| 摘要 |
Compounds, pharmaceutical compositions including the compounds, and metho ds of preparation and use thereof are disclosed. The compounds are amide, ke tone, and ester compounds prepared from certain azabicycloalkane carboxylic acids. The resulting compounds exhibit selectivity for, and bind with high a ffinity to, neuronal nicotinic receptors of the a4ß2 subtype in the central nervous system (CNS). The compounds and compositions can be used to treat an d/or prevent a wide variety of conditions or disorders, such as those disord ers characterized by dysfunction of nicotinic cholinergic neurotransmission, including disorders involving neuromodulation of neurotransmitter release, such as dopamine release. CNS disorders, which are characterized by an alter ation in normal neurotransmitter release, are another example of disorders t hat can be treated and/or prevented. The compounds can: (i) alter the number of nicotinic cholinergic receptors of the brain of the patient, (ii) exhibi t neuroprotective effects, and (iii) when employed in effective amounts, not result in appreciable adverse side effects (e.g. side effects such as signi ficant increases in blood pressure and heart rate, significant negative effe cts upon the gastrointestinal tract, and significant effects upon skeletal m uscle).
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