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A research team composed by researchers from three Spanish Universities has developed a new family of I2 Imidazoline Receptor ligands with anti-inflammatory and neuroprotective activity, opening a new therapeutic approach for Alzheimer’s disease treatment. The compounds are characterized by presenting considerably less cardiovascular side-effects compared to existing ones. A pharmaceutical company interested in developing an Alzheimer’s disease drug is being sought for a licensing agreement.
Alzheimer’s disease is the largest unmet medical need in neurology. Existing drugs have scarce or limited efficacy and no new cognitive enhancer drugs are available currently.
A new family of I2 Imidazoline Receptor ligands (compounds referred to as I2-IR ligands), selective against I2-IR and with potential less side-effects, has been developed by a research team composed by researchers from three Spanish Universities. The team has specialists in the area of synthesis of heterocyclic compounds with interest in the treatment of Alzheimer’s disease, neuropharmacology and neuropsychopharmacology.
The new family of synthetic compounds developed relates to the field of compounds with high affinity for imidazoline receptors of the I2-type, which have been associated with prevention or treatment of human brain disorders, such as depression and Alzheimer’s disease, pain modulation, and inflammation.
I2-IR are involved in physiologic processes related to analgesia, anti-inflammation and neuroprotection among others, which offers a wide range of applications for compounds targeting this type of proteins.
It is also known that in Alzheimer’s disease brain patients the density (Bmax) of I2 imidazoline binding sites is significantly higher than in control samples, and that I2-IR ligands have neuroprotectant properties. In this regard, other I2-IR ligands have been developed and tested, but most of them show cardiac side-effects due to their activity upon α2-adrenergic receptors (α2-AR).
Inspired in this rational, researchers focused their effort on developing compounds targeting selectively I2-IR; avoiding side-effects due to α2-AR activation and opening a new therapeutic approach for Alzheimer’s disease treatment.
However, given the nature of I2-IR, other indications may also be targeted, such as osteoarthritis pain.
- Potentially less cardiovascular side-effects.
- A new therapeutic approach for Alzheimer’s disease treatment with anti-inflammatory and neuroprotective activity.
This project is currently in a preclinical stage of development. In vitro and in vivo assays have been performed with the new family of compounds in order to evaluate:
• Activity and selectivity upon I2-IR (in vitro).
• Central Nervous System (CNS) penetration.
• Cognitive capabilities improvement in two murine models of neurodegeneration and brain disorders.
• Anti-inflammatory activity (in vivo assessment).
• Induction of amyloid precursor protein (APP) degradation (in vivo).
European Patent application filed on December 21st, 2017.
The research team seeks pharmaceutical companies in all countries engaged in the development of Alzheimer’s disease drugs and interested in a license agreement. The company should be able to continue the development of the invention as well as to perform dose-response, toxicity and side effects studies.