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  Multiple ligands: cannab-PPAR, cannab-opioid
 

Designed multiple ligands are compounds with a well-defined multi-target profile to distinguish them from nonselective (or "dirty") drugs. They are of particular relevance in highly complex diseases such as those related to metabolism and the central nervous system (CNS).

Thus the aim of this project is to incorporate two activities into a single lead molecule by linking, fusing or merging two pharmacophore groups of PPAR, cannabinoid, and opioid ligands and study them for obesity, pain, and other complex diseases. The picture summarises the three strategies we are applying. The two circles represent two different pharmacophores.

 
Multiple Ligands
 

References:

 

- Perez-Fernandez, R.; Fresno, N.; Macias-Gonzalez, M.; Elguero, J.; Decara, J.; Giron, R.; Rodriguez-Alvarez, A.; Martin, M.I.; Rodriguez de Fonseca, F.; Goya, P.
“Discovery of Potent Dual PPARa Agonists/CB1 Ligands”  
ACS Med. Chem. Lett. 2011, 2(11), 793-797.

 

- Goicoechea, C., Sanchez, E., Cano, C., Jagerovic, N., Martín, M. I.

Analgesic activity and pharmacological characterization of N-[1-phenylpyrazol-3-yl]-N-[1-(2-phenethyl)-4-piperidyl] propenamide, a new opioid agonist acting peripherally

Eur. J. Pharm.  2008, 595, 22-29.

 

- Dardonville, C., Fernández-Fernández, C., Gibbons, S.L., Ryan, G. J., Jagerovic, N., Gabilondo, A., Meana, J. J., Callado, L. F.
Synthesis, binding and in vivo studies of new hybrid derivatives of fentanyl active at the mu-opioid receptor and I2;-imidazoline binding sites.
Bioorg. Med. Chem. 2006, 14, 6570-6580.

 

- Dardonville. C., Jagerovic, N., Callado, L. F., Meana, J.
Fentanyl derivatives bearing aliphatic alkaneguanidinium moieties: a new series of hybrid molecules with significant binding affinity for mu-opioid receptors and I-2-imidazoline binding sites.
Bioorg. Med. Chem. Lett. 2004, 14, 491-493.

 

Patents:

• Rodríguez de Fonseca F., Macias M., Serrano A., Goya P., Alvarado M., Elguero J., Jagerovic N.

"Dual peroxisome proliferator activated receptor alpha (PPAR alpha)/cannabinoid receptor ligands"

Application number: ES200702691, WOES000653, WO2009050318

(Titular entity: Fundación IMABIS/CSIC

 

• Jagerovic N., Fernández Fernández C., Goya P., Callado L. F., Meana J. J.

"Pyrazolecarboxamide derivatives, method of obtaining same and use thereof as inverse antagonists/agonists of the cannabinoid CB1 and opioid m receptor"

Application number: ES2289888; WO2006ES70132; ES20050002196; WO2007028849

(Titular entity: CSIC/UPV)