Substituted 1-phenyl-2-cyclopropylmethylamines with high affinity and selectivity for sigma sites

…, A Marrazzo, O Prezzavento, L Pasquinucci…

Index: Ronsisvalle, Giuseppe; Marrazzo, Agostino; Prezzavento, Orazio; Pasquinucci, Lorella; Falcucci, Barbara; Di Toro, Rosanna; Spampinato, Santi Bioorganic and Medicinal Chemistry, 2000 , vol. 8, # 6 p. 1503 - 1513

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Citation Number: 23

Abstract

A series of 1-phenyl-2-cyclopropylmethylamines structurally related to (+)-and (−)-MPCB were synthesized and their binding affinities for σ1, σ2, opioid and dopamine (D2) receptors were evaluated. Substitution of the cis-N-normetazocine with different aminic moieties provided compounds with high affinity and selectivity for σ binding sites with respect to opioid and dopamine (D2) receptors. The observed increase in σ2 affinity as compared to ...