An α7 nicotinic acetylcholine receptor sequence was cloned from Rhesus monkey (Macaca mulatta). This clone differs from the mature human α7 nicotinic acetylcholine receptor in only four amino acids, two of which are in the extracellular domain. The monkey α7 nicotinic receptor was characterized in regard to its functional responses to acetylcholine, choline, cytisine, and the experimental α7-se...

Activation of cortical nicotinic receptors by cholinergic axons from the basal forebrain (BF) significantly impacts cortical function, and the loss of nicotinic receptors is a hallmark of aging and neurodegenerative disease. We have previously shown that stimulation of BF axons generates a fast α7 and a slow non-α7 receptor-dependent response in cortical interneurons. However, the synaptic mech...

The recent discovery of the G(i) protein-coupled receptor GPR109A (HM74A in humans; PUMA-G in mice) as a receptor for nicotinic acid has provided the opportunity to gain greater understanding of the underlying biology contributing to the clinical efficacy (increases in HDL, decreases in VLDL, LDL, and triglycerides) and the characteristic side-effect profile of nicotinic acid. GPR109A has been ...

lbogaine noncompetitively blocked (IC,, 20 nM) “NaCI influx partially reversible in PC12 ceils. In viva, ibogaine at 10 mg/kg through ganglionic-type nicotinic receptor channels of rat completely blocked epibatidine-elicited antinociception in rheochromocytoma PC1 2 cells. The major metabolite O-desmice, a response that is mediated by central nicotinic receptor ;I-~ethylibogaine was 75fold less...

Ibogaine noncompetitively blocked (IC50 approximately 20 nM) 22NaCl influx through ganglionic-type nicotinic receptor channels of rat pheochromocytoma PC12 cells. The major metabolite O-des-methylibogaine was 75-fold less active, and O-t-butyl-O-des-methylibogaine was 20-fold less active. Ibogaine was relatively weak as a blocker (IC50 approximately 2000 nM) of the neuromuscular-type nicotinic ...

In this study, we present the identification and characterization of hamster and guinea pig nicotinic acid receptors. The hamster receptor shares approximately 80-90% identity with the nucleotide and amino acid sequences of human, mouse, and rat receptors. The guinea pig receptor shares 76-80% identity with the nucleotide and amino acid sequences of these other species. [(3)H]nicotinic acid bin...

Abstract— In screening the venoms of various snake species, we found that venom Madagascar cat-eyed Madagascarophis colubrinus competes with α-bungarotoxin for binding to nicotinic acetylcholine receptor from Torpedo californica . Using liquid chromatography, a peptide inhibits α‑bungartoxin this was isolated and named macoluxin. The amino acid sequence 23-amino determined by automatic Edman de...

Nicotinic acid has been used clinically for over 40 years in the treatment of dyslipidemia producing a desirable normalization of a range of cardiovascular risk factors, including a marked elevation of high density lipoprotein and a reduction in mortality. The precise mechanism of action of nicotinic acid is unknown, although it is believed that activation of a G(i)-G protein-coupled receptor m...

Multiple lines of evidence, from molecular and cellular to epidemiologic, have implicated nicotinic transmission in the pathology of Alzheimer's disease. In this review we present evidence for nicotinic receptor-mediated protection against beta-amyloid and glutamate neurotoxicity, and the signal transduction involved in this mechanism. The data are based mainly on our studies using rat-cultured...

Previous studies have shown that nicotinic cholinergic agonists induce muscle cell degeneration. Although an involvement of calcium is well documented, subsequent intracellular steps have not been identified. The present experiments test whether nitric oxide (NO) may play such a role. Both the irreversible nitric oxide synthase inhibitor L-5N-iminoethyl ornithine and L-nitroarginine methyl este...