title: Novel ligands rationally designed for characterizing I2-imidazoline binding sites nature and functions.
abstract: 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.
authors.affiliation: Dipartimento di Scienze Chimiche, Università degli Studi di Camerino, via S. Agostino 1, 62032 Camerino, Italy.
authors.forename: Francesco
authors.initials: F
authors.lastname: Gentili
authors.forename: Claudia
authors.initials: C
authors.lastname: Cardinaletti
authors.forename: Cristian
authors.initials: C
authors.lastname: Vesprini
authors.forename: Francesca
authors.initials: F
authors.lastname: Ghelfi
authors.forename: Aniket
authors.initials: A
authors.lastname: Farande
authors.forename: Mario
authors.initials: M
authors.lastname: Giannella
authors.forename: Alessandro
authors.initials: A
authors.lastname: Piergentili
authors.forename: Wilma
authors.initials: W
authors.lastname: Quaglia
authors.forename: Laura
authors.initials: L
authors.lastname: Mattioli
authors.forename: Marina
authors.initials: M
authors.lastname: Perfumi
authors.forename: Alan
authors.initials: A
authors.lastname: Hudson
authors.forename: Maria
authors.initials: M
authors.lastname: Pigini
mesh_terms: 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
chemical_list: D000700:Analgesics; D007093:Imidazoles; D054755:Imidazoline Receptors; D048288:Imidazolines; D008024:Ligands; D018341:Receptors, Adrenergic, alpha-2; D009020:Morphine