Novel ligands rationally designed for characterizing I2-imidazoline binding sites nature and functions.
The study of two series of 2-aryl-ethylen-imidazolines 3-7 and 8-12 inspired by I2-IBS ligands phenyzoline (1) and diphenyzoline (2), respectively, confirmed the interesting "positive" or "negative" morphine analgesia modulation displayed by their corresponding leads and demonstrated that these effects might be correlated with morphine tolerance and dependence, respectively. By comparative examination of rationally designed compounds, some analogies between binding site cavity of I2-IBS proteins and alpha 2C-adrenoreceptor emerged.
Gentili
Francesco
F
Dipartimento di Scienze Chimiche, Università degli Studi di Camerino, via S. Agostino 1, 62032 Camerino, Italy.
Cardinaletti
Claudia
C
Vesprini
Cristian
C
Ghelfi
Francesca
F
Farande
Aniket
A
Giannella
Mario
M
Piergentili
Alessandro
A
Quaglia
Wilma
W
Mattioli
Laura
L
Perfumi
Marina
M
Hudson
Alan
A
Pigini
Maria
M
D000700:Analgesics / Q000494:pharmacology; D000818:Animals; D015195:Drug Design; D007093:Imidazoles / Q000138:chemical synthesis / Q000378:metabolism*; D054755:Imidazoline Receptors / Q000737:chemistry* / Q000502:physiology*; D048288:Imidazolines / Q000737:chemistry* / Q000494:pharmacology; D008024:Ligands; D051379:Mice; D009020:Morphine / Q000494:pharmacology; D010146:Pain / Q000188:drug therapy; D051381:Rats; D018341:Receptors, Adrenergic, alpha-2 / Q000187:drug effects
D000700:Analgesics; D007093:Imidazoles; D054755:Imidazoline Receptors; D048288:Imidazolines; D008024:Ligands; D018341:Receptors, Adrenergic, alpha-2; D009020:Morphine