chapter  11
12 Pages

Lobeline: A Natural Product with High Affinity for Neuronal Nicotinic Receptors and a Vast Potential for Use in Neurological Disorders*

Neuronal nicotinic acetylcholine receptors (nAChRs) have initiated a flurry of research in the past decade with such therapeutic targets as Alzheimer’s disease (AD), Parkinson’s disease (PD), anxiety, smoking cessation, attention deficit hyperactivity disorder (ADHD), Tourette’s syndrome (TS), schizophrenia, and analgesia. The agents acting via these receptors have been termed cholinergic channel modulators (ChCMs). This is due, in part, to the broad diversity of pharmacological activity associated with the central cholinergic nervous

system and the numerous possibilities of receptor subtypes. As a result of this vast arrangement of subtypes there is an ongoing effort to elucidate the pharmacology associated with each known subtype. For this to become a reality, new compounds must be obtained with specificity for these receptors. Lobeline (1, Figure 11.1), the major alkaloid found in the plant Lobelia inflata, has been reported to bind with high affinity to nicotinic receptors1 and elicit a diverse array of pharmacological activities.2