Loading...
*  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
*  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
*  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
*  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
*  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
*  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
*  Umespirone - Wikipedia
... and also has weak affinity for the sigma receptor (Ki = 558 nM). Unlike many other anxiolytics and antipsychotics, umespirone ... Itzhak Y, Ruhland M, Krähling H (February 1990). "Binding of umespirone to the sigma receptor: evidence for multiple affinity ... It behaves as a 5-HT1A receptor partial agonist (Ki = 15 nM), D2 receptor partial agonist (Ki = 23 nM), and α1-adrenoceptor ... Krähling H, Fuchs A, Ruhland M, Schön U, Mol F, Tulp M (November 1988). "KC 9172 (free base of KC 7218)--an antipsychotic/ ...
  https://en.wikipedia.org/wiki/Umespirone
*  Nemonapride - Wikipedia
Nemonapride acts as a D2 and D3 receptor antagonist, and is also a potent 5-HT1A receptor agonist. It has affinity for sigma ... Nemonapride (エミレース, Emilace (JP)) is an atypical antipsychotic approved in Japan for the treatment of schizophrenia. It was ...
  https://en.wikipedia.org/wiki/Nemonapride
*  3-PPP - Wikipedia
... acts as an agonist of presynaptic D2 receptors but as an antagonist of postsynaptic D2 receptors, and has antipsychotic effects ... "Rat liver and kidney contain high densities of sigma 1 and sigma 2 receptors: characterization by ligand binding and ... 3-PPP is the enantiomer that acts as an agonist of the sigma receptors; it is also an agonist of both D2 presynaptic and ... 3-PPP (N-n-propyl-3-(3-hydroxyphenyl)piperidine) is a mixed sigma σ1 and σ2 receptor agonist (with similar affinity for both ...
  https://en.wikipedia.org/wiki/3-PPP
*  Rimcazole - Wikipedia
Rimcazole is an antagonist of the sigma receptor as well as a dopamine reuptake inhibitor. Sigma receptors are thought to be ... was originally researched as a potential antipsychotic with a different mechanism of action to traditional antipsychotic drugs ... correlation with binding to sigma receptors rather than dopamine transporters. Neuropharmacology. 2001 Dec;41(7):878-86.. ... Clinical trials with sigma ligands. Pharmacopsychiatry. 2004 Nov;37 Suppl 3:S214-20. Katz JL, Libby TA, Kopajtic T, Husbands SM ...
  https://en.wikipedia.org/wiki/Rimcazole
*  Remoxipride - Wikipedia
Remoxipride acts as a selective D2 and D3 receptor antagonist and also has high affinity for the sigma receptor, possibly ... Remoxipride (Roxiam) is an atypical antipsychotic (although according to some sources it is a typical antipsychotic) which was ... Typical antipsychotic Benzamide Grind, M; Nilsson, MI; Nilsson, L; Oxenstierna, G; Sedvall, G; Wahlén, A (1989). "Remoxipride ... José Miguel Vela; Helmut Buschmann; Jörg Holenz; Antonio Párraga; Antoni Torrens (2007). Antidepressants, Antipsychotics, ...
  https://en.wikipedia.org/wiki/Remoxipride
*  Ditolylguanidine - Wikipedia
... a selective ligand that labels sigma-type receptors for psychotomimetic opiates and antipsychotic drugs". Proc. Natl. Acad. Sci ... Ditolylguanidine is a sigma receptor agonist. It is somewhat selective for sigma receptors, but non-selective between the two ... Katnik, C; Guerrero, WR; Pennypacker, KR; Herrera, Y; Cuevas, J (2006). "Sigma-1 receptor activation prevents intracellular ... Glennon, RA (2005). "Pharmacophore identification for sigma-1 (sigma1) receptor binding: application of the "deconstruction- ...
  https://en.wikipedia.org/wiki/Ditolylguanidine
*  Clocapramine - Wikipedia
"In vitro receptor binding and in vivo receptor occupancy in rat and guinea pig brain: risperidone compared with antipsychotics ... Morio Y, Tanimoto H, Yakushiji T, Morimoto Y (February 1994). "Characterization of the currents induced by sigma ligands in ... February 1995). "Atypicality of several antipsychotics on the basis of in vivo dopamine-D2 and serotonin-5HT2 receptor ... It has also been shown to have affinity for the σ receptors. Clocapramine's affinity for the 5-HT2A receptor is greater than ...
  https://en.wikipedia.org/wiki/Clocapramine
*  NE-100 - Wikipedia
... and more than 205 times selectivity over the sigma-2 receptor. NE-100 was one of the earliest selective sigma-1 receptor ... and Biological Characterization of Novel Arylalkoxyphenylalkylamine s Ligands as Potential Antipsychotic Drugs". Journal of ... Okuyama S, Nakazato A (1999). "NE-100: A novel sigma receptor antagonist". CNS Drug Rev. 2 (2): 226-237. Berardi F, Ferorelli S ... NE-100 or 4-methoxy-3-(2-phenylethoxy)-N,N-dipropylbenzeneethanamine is a selective sigma-1 receptor antagonist, with a ...
  https://en.wikipedia.org/wiki/NE-100
*  Blonanserin - Wikipedia
... and mACh receptors and the monoamine transporters, though it does possess low affinity for the sigma receptor (IC50 = 286 nM). ... "Striatal and extrastriatal dopamine D2 receptor occupancy by a novel antipsychotic, blonanserin: a PET study with [11C] ... Towards human receptors unless otherwise specified. Blonanserin has antagonistic action at dopamine-D3 receptors that ... Dopamine Receptor D3 Lipinski's rule of five Wen, YG; Shang, DW; Xie, HZ; Wang, XP; Ni, XJ; Zhang, M; Lu, W; Qiu, C; Liu, X; Li ...
  https://en.wikipedia.org/wiki/Blonanserin
*  Azapirone - Wikipedia
... α2-adrenergic receptor (as antagonists) Actions at D4, 5-HT2C, 5-HT7, and sigma receptors have also been shown for some ... February 1995). "Atypicality of several antipsychotics on the basis of in vivo dopamine-D2 and serotonin-5HT2 receptor ... 5-HT1A receptor (as partial or full agonists) 5-HT2A receptor (as inverse agonists) D2 receptor (as antagonists or partial ... Itzhak Y, Ruhland M, Krähling H (February 1990). "Binding of umespirone to the sigma receptor: evidence for multiple affinity ...
  https://en.wikipedia.org/wiki/Azapirone
*  Methamphetamine - Wikipedia
Methamphetamine binds to and activates both sigma receptor subtypes, σ1 and σ2, in the brain. Sigma receptor activation by ... Antipsychotics such as haloperidol are useful in treating agitation and psychosis from methamphetamine overdose. Beta blockers ... Methamphetamine is also an agonist of the alpha-2 adrenergic receptors and sigma receptors with a greater affinity for σ1 than ... The NMDA receptor is unique among all neurotransmitter receptors in that its activation requires the simultaneous binding of ...
  https://en.wikipedia.org/wiki/Methamphetamine
*  Sertraline - Wikipedia
... and the sigma σ1 receptor (but not the σ2 receptor). However, its affinities for these sites are around 100-fold or more lower ... According to the label, sertraline is contraindicated in individuals taking monoamine oxidase inhibitors or the antipsychotic ... affinity for the sigma σ1 receptor. Conversely, it has low (micromolar) and insignificant affinity for the σ2 receptor. It acts ... Hashimoto, K (2009). "Sigma-1 Receptors and Selective Serotonin Reuptake Inhibitors: Clinical Implications of their ...
  https://en.wikipedia.org/wiki/Sertraline
*  Fluvoxamine - Wikipedia
Its actions at the sigma receptor may afford it a unique advantage among antidepressants in treating the cognitive symptoms of ... Bondy, Brigitta; Illja Spellmann (2007). "Pharmacogenetics of Antipsychotics: Useful For the Clinician?". Curr Opin Psychiatry ... Hindmarch, I; Hashimoto, K (April 2010). "Cognition and depression: the effects of fluvoxamine, a sigma-1 receptor agonist, ... Hashimoto, K (September 2009). "Sigma-1 receptors and selective serotonin reuptake inhibitors: clinical implications of their ...
  https://en.wikipedia.org/wiki/Fluvoxamine
*  Cocaine intoxication - Wikipedia
Narayanan, Sanju; Mesangeau, Christophe; Poupaert, Jacques H.; McCurdy, Christopher R. (2011-01-01). "Sigma receptors and ... Agitated patients are best treated with benzodiazepines, but antipsychotics such as haloperidol and olanzapine may also be ... Kivell, Bronwyn M.; Ewald, Amy W. M.; Prisinzano, Thomas E. (2014-01-01). "Salvinorin A analogs and other κ-opioid receptor ... Adding to its complex toxicity, cocaine targets muscarinic acetylcholine, N-methyl-D-aspartate (NMDA), sigma, and kappa-opioid ...
  https://en.wikipedia.org/wiki/Cocaine_intoxication