Brucine

About: Brucine is a research topic. Over the lifetime, 586 publications have been published within this topic receiving 6866 citations. The topic is also known as: 10,11-dimethoxy strychnine.

Subtype-selective positive cooperative interactions between brucine analogs and acetylcholine at muscarinic receptors: functional studies.

Abstract: In radioligand binding studies, it has been reported that brucine, N-chloromethyl brucine, and brucine N-oxide increased the affinity of acetylcholine for M1, M3, and M4 muscarinic receptors, respectively, in a manner consistent with the predictions of the ternary complex allosteric model. We now demonstrate an equivalent ability of these three allosteric agents to modulate the actions of acetylcholine in functional studies in membranes and in whole cells. The enhancing actions of brucine and brucine N-oxide on acetylcholine (ACh) potency at M1 and M4 receptors respectively have been confirmed in guanosine-5'-O-(3-[35S]thio)triphosphate, GTPase, cAMP, and intracellular Ca2+ mobilization assays of function. In general, neither the basal nor the maximally stimulated response to ACh is affected. The subtype-selective allosteric effects of N-chloromethyl brucine on M2 and M3 receptors were shown to be qualitatively and quantitatively the same in guanosine-5'-O-(3-[35S]thio)triphosphate functional assays, in terms of both its affinity and cooperativity with ACh, as those found in binding assays. Neutral cooperativity of N-chloromethyl brucine with ACh on M4 receptor function was also observed, thereby demonstrating its "absolute subtype selectivity": a lack of action at any concentration at M4 receptors and an action at M2 and M3 receptors. The enhancing action of N-chloromethyl brucine on neurogenically released ACh binding at M3 receptors was also detected in whole tissue as an increased contraction of the isolated guinea pig ileum to submaximal electrical stimulation. In conclusion, these functional studies confirm that brucine analogs are allosteric enhancers of ACh affinity at certain muscarinic receptor subtypes.

Cholesteric states of micellar solutions

Abstract: The effects of optically active compounds on amphiphilic nematics are reported. The following systems have been studied : (1) caesium decylsulphate, decanol, water plus tartaric acid ; (2) ammonium decylsulphate, ammonium sulphate, decanol, water plus brucine sulphate ; and (3) decylammonium chloride, water plus cholesterol. Phase transitions to cholesteric states are induced by the optically active compounds in all systems. Brucine sulphate has the highest twisting power ; tartaric acid the lowest. The results are analysed on the basis of intermolecular interactions and an explanation is proposed for the observed differences in twisting power.