wakefulness

Bavisant (JNJ-31001074) 是一种特异性和口服活性的人 H3 受体拮抗剂。 Bavisant 可用于作用机制的研究，包括觉醒和认知以及 ADHD 的治疗。

9-FLUORENOL 是一种多巴胺再摄取抑制剂，IC50 为 9 µM，是一种化合物的主要代谢物，被开发为一种觉醒促进剂。

Bavisant (JNJ-310010740) dihydrochloride is a highly selective, orally active antagonist of the human H3 receptor with a novel mechanism of action, involving wakefulness and cognition.

Bavisant dihydrochloride hydrate (JNJ31001074AAC) is a highly selective, orally active antagonist of the human H3 receptor with a novel mechanism of action, involving wakefulness and cognition, with potential as a treatment for ADHD. in vivo: Mean change

Orexin 2 Receptor Agonist 3 是一种口服有效且能穿透大脑的食欲素受体 2 (OX2) 激动剂，具有 EC50 值为 2.5 nM。它能够增加 orexin/ataxin-3 NT1 小鼠模型和健康比格犬的清醒时间。该化合物可用于嗜睡症研究。

R06039-696 是一种神经肽 S 受体 (NPSR) 激动剂，EC50为 91 nM。R06039-696 通过激活神经肽 S 受体，参与调节觉醒、应激、焦虑反应、记忆过程和食物摄取等多种生物功能。

R06039-691 是一种神经肽 S 受体 (NPSR) 激动剂，EC50为93 nM。它通过激活NPSR参与调节觉醒、应激和焦虑反应、记忆过程及食物摄入等多种生物学功能。

Sunobinop (S 117957) TFA 是一种口服有效、可穿透 blood-brain barrier 的选择性 human nociceptin/orphanin FQ receptor (NOP) 部分激动剂，对人源靶点具有高亲和力 (Ki=3.3 nM；EC50=4.03 nM；Emax=47.8%)，且不激活 μ 和 κ opioid receptors。该化合物通过激活 NOP receptor 可显著缩短大鼠觉醒时间并增加 non-rapid eye movement sleep，在有效剂量下对学习、记忆、奖赏、呼吸及肠道功能未见明显副作用；同时在特定信号通路 (如β-Arrestin 2 recruitment) 中表现出竞争性拮抗剂特征，可用于失眠症、中重度 alcohol use disorder 及膀胱过度活动症相关尿失禁的研究。

Basimglurant (RG7090; RO4917523) sulfate 是一种可口服、具脑穿透性的选择性 mGluR5 负性变构调节剂，Ki 为 1.4 nM (对 [³H]-ABP688) 和 35.6 nM (对 [³H]-MPEP)。Basimglurant sulfate 可抑制 mGlu5 介导的信号通路及受体组成型活性，调节伏隔核多巴胺水平，具有抗焦虑、类抗抑郁、镇痛和促觉醒作用，并可改变非快速眼动睡眠的 δ 波功率，适用于抑郁症、脆性 X 综合征及焦虑症等研究。

Adrafinil, (R)- is the R isomer of Adrafinil -- a eugeroic that was formerly used to promote alertness, attention, wakefulness, mood, and other parameters, particularly in the elderly.

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.

Potent trace amine 1 (TA1) receptor agonist (EC50 values are 0.12, 35 and 17-85 nM for mouse, rat and human receptors, respectively). Increases wakefulness and reduces REM and NREM sleep duration in wild type mice. Inhibits spontaneous locomotor activity in dopamine transport (DAT) knockout mice. Espinoza et al (2018) Biochemical and functional characterization of the trace amine-associated receptor 1 (TAAR1) agonist RO5263397. Front.Pharmacol. 9 645 PMID:29977204 |Galley et al (2015) Discovery and characterization of 2-aminooxazolines as highly potent, selective, and orally active TAAR1 agonists. ACS.Med.Chem.Letts. 7 192 PMID:26985297 |Schwartz et al (2017) Trace amine-associated receptor 1 regulates wakefulness and EEG spectral composition. Neuropsychopharmacology. 42 1305 PMID:27658486

Irdabisant (CEP-26401) hydrochloride 是一种选择性、口服活性的组胺H3受体拮抗剂/逆激动剂，具备良好的血脑屏障渗透性。该化合物对大鼠和人类的H3受体具有高亲和力，其Ki值分别为7.2 nM和2.0 nM。此外，Irdabisant hydrochloride在抑制hERG电流方面表现出较低的活性，IC50为13.8 μM。在大鼠社会认知模型中，它展现了认知增强和唤醒的效果，可作为精神分裂症或认知障碍研究的潜在工具。

Paraxanthine-D6 is intended for use as an internal standard for the quantification of paraxanthine by GC- or LC-MS. Paraxanthine (T4973) is an active metabolite of caffeine. It is formed via N3-demethylation of caffeine by the cytochrome P450 (CYP) isoform CYP1A2. Paraxanthine (T4973) is an adenosine A1 and A2 receptor antagonist. In vivo,paraxanthine increases striatal cGMP and extracellular striatal dopamine levels and locomotor activity,as well as inhibits motor depression induced by the adenosine A1 agonist CPA or the adenosine A2 receptor agonist CGS 21680 in rats not habituated to caffeine. It also promotes wakefulness and increases locomotor activity and core temperature in narcoleptic transgenic mice without increasing behavioral anxiety.

Neuropeptide S(Mouse) TFA, an endogenous agonist for the neuropeptide S receptor (NPSR) with an EC50 value of 3 nM, plays a significant role in physiological processes by inducing the mobilization of intracellular Ca2+. This compound elevates locomotor activity and wakefulness, and simultaneously decreases anxiety-like behavior in mice.

Neuropeptide S(Rat) TFA, a robust endogenous agonist for the neuropeptide S receptor (NSPR) with an EC50 of 3.2 nM, enhances locomotor activity and promotes wakefulness while concurrently diminishing anxiety-like behavior in mice.

Firazorexton hydrate (TAK-994)为一种高效的食欲素2型受体(OX2R)激动剂，EC50值为19 nM。在发作性睡病小鼠模型中，该化合物能够有效减少觉醒碎片和猝倒样发作的发生。

RTIOXA-43是一种OX2R/OX1R（食欲素受体，orexin receptor）双重激动剂，可以增加清醒并减轻发作性睡症状，常用于嗜睡症和神经信号传导相关研究。

APD-916 是一种 H3 受体拮抗剂，具有优良的药代动力学特性。口服 APD-916 已被证明能提高多种动物模型的清醒程度。

Orexin B, human-13C6,15N (Human orexin B-13C6,15N) TFA 是经过13C 和 15N 标记的 Orexin B, human。这种化合物是食欲素受体 (Orexin Receptor, OX Receptor) 的激动剂，对 OXR1 和 OXR2 的 Ki 值分别为 420 nM 和 36 nM。Orexin B, human 在调节食欲、觉醒、心血管功能和神经内分泌方面起重要作用。

Orexin B, human-13C18,15N3 (Human orexin B-13C18,15N3) TFA 是通过13C 和13N 标记的 Orexin B, human。作为一种食欲素受体 (Orexin Receptor, OX Receptor) 的激动剂，该化合物对 OXR1 和 OXR2 的 Ki 分别为 420 nM 和 36 nM。Orexin B, human 在调节食欲、觉醒、心血管功能和神经内分泌方面发挥作用。

Potent endogenous neuropeptide S receptor (NPSR) agonist (EC50 = 3 nM). Induces mobilization of intracellular Ca2+. Increases locomotor activity and wakefulness in mice. Also reduces anxiety-like behavior in mice.

Potent endogenous neuropeptide S receptor (NSPR) agonist (EC50 = 3.2 nM). Increases locomotor activity and wakefulness in mice. Also reduces anxiety-like behavior in mice.

Potent endogenous neuropeptide S receptor agonist (EC50 = 9.4 nM). Increases locomotor activity and wakefulness in mice. Also reduces anxiety-like behavior in mice.