Baogongteng A (BGT-A), a naturally occurring tropane muscarinic agonist isolated from Chinese medicinal plant, exhibits a bioactive effect different from those of many tropane alkaloids that are muscarinic antagonists. A series of racemic derivatives of BGT-A was synthesized to study the structure-activity relationships (SAR). To explore further the SAR in this series and to ultimately design m...

The relative lack of specificity of atropine as a competitive antagonist of muscarinic receptors is a frequent cause of undesirable parasympathetic side effects. Consequently, new tropane alkaloids with potentially greater selectivity are usually seen with real interest. The cholinergic antagonistic effects of a purified mixture of tropane alkaloids extracted from Schizanthus hookeri were evalu...

The alpha7 nicotinic acetylcholine receptor (nAChR)-selective partial agonist tropisetron is a conjugate of an indole and a tropane group. We tested compounds structurally related to either the indole or tropane domains of tropisetron on oocytes expressing human alpha7. alpha4beta2, or alpha3beta4 nAChR or rat 5HT(3A) receptors. The simple compounds tropane and tropinone had alpha7-selective ag...

Secondary metabolites of Solanaceae plants, sharing tropane skeleton as a common structural feature, are sharply divided into two classes: tropine and ecgonine derivatives. The first group, represented by well known alkaloids: atropine and scopolamine, which are considered to be model anticholinergic drugs, continues to provide inspiration in the search for more selective muscarinic receptor an...

Toxic shock syndrome toxin 1 (TSST-1), produced by Staphylococcus aureus (including methicillin-resistant S. aureus), is a superantigenic toxin responsible for toxic shock syndrome as well as neonatal TSS-like exanthematous disease. TSST-1 exhibits its deleterious effects by leading to the abnormal proliferation of, e.g., Vbeta2+ T cells and overproduction of proinflammatory cytokines. In the p...

Cocaine is a tropane alkaloid that is obtained from the leaves of the coca plant. It has a small number of legitimate medical applications. Historically, it was useful as a topical anesthetic in eye and nasal surgery, although it is now predominantly used for nasal and lacrimal duct surgery. From numerous studies it is known that it causes irreversible structural changes on the brain, heart and...

Cocaine and amphetamines (‘stimulants’) are distinct central nervous system stimulants with similar effects (Pleuvry, 2009; Holman, 1994). Cocaine is a crystalline tropane alkaloid extracted from coca leaves. Amphetamines are a subclass of phenylethylamines with primarily stimulant effects, including amphetamine, methamphetamine, methcathinone and cathinone and referred to as ‘amphetamines’ in ...

hallucinations is unusual for intoxication with atropine or scopolamine, but could be explained by delayed digestion of non-ground Jimson weed seeds. Postprandial ‘inability to vomit’, followed by unconsciousness and auditory hallucinations, as reported by this patient, clearly is consistent with tropane alkaloid poisoning, and, together with laboratory results (50 seeds D. stramonium/kg of gra...