04 March 2024
Orexins or hypocretins are two neuropeptides (OX-A and OX-B) that are synthesized in the hypothalamus, and serve as ligands for the G protein-coupled receptors OX1 and OX2. While the role of orexins was initially thought to be limited to the regulation of circadian rhythms, the identification of orexinergic neurons in diverse brain regions, such as the amygdala, hypothalamus, lateral hypothalamic area, and ventral tegmental area of the midbrain, has led to re-evaluation of their function. Indeed, recent research suggests that orexins may also be involved in the control of a wide range of behaviors, including emotion, reward, and panic among others.
While orexin A is able to bind both OX1 and OX2, orexin B is specific to OX2, implying that the two receptors have at least partially distinct functions. Therefore, the development of selective synthetic inhibitors is crucial for further elucidating their biological role. BI-5121 is a highly potent and selective OX1 antagonist suitable for in vivo use, developed through combined structural biology and medicinal chemistry approaches.
You can now study the signaling mechanisms of type 1 orexin receptors with BI-5121, available free of charge on opnMe. Ordering BI-5121 does not subject you to any intellectual property limitations as you retain full ownership and control of your results, which we encourage you to publish.
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About BI-5121:
BI-5121 is a highly potent and selective OX1 antagonist displaying IC50 values of 1.6 nM and 62.6 nM in human orexin receptor type 1 and orexin receptor type 2 IPOne Homogeneous Time Resolved Fluorescence assays respectively. Its in vivo efficacy has been demonstrated in the behavioral 5-choice serial reaction time impulsivity task in Lister Hooded rats. BI-6199, a structurally very close analogue, is available as a negative control.
About opnMe:
opnMe.com, the open innovation portal of Boehringer Ingelheim, fosters science and collaboration initiatives in areas of high unmet medical need. As part of our first pillar, the “Molecules to Order”, we share well-characterized tool compounds free of charge with no IP strings attached. These are complemented by “Molecules for Collaboration” where we offer access to unprecedented, often unpublished molecules, together with an attractive funding package. Interested scientists are invited to submit testable research hypotheses with these assets. With our “opn2EXPERTS” program, we enlist scientific advice on key biologic issues to fuel further drug discovery and deliver novel solutions that benefit unmet patient needs, such as our recent call on “unraveling the role of AGR2 in lung fibrosis”.