Sigma receptors modulate nicotinic receptor function in adrenal chromaffin cells

  title={Sigma receptors modulate nicotinic receptor function in adrenal chromaffin cells},
  author={Ian A. Paul and Anthony S. Basile and Eduardo Rojas and Moussa B. H. Youdim and B de Costa and Phil Skolnick and Harvey B Pollard and Gemma A. J. Kuijpers},
  journal={The FASEB Journal},
  pages={1171 - 1178}
Neither the physiological function of sigma (σ) receptors nor the cellular mechanism responsible for the pharmacological effects of σ receptor ligands is known. We now report that σ receptor ligands noncompetitively inhibit nicotine‐stimulated catecholamine release from bovine adrenal chromaffin cells in a concentration‐dependent and reversible manner. The rank order of potency of ligands to inhibit nicotine‐stimulated catecholamine release is significantly correlated (P < 0.005) with that… Expand
Sigma‐1 receptor ligands inhibit catecholamine secretion from adrenal chromaffin cells due to block of nicotinic acetylcholine receptors
SSRIs and other sigma‐1 receptor ligands inhibit secretion evoked by cholinergic stimulation because of direct block of Ca2+entry via nAChRs, suggesting that s Sigma‐1 receptors do not acutely regulate catecholamine secretion. Expand
Inhibitory effect of strychnine on acetylcholine receptor activation in bovine adrenal medullary chromaffin cells
It is suggested that strychnine interacts with the agonist binding site of the nicotinic acetylcholine receptor in chromaffin cells, thus exerting a pharmacological effect independently of the glycine receptor. Expand
Ibogaine acts at the nicotinic acetylcholine receptor to inhibit catecholamine release 1 Published on the World Wide Web on 8 May 1998. 1
Evidence is provided for a mechanism of action ibogaine at the nicotinic ACh receptor which is consistent with a model in which the initial high transient brain concentrations of Ibogaine act at multiple cellular sites and then have a selective action at the Nicotinic receptor cation channel following its metabolism to lower brain concentrations. Expand
Apparent desensitization of a σ receptor sub-population in neonatal rat cardiac myocytes by pre-treatment with σ receptor ligands
It is suggested that the effects of σ receptor ligands are mediated via two receptor subtypes, one stimulatory and the other inhibitory, and only the inhibitory subtype is subject to desensitization. Expand
Possible expression of a σ1 site in rat pheochromocytoma (PC12) cells
Abstract To examine the functional interaction between the σ binding sites and nicotinic acetylcholine receptors, we investigated the effects of various σ receptor ligands on nicotine-evoked Ca 2+Expand
Agonists and Antagonists of Nicotinic Acetylcholine Receptors
The natural alkaloids nicotine and muscarine (Fig. 1) were the key pharmacologic tools that uncovered the two families of acetylcholine (ACh) receptors in the CNS. These families were defined by theExpand
Neuroprotective and anti-amnesic potentials of sigma (σ) receptor ligands
Abstract 1. 1. Although the physical nature of sigma (σ) receptors have not yet been fully defined, several classes of selective ligands have been characterised, demonstrating a plethora ofExpand
Sigma receptors [σRs]: biology in normal and diseased states
This review of the literature examines the mechanism of action of the σRs, their interaction with neurotransmitters, pharmacology, location and adverse effects mediated through them. Expand
sigma Receptor Activation Does Not Mediate Fentanyl-Induced Attenuation of Muscarinic Coronary Contraction
Neither sigma nor opioid receptoractivation is a prerequisite for fentanyl-induced inhibition of muscarinic coronary contraction, and the effects of inhibiting various points in the signal transduction pathway distal to naloxone-sensitive opioid receptor activation on acetylcholine-induced contraction are assessed. Expand
Differential effects of cytochrome P-450 induction on ligand binding to σ receptors
The identity of the sigma receptor as a form of cytochrome P-450 was investigated in rats treated with 3-methylcholanthrene or phenobarbital. The density of [3H]N,N'-di(o-tolyl)guanidine (DTG)Expand


Sigma receptors. Putative links between nervous, endocrine and immune systems.
  • T. Su
  • Biology, Medicine
  • European journal of biochemistry
  • 1991
The sigma receptor is a neuronal substrate that binds several psychoactive compounds. These include cocaine, some steroids, dextromethorphan, phencyclidine (PCP), and benzomorphans such asExpand
Naloxone-inaccessible sigma receptor in rat central nervous system.
  • S. Tam
  • Chemistry, Medicine
  • Proceedings of the National Academy of Sciences of the United States of America
  • 1983
It has been postulated that the psychotomimetic effects of opiates of the benzomorphan series are due to their activity at the sigma receptor, and the drug selectivity and regional distribution of this sigma binding site in the rat central nervous system are different from that of the mu and delta opioid receptors and phencyclidine receptors. Expand
Neuropeptide Y inhibits the nicotine-mediated release of catecholamines from bovine adrenal chromaffin cells.
The possible role of neuropeptide Y (NPY) in catecholamine secretion was studied by using bovine adrenal chromaffin cells. NPY produced a concentration-dependent inhibition of nicotine-stimulatedExpand
Evidence for a role of haloperidol‐sensitive σ‐'opiate' receptors in the motor effects of antipsychotic drugs
Haloperidol exhibits a high affinity for a subclass of σ-"opiate" binding sites which have a unique anatomic distribution and a unique drug selectivity pattern, which suggest that σ-binding sites represent biologically functional receptors that are active in the neural control of movement. Expand
Biochemical, behavioral, and electrophysiologic actions of the selective sigma receptor ligand (+)-pentazocine.
Pharmacologic actions for the selective sigma receptor ligand (+)-pentazocine are demonstrated and some overlapping pharmacologic properties of the sigma and PCP receptor sites despite differences in central nervous system distribution are suggested. Expand
Presence of sigma and phencyclidine (PCP)-like receptors in membrane preparations of bovine adrenal medulla.
The binding of [3H]-(+)SKF-10047 to both receptors showed marked stereoselectivity for the dextrorotatory (+) isomer of SKF- 10047 and was insensitive to the receptor specific opioid ligands DAGO (mu), DSLET (delta) and U-69593 (kappa). Expand
Autoradiographic visualization of haloperidol-sensitive sigma receptors in guinea-pig brain
The anatomical distribution of the haloperidol-sensitive sigma receptors is distinct from the pattern of phencyclidine receptors and suggests sigma compounds may effect endocrine, emotional and motor behavior. Expand
Role of intracellular pH in secretion from adrenal medulla chromaffin cells.
It is concluded that the pH of the chromaffin granule modulates secretion by affecting some step in the secretory process unrelated to the rise in [Ca2+]i. Expand
Kinetic characterization of the phencyclidine-N-methyl-D-aspartate receptor interaction: evidence for a steric blockade of the channel.
The nature of the interactions between the N-methyl-D-aspartate (NMDA) and the phencyclidine (PCP) receptors was studied in membranes obtained from rat cerebral cortex and washed repeatedly to removeExpand
The effects of morphine- and nalorphine- like drugs in the nondependent and morphine-dependent chronic spinal dog.
It has been shown that buprenorphine is a partial agonist of the mu type which both suppressed and precipitated abstinence in the morphine-dependent dog while morphine and propoxyphene are stronger agonists. Expand