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.