50 of approximately 0.6 μM.
β-Endorphin (1-27) is an endogenous peptide that binds to μ-, δ-, and κ-opioid receptors (Kis = 5.31, 6.17, and 39.82 nM, respectively, in COS-1 cells expressing rat receptors). It binds to rat and mouse brain membrane preparations (IC50s = 1.1 and 5.7 nM, respectively) and induces chemotaxis of human monocytes in vitro when used at a concentration of 1 nM. Intracerebroventricular administration of β-endorphin (1-27) increases the latency to tail withdrawal in response to thermal stimulation in mice with a median antinociceptive dose (AD50) of 1,500 pmol per animal. It inhibits antinociception induced by β-endorphin in mice in response to thermal stimuli when administered at a dose of 65 pmol per animal. In rats, β-endorphin (1-27) does not affect drug-associated place preference when administered at doses up to 20 μg, i.c.v., but inhibits β-endorphin-induced place preference when administered at a dose of 10 μg per animal.
Ligustrazine Hydrochloride, is a natural substance discovered in the plant Ligusticum chuanxiong Hort. It inhibits platelet aggregation, improves atherosclerosis situation, protects endothelium injury, and has antithrombotic effects.in vivo,ligustrazine hydrochloride at 10 and 20 mg/kg produced significant analgesic effects against mechanical stimuli,and ligustrazine hydrochloride at 80 mg/kg, also significantly alleviated cold hypersensitivity manifested by reduction in cold vocalization temperature.
CY208-243 is a D1 agonist. CY208-243 attenuates the pattern electroretinogram to low spatial frequency stimuli in the monkey. CY208-243 stimulates adenylate cyclase in rat striatal homogenates with an EC50 of 125 nM. CY208,243 was superior in improving the strength of neuronal outcome sensitivity to the working memory-related choice behavior in the T-maze.