Synthesis and pharmacological evaluation of some (pyridyl)cyclopropylmethyl amines and their methiodides as nicotinic receptor ligands.

Guandalini, Luca; Dei, Silvia; Manetti, Dina; Romanelli, Maria Novella; Scapecchi, Serena; Teodori, Elisabetta; Varani, K.

A series of 3- and (4-pyridyl)cyclopropylmethyl amines and their quaternary ammonium derivatives have been synthesized; they can be considered as rigid analogues of nicotine. The compounds have been tested on rat cerebral cortex to measure the affinity for the central nicotinic receptor. Only the methiodides show affinity in the micromolar range. The results obtained can provide useful information on the topography of the nicotinic receptor-binding site.

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Titolo:	Synthesis and pharmacological evaluation of some (pyridyl)cyclopropylmethyl amines and their methiodides as nicotinic receptor ligands.
Autori di Ateneo:	GUANDALINI, LUCA DEI, SILVIA MANETTI, DINA ROMANELLI, MARIA NOVELLA SCAPECCHI, SERENA TEODORI, ELISABETTA K. VARANI mostra contributor esterni nascondi contributor esterni
Autori:	GUANDALINI, LUCA; DEI, SILVIA; MANETTI, DINA; ROMANELLI, MARIA NOVELLA; SCAPECCHI, SERENA; TEODORI, ELISABETTA; K. VARANI
Data di pubblicazione:	2002
Rivista:	IL FARMACO
Volume:	57
Pagina iniziale:	487
Pagina finale:	496
Abstract:	A series of 3- and (4-pyridyl)cyclopropylmethyl amines and their quaternary ammonium derivatives have been synthesized; they can be considered as rigid analogues of nicotine. The compounds have been tested on rat cerebral cortex to measure the affinity for the central nicotinic receptor. Only the methiodides show affinity in the micromolar range. The results obtained can provide useful information on the topography of the nicotinic receptor-binding site.
Handle:	http://hdl.handle.net/2158/312482
Appare nelle tipologie:	1a - Articolo su rivista

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