PF-5006739 is an effective and selective inhibitor of CK1δ ε (IC50s: 3.9 nM and 17.0 nM, respectively). PF-5006739 is a potential therapeutic agent for a range of psychiatric disorders with low nanomolar in vitro potency for CK1δ ε and high kinome selecti
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
ABD459 is a neutral antagonist of the central cannabinoid 1 (CB1) receptor (Ki = 8.6 nM). It inhibits food consumption in nonfasted mice without affecting motor activity. ABD459 reduces active food seeking for 5-6 hours after treatment, with no rebound after washout. ABD459 also diminishes rapid eye movement (REM) sleep, with no alterations of wakefulness or non-REM sleep.
AT-1001 is an α3β4 nAChR partial agonist. AT-1001 attenuates stress-induced reinstatement of nicotine seeking in a rat model of relapse and induces minimal withdrawal in dependent rats. AT-1001 also potently and reversibly blocks epibatidine-induced inward currents in HEK cells transfected with α3β4 nAChR. Importantly, AT-1001 potently and dose-dependently blocks nicotine self-administration in rats, without affecting food responding. When tested in a nucleus accumbens (NAcs) synaptosomal preparation, AT-1001 inhibits nicotine-induced [³H]dopamine release poorly and at significantly higher concentrations compared with mecamylamine and conotoxin MII.
AZD-8418 is an mGlu2 receptor positive allosteric modulators that attenuates nicotine-taking and nicotine-seeking behavior. Acute treatment with AZD8418 (0.37, 1.12, 3.73, 7.46, and 14.92 mg kg) and AZD8529 (1.75, 5.83, 17.5, and 58.3 mg kg) deceased nicotine self-administration and had no effect on food-maintained responding. Chronic treatment with AZD8418 attenuated nicotine self-administration, but tolerance to this effect developed quickly. The inhibition of nicotine self-administration by chronic AZD8529 administration persisted throughout the 14 days of treatment. Chronic treatment with either PAMs inhibited food self-administration. AZD8418 (acute) and AZD8529 (acute and subchronic) blocked cue-induced reinstatement of nicotine- and food-seeking behavior.
[Glp5,(Me)Phe8,Sar9] Substance P (5-11) (DiMe-C7) 是一种 Substance P 类似物,在大鼠大脑中对神经激肽 1 受体 (NK1R) 的作用与 Substance P 大致相等,但作用时间大大延长。[Glp5,(Me)Phe8,Sar9] Substance P (5-11) 能选择性地激活大鼠大脑间脑和中脑皮层的多巴胺代谢。[Glp5,(Me)Phe8,Sar9] Substance P (5-11) 还可增加大鼠运动活性,诱导成瘾剂寻求行为的恢复。