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Guanidinium and aminoimidazolinium derivatives of N-(4-piperidyl)propanamides as potential ligands for mu opioid and I-2-imidazoline receptors: Synthesis and pharmacological screening

AuthorsMontero, Ana; Goya, Pilar ; Jagerovic, Nadine ; Callado, Luis F.; Meana, J. Javier; Girón, Rocío; Goicoechea, Carlos; Martín, M. Isabel
Issue DateApr-2002
PublisherPergamon Press
CitationBioorganic & Medicinal Chemistry 10 : 1009–1018 (2002)
AbstractDerivatives of N-(1-phenethyl-4-piperidyl)propanamides incorporating guanidinium and 2-aminoimidazolinium groups have been prepared by a synthetic approach involving first introduction of a spacer between the piperidine and the functional group by reductive amination of piperidinone. The formation of each of these functional groups was carried out using N-N0-di(tertbutoxycarbonyl) thiourea and 2-methylthioimidazolinium iodide, respectively. These structures have been designed to incorporate two pharmacologic goals into one entity. Radioligand binding assays have been used to study their affinity for opioid (m, d and k) and I2-imidazoline receptors. Two of them, 10 and 16, showed high affinity for m opioid receptors and functionally they had moderate analgesic properties in the hot plate and writhing tests. The in vitro studies on guinea pig ileum (GPI) indicated that both compounds are m opioid agonists. In what concerns I2-imidazoline receptor activity, these derivatives showed low affinity around 6 to 7 times less than idazoxan.
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