*  Protein Kinase A Activation Down-Regulates, Whereas Extracellular Signal-Regulated Kinase Activation Up-Regulates σ-1 Receptors...
Snyder SH and Largent BL (1989) Receptor mechanisms in antipsychotic drug action: focus on sigma receptors. J Neuropsychiatry ... Hayashi T and Su TP (2003a) Sigma-1 receptors (sigma(1) binding sites) form raft-like microdomains and target lipid droplets on ... Hayashi T and Su TP (2003b) Intracellular dynamics of sigma-1 receptors (sigma(1) binding sites) in NG108-15 cells. J Pharmacol ... There are two superfamilies of dopamine (DA) receptors, designated D1- and D2-like receptors. D1 and D2 receptors are coupled ...
  http://jpet.aspetjournals.org/content/320/1/202
*  Pharmacological Characterization of Sigma Binding Sites in Guinea Pig Brain Membranes | SpringerLink
... biochemical and behavioral characterization of sigma binding sites is currently the focus of intense investigation. First ... Snyder, S.H. and Largent, B.L., 1989, Receptor mechanisms in antipsychotic drug action: focus on sigma receptors, J. ... Sigma Receptor Haloperidol Administration Sigma Ligand Opioid Receptor Subtype Sigma Binding These keywords were added by ... Vaupel, D.B. and Su, T.-P., 1987, Guinea pig vas deferens may contain both sigma receptors and phencyclidine receptors, Eur. J ...
  https://link.springer.com/chapter/10.1007/978-1-4684-5907-4_5
*  New Products
BD-1047 2HBr is a selective functional antagonist of sigma receptors, shows antipsychotic activity in animal models predictive ... OPC21268 is a non-peptide AVP Receptor V (Vasopressin Receptor) antagonist that shows 1000-fold selectivity for V1 receptors ... Toll-like receptor modulator Toll-like receptors (TLRs) are a class of proteins that play a key role in the innate immune ... Asenapine hydrochloride inhibits adrenergic receptor (α1, α2A, α2B, α2C) with Ki of 0.25-1.2 nM and also inhibits 5-HT receptor ...
  http://www.adooq.com/new-products
*  Gevotroline - Wikipedia
ISBN 0-8493-7632-7. Snyder SH, Largent BL (1989). "Receptor mechanisms in antipsychotic drug action: focus on sigma receptors ... It acts as a balanced, modest affinity D2 and 5-HT2 receptor antagonist and also possesses high affinity for the sigma receptor ... Matheson GK, Guthrie D, Bauer C, Knowles A, White G, Ruston C (January 1991). "Sigma receptor ligands alter concentrations of ... Atypical antipsychotic Atiprosin Azepindole David J. Triggle (1996). Dictionary of Pharmacological Agents. Boca Raton: Chapman ...
  https://en.wikipedia.org/wiki/Gevotroline
*  Pain reliever may help relieve the vision damage of glaucoma | EurekAlert! Science News
... like the antipsychotic haloperidol that target the sigma receptor, already are taken by patients. ... Her target in the astrocytes is sigma-1 receptor, or S1R, a protein found throughout the body that is believed to have the ...
  https://www.eurekalert.org/pub_releases/2017-05/mcog-prm050117.php
*  Plus it
A selective ligand that labels sigma-type receptors for psychotomimetic opiates and antipsychotic drugs. Proc Natl Acad Sci USA ... The present data exclude the possibility that [3H]idazoxan labeled a histamine receptor, in particular an H2 receptor or an ... 1997) Imidazoline receptors: Basic knowledge, recent advances and future prospects for therapy and diagnosis. Drugs Fut 22:757- ... 1989) Calculating receptor number from binding experiments using same compound as radioligand and competitor. Trends Pharmcaol ...
  http://jpet.aspetjournals.org/content/285/1/170
*  Sigma Receptor (σR) | SpringerLink
... are a relatively novel group of receptors originally discovered in the central nervous system [CNS] of mammals in 1976. They ... Consequently, it is thought that the σR may mediate the immunosuppressant, antipsychotic, and neuroprotective effects of many ... Su TP, Hayashi T. Understanding the molecular mechanism of sigma-1 receptors: towards a hypothesis that sigma-1 receptors are ... Sigma receptors [σRs] are a relatively novel group of receptors originally discovered in the central nervous system [CNS] of ...
  https://link.springer.com/referenceworkentry/10.1007%2F978-3-319-67199-4_101870
*  Amitriptyline - Wikipedia
... a selective ligand that labels sigma-type receptors for psychotomimetic opiates and antipsychotic drugs". Proc. Natl. Acad. Sci ... the histamine H1 and H2 receptors, and the muscarinic acetylcholine receptors, and as an agonist of the sigma σ1 receptor. It ... and H₄R receptors with 34 antidepressants and antipsychotics". Naunyn Schmiedebergs Arch. Pharmacol. 385 (2): 145-70. doi: ... "Inverse agonist actions of typical and atypical antipsychotic drugs at the human 5-hydroxytryptamine(2C) receptor". J. ...
  https://en.wikipedia.org/wiki/Amitriptyline
*  Lofepramine - Wikipedia
... a selective ligand that labels sigma-type receptors for psychotomimetic opiates and antipsychotic drugs". Proc. Natl. Acad. Sci ... and H₄R receptors with 34 antidepressants and antipsychotics". Naunyn Schmiedebergs Arch. Pharmacol. 385 (2): 145-70. doi: ... It is a weak-intermediate level antagonist of the muscarinic acetylcholine receptors. Lofepramine has been said to be a prodrug ... Wander TJ, Nelson A, Okazaki H, Richelson E (1986). "Antagonism by antidepressants of serotonin S1 and S2 receptors of normal ...
  https://en.wikipedia.org/wiki/Lofepramine
*  Imipramine - Wikipedia
... a selective ligand that labels sigma-type receptors for psychotomimetic opiates and antipsychotic drugs". Proc. Natl. Acad. Sci ... Sigma receptor: activity on sigma receptors is present, but it is very weak (Ki = 520 nM) and it is about half that of ... Robson MJ, Elliott M, Seminerio MJ, Matsumoto RR (2012). "Evaluation of sigma (σ) receptors in the antidepressant-like effects ... Hindmarch I, Hashimoto K (2010). "Cognition and depression: the effects of fluvoxamine, a sigma-1 receptor agonist, ...
  https://en.wikipedia.org/wiki/Imipramine
*  Nortriptyline - Wikipedia
... a selective ligand that labels sigma-type receptors for psychotomimetic opiates and antipsychotic drugs". Proc. Natl. Acad. Sci ... and H₄R receptors with 34 antidepressants and antipsychotics". Naunyn Schmiedebergs Arch. Pharmacol. 385 (2): 145-70. doi: ... Monsma FJ, Shen Y, Ward RP, Hamblin MW, Sibley DR (1993). "Cloning and expression of a novel serotonin receptor with high ... Ghoneim OM, Legere JA, Golbraikh A, Tropsha A, Booth RG (2006). "Novel ligands for the human histamine H1 receptor: synthesis, ...
  https://en.wikipedia.org/wiki/Nortriptyline
*  Desipramine - Wikipedia
... a selective ligand that labels sigma-type receptors for psychotomimetic opiates and antipsychotic drugs". Proc. Natl. Acad. Sci ... Hindmarch I, Hashimoto K (2010). "Cognition and depression: the effects of fluvoxamine, a sigma-1 receptor agonist, ... and H₄R receptors with 34 antidepressants and antipsychotics". Naunyn Schmiedebergs Arch. Pharmacol. 385 (2): 145-70. doi: ... Wander TJ, Nelson A, Okazaki H, Richelson E (1986). "Antagonism by antidepressants of serotonin S1 and S2 receptors of normal ...
  https://en.wikipedia.org/wiki/Desipramine
*  Treatment of behavioural disturbances in Parkinson's disease | Springer for Research & Development
1991) Cloning of the gene for a human dopamine D4 receptor with high affinity for the antipsychotic clozapine. Nature 350: 610- ... Walker JM, Matsumoto RR, Bowen WD, Gans DL, Jones KD, Walker FO (1988) Evidence for a role of haloperidol-sensitive sigma " ... "opiate" receptors in the motor effects of antipsychotic drugs. Neurology 38: 961-965.PubMedCrossRefGoogle Scholar ... Seeman P (1992) Dopamine receptor sequences, therapeutic levels of neuroleptics occupy D2 receptors, clozapine occupies D4. ...
  https://rd.springer.com/chapter/10.1007/978-3-7091-6846-2_15
*  Evidence for the Role of Metabotropic Glutamate (mGlu)2 Not mGlu3 Receptors in the Preclinical Antipsychotic Pharmacology of...
Materials. PCP and d-amphetamine sulfate (Sigma-Aldrich, St. Louis, MO) were dissolved in 0.9% saline. Risperidone (Toronto ... The relative contribution of mGlu2 versus mGlu3 receptors in the antipsychotic pharmacology of mGlu2/3 receptor agonists has ... 2 Not mGlu3 Receptors in the Preclinical Antipsychotic Pharmacology of the mGlu2/3 Receptor Agonist (-)-(1R,4S,5S,6S)-4-Amino-2 ... 2 Not mGlu3 Receptors in the Preclinical Antipsychotic Pharmacology of the mGlu2/3 Receptor Agonist (-)-(1R,4S,5S,6S)-4-Amino-2 ...
  http://jpet.aspetjournals.org/content/326/1/209.long
*  Sigma receptor - Wikipedia
... and the antipsychotic haloperidol may interact with σ-receptors as biased agonists/antagonists at sigma 1 (versus sigma 2.) ... Leonard BE (2004). "Sigma receptors and sigma ligands: background to a pharmacological enigma". Pharmacopsychiatry. 37 Suppl 3 ... Wang J, Mack AL, Coop A, Matsumoto RR (November 2007). "Novel sigma (sigma) receptor agonists produce antidepressant-like ... Skuza G, Rogóz Z (2006). "The synergistic effect of selective sigma receptor agonists and uncompetitive NMDA receptor ...
  https://en.wikipedia.org/wiki/Sigma_receptor
*  Panamesine - Wikipedia
... is a sigma receptor antagonist that was under development by Merck as a potential antipsychotic for the treatment of ... It is a selective antagonist of both sigma receptor subtypes, the σ1 and σ2 receptors (IC50 = 6 nM).[additional citation(s) ... like dopamine receptors after treatment with the sigma ligand EMD 57445, a putative atypical antipsychotic". Psychopharmacology ... has high affinity for the sigma receptors (IC50 = 24 nM) and the dopamine D2 (IC50 = 23 nM) and D3 receptors, with potent ...
  https://en.wikipedia.org/wiki/Panamesine
*  US9139525B2 - N-oxide and/or di-N-oxide derivatives of dopamine receptor stabilizers/modulators displaying improved...
... investigating the properties of sigma receptor ligands in schizophrenic patients have not generated evidence of antipsychotic ... Two of the most extensively studied selective sigma receptor antagonists, BW234U (rimcazole) and BMY14802, have both failed in ... In this context, also partial dopamine receptor agonists, i.e. dopamine receptor ligands with some, but not full, intrinsic ... EP 0675118) disclose bifenylderivatives of piperazines, which exhibits dopamine D2 receptor antagonism and/or 5-HT2 receptor ...
  https://patents.google.com/patent/US9139525B2/en
*  BMY-14802 - Wikipedia
... is a drug with antipsychotic effects which acts as both a sigma receptor antagonist and a 5-HT1A receptor agonist. It also has ... "A role for sigma binding in the antipsychotic profile of BMY 14802?". NIDA Research Monograph. 133: 125-57. PMID 8232511. ... Kitanaka J, Kitanaka N, Tatsuta T, Hall FS, Uhl GR, Tanaka K, Nishiyama N, Morita Y, Takemura M (May 2009). "Sigma1 receptor ... Paquette MA, Foley K, Brudney EG, Meshul CK, Johnson SW, Berger SP (July 2009). "The sigma-1 antagonist BMY-14802 inhibits L- ...
  https://en.wikipedia.org/wiki/BMY-14802
*  Streamlining in silico profiling
... the sigma 1 receptor; and the progesterone receptor (Figure 4B). These off-target interactions are associated with a broad ... range of effects, including those of antiretroviral drugs, antipsychotic medications and antiprogestins. ... The 5-HT1A receptor, the dopamine receptors D2 and D4 and the chemokine receptors CCR1 and CCR2 are all indicated from the ... The histamine receptors are part of the GPCR target family. Investigating which other GPCRs have highly potent binders similar ...
  https://www.elsevier.com/rd-solutions/industry-insights/pharma-and-life-sciences/t-y/streamlining-in-silico-profiling
*  Identification of drugs including a dopamine receptor antagonist that selectively target cancer stem cells. | Sigma-Aldrich
Sigma-Aldrich offers abstracts and full-text articles by [Eleftherios Sachlos, Ruth M Risueño, Sarah Laronde, Zoya Shapovalova ... Surprisingly, thioridazine, an antipsychotic drug, selectively targets the neoplastic cells, and impairs human somatic CSCs ... Sigma-Aldrich Products are sold exclusively through Sigma-Aldrich, Inc. Site Use Terms , Privacy ... The drug antagonizes dopamine receptors that are expressed on CSCs and on breast cancer cells as well. These results suggest ...
  https://www.sigmaaldrich.com/catalog/papers/22632761
*  Pharmacological Profile of Lurasidone, a Novel Antipsychotic Agent with Potent 5-Hydroxytryptamine 7 (5-HT7) and 5-HT1A...
Evidence of Antipsychotic Mechanisms.. Lurasidone and other antipsychotics dose-dependently inhibited dopamine D2 receptor- ... sigma, L-type Ca2+ channel, N-type Ca2+ channel, 5-HT uptake site, and dopamine uptake site (data not shown). ... In vitro receptor binding experiments in the present study have shown Ki values in typical and atypical antipsychotics, which ... Comparison of receptor binding profiles between lurasidone and other antipsychotic agents. Values are means ± S.E.M. of three ...
  http://jpet.aspetjournals.org/content/334/1/171.long
*  Sigma-2 receptor - Wikipedia
... while sigma-2 receptor activation has been shown to antagonize effects of PCP, implying antipsychotic capabilities. Sigma ... The sigma-2 receptor (σ2R) is a sigma receptor subtype that has been found highly expressed in malignant cancer cells, and is ... The position of the sigma-2 receptor had not previously been located on the human chromosome. The sigma-2 receptor is a ... Tumor cells are shown to over-express sigma-2 receptors, allowing for potential cancer therapies as many sigma-2 receptor ...
  https://en.wikipedia.org/wiki/Sigma-2_receptor
*  NPC 16377, a potent and selective sigma-ligand. I. Receptor binding, neurochemical and neuroendocrine profile. | Journal of...
... other sigma-ligands and atypical antipsychotics, while having no effect on dopamine turnover. Given these data, NPC 16377 ... NPC 16377, a potent and selective sigma-ligand. I. Receptor binding, neurochemical and neuroendocrine profile.. E W Karbon, M E ... NPC 16377, a potent and selective sigma-ligand. I. Receptor binding, neurochemical and neuroendocrine profile.. E W Karbon, M E ... NPC 16377, a potent and selective sigma-ligand. I. Receptor binding, neurochemical and neuroendocrine profile.. E W Karbon, M E ...
  http://jpet.aspetjournals.org/content/265/2/866
*  BD-1047 - Wikipedia
BD-1047 is a sigma receptor antagonist, selective for the σ1 subtype. It has effects in animal studies suggestive of ... a sigma1 receptor antagonist, in the animal models predictive of antipsychotic activity". Pharmacological Reports : PR. 58 (5 ... "Intrathecal injection of the sigma(1) receptor antagonist BD1047 blocks both mechanical allodynia and increases in spinal NR1 ... "Ethanol Stimulates Endoplasmic Reticulum Inositol Triphosphate and Sigma Receptors to Promote Withdrawal-Associated Loss of ...
  https://en.wikipedia.org/wiki/BD-1047
*  Sigma receptor binding agent containing indanone derivative - Patent application
However, subsequent studies revealed that the sigma receptors are non-opiate receptors and that multitude of antipsychotic ... the sigma receptor binding agent described in 1) or 2), which is a sigma receptor antagonist or a sigma receptor agonist; 4) ... receptor binding agent is a sigma receptor antagonist or a sigma receptor agonist. 4. The method for treatment according to ... Sigma Receptor Binding Assay (1) Preparation of Receptor [0206]The receptor was prepared by the following procedure according ...
  http://www.patentsencyclopedia.com/app/20090137629