orexin 1 receptor

Orexin Receptor Activator-1 is an agonist for the orexin receptor (Orexin Receptor). It is utilized in the research of orexin-related disorders.

Orexin Receptor Modulator-1 is a compound utilized in the study of various conditions including substance addiction, panic disorder, anxiety, post-traumatic stress disorder (PTSD), pain, depression, seasonal affective disorder (SAD), eating disorders, and hypertension [1].

JNJ-54717793 is an orally active, brain-penetrating compound that acts as a selective and high-affinity antagonist of the orexin-1 receptor (OX1R) with a plasma EC50 of 85 ng mL. It demonstrates K_i values of 16 nM for hOX1R (human OX1R) and 700 nM for hOX2R, indicating its strong preference for hOX1R over hOX2R. JNJ-54717793 is recognized for its effectiveness in the treatment of anxiety disorders.

Orexin B, rat, mouse Acetate (Rat orexin B) is an endogenous agonist at Orexin receptor with Kis of 420 and 36 nM for OX1 and OX2, respectively.

GSK1059865 is a potent antagonist of the orexin 1 receptor.

(R)-YNT-3708 is a specific Orexin 1 receptor (OX1R) agonist with an EC50 value of 7.48 nM for OX1R. The EC50 ratio of OX2R to OX1R is 22.5. This compound demonstrates analgesic and enhancing effects by activating OX1R in mice.

ACT-335827 is an orally available, brain-penetrant, orexin type 1 receptor-selective antagonist, with IC50 values of 6 nM for OXR1 and 417 nM for OXR2. It is suitable for studies related to neurological disorders [1].

Almorexant (ACT 078573) is a potent and competitive dual orexin 1 receptor (OX1) orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM for OX1 and OX2, respectively.

ACT-462206 is an orally available Orexin 1 Orexin 2 receptor antagonist that crosses the blood-brain barrier.ACT-462206 is highly potent and can be used in studies of sleep and anxiety.

TCS 1102 is an effective, dual orexin receptor antagonist (Ki: 0.2 3 nM for OX2 1 receptors).

MK-1064 (Urokinase inhibitor 1) is a selective orexin 2 receptor antagonist (2-SORA).

Orexin Receptor Antagonist 2 (compound 30), characterized by its potent antagonistic activity with pKis of 7.69 and 9.78, holds promise for insomnia research[1].

SB-334867 free base (SB334867A free base) is a selective antagonist of the orexin-1 (OX1) receptor.

Almorexant hydrochloride (ACT 078573 hydrochloride) is an orally active dual orexin receptor antagonist that blocks the intracellular Ca2+ signaling pathway and, to a certain extent, blocks the excitatory effects of methamphetamine. Almorexant hydrochloride Induces apoptosis and can be used to study sleep disorders.

HIV-1 inhibitor-40 (Compound 4ab), an HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI) with an EC50 of 1.9 nM, exhibits no significant acute toxicity in vivo and functions as a highly sensitive inhibitor of the orexin receptor antagonist CYP.

ORN-0829 hydrate is a potent dual orexin 1 2 receptor antagonist for the treatment of insomnia.

RTIOX-372 is a potent and selective orexin-1 receptor antagonist.

JNJ-61393215 is a novel selective orexin-1 receptor (OX1R) antagonist.

[Ala11,D-Leu15]-Orexin B(human) TFA is a potent, selective agonist for the orexin-2 receptor (OX2), demonstrating 400-fold higher selectivity for OX2 (EC50=0.13 nM) compared to the orexin-1 receptor (OX1) with an EC50 of 52 nM.

OXA(17-33) TFA is a potent and selective agonist for the orexin-1 receptor (OX1), with approximately 23-fold higher affinity for OX1 (EC50 = 8.29 nM) compared to the orexin-2 receptor (OX2) (187 nM) [1].

Orexin B, rat, mouse (Rat orexin B) TFA, an endogenous agonist for orexin receptors, binds to and activates the orphan G protein-coupled receptors OX1-R and OX2-R, playing a crucial role in stimulating food intake, increasing energy expenditure, and regulating sleep-wake cycles [1] [2] [3].

Hypocretin (70-98), human, is a polypeptide that binds to the orexin receptor OX1R and facilitates apoptosis [1].

Firazorexton hydrate (TAK-994) is a brain-penetrant, orally active agonist of the orexin type 2 receptor (OX2R) with a potent EC50 of 19 nM, effectively reducing wakefulness fragmentation and cataplexy-like episodes in mouse models of narcolepsy [1].

CVN766 is an orally active orexin 1 receptor antagonist with blood-brain permeability, demonstrating IC50 values of 8 nM for OX1R and >10 μM for OX2R. CVN766 can be used to study schizophrenia [1].