Role of hsp90 and the hsp90-binding immunophilins in signalling
... binding site on hsp90. Using several intracellular receptors and the tumor suppressor p53 as examples, we review evidence that dynamic assembly of heterocomplexes with hsp90 is required for rapid movement through the cytoplasm to the nucleus along microtubular tracks. The role of the immunophilin in ...
... binding site on hsp90. Using several intracellular receptors and the tumor suppressor p53 as examples, we review evidence that dynamic assembly of heterocomplexes with hsp90 is required for rapid movement through the cytoplasm to the nucleus along microtubular tracks. The role of the immunophilin in ...
Brassinosteroid Signal Transduction from Receptor Kinases to
... suppresses the phenotype of a weak bri1 allele (52, 60). The bak1 loss-of-function mutant resembles weak bri1 mutants (52), and overexpression of a kinase-inactive bak1 mutant protein causes severe dwarf phenotypes similar to strong bri1 mutants, presumably due to a dominant negative effect (52). Re ...
... suppresses the phenotype of a weak bri1 allele (52, 60). The bak1 loss-of-function mutant resembles weak bri1 mutants (52), and overexpression of a kinase-inactive bak1 mutant protein causes severe dwarf phenotypes similar to strong bri1 mutants, presumably due to a dominant negative effect (52). Re ...
Striatal D2 / D3 Receptor Occupancy, ... and Side Effects with Amisulpride: An Iodine-123-Iodobenzamide SPET Study
... The mean dosage of amisulpride was 455.1 ± 278.8 mg daily. Striatal IBZM binding of the patient group, expressed as [STR–BKG]/ BKG, ranged from 0.0–1.12 (mean 0.43 ± 0.32) versus a mean striatal IBZM binding of 0.95 ± 0.10 (range: 0.78–1.12) for the healthy control group. No differences were found b ...
... The mean dosage of amisulpride was 455.1 ± 278.8 mg daily. Striatal IBZM binding of the patient group, expressed as [STR–BKG]/ BKG, ranged from 0.0–1.12 (mean 0.43 ± 0.32) versus a mean striatal IBZM binding of 0.95 ± 0.10 (range: 0.78–1.12) for the healthy control group. No differences were found b ...
Blum et al. 2011 - Boston University
... substantiated the substance’s action as partial agonist at the mu-opioid receptor. These findings were underscored by the substance’s general pharmacological profile. Furthermore, buprenorphine was one of the first narcotic analgesics to be assessed for its abuse liability in humans. Buprenorphine w ...
... substantiated the substance’s action as partial agonist at the mu-opioid receptor. These findings were underscored by the substance’s general pharmacological profile. Furthermore, buprenorphine was one of the first narcotic analgesics to be assessed for its abuse liability in humans. Buprenorphine w ...
Inhibition of Bladder Activity by 5 - Duke Statistical
... In a recent cystometric study of the 5-HT1A receptor agonist (R)-(⫹)-8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) (Thor et al., 2002), normal cat bladders were filled either with saline to innocuously initiate micturition via activation of myelinated A␦ fibers or with dilute acetic acid to noc ...
... In a recent cystometric study of the 5-HT1A receptor agonist (R)-(⫹)-8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) (Thor et al., 2002), normal cat bladders were filled either with saline to innocuously initiate micturition via activation of myelinated A␦ fibers or with dilute acetic acid to noc ...
Opioid and Cannabinoid Modulation of Precipitated Withdrawal in
... et al., 1998). As in the case of opioids, mice will self-administer the cannabinoid aminoalkylindole WIN 55,212-2 (Martellotta et al., 1998). Through the use of these models, the neurochemical mechanisms underlying cannabinoid dependence can now be systematically investigated. Substantial evidence i ...
... et al., 1998). As in the case of opioids, mice will self-administer the cannabinoid aminoalkylindole WIN 55,212-2 (Martellotta et al., 1998). Through the use of these models, the neurochemical mechanisms underlying cannabinoid dependence can now be systematically investigated. Substantial evidence i ...
Reinstatement of Morphine-Conditioned Reward is Blocked by
... with 10 mg/kg of chlordiazepoxide during the extinction phase and was challenged with morphine. To test the ‘conditioned opioid withdrawal hypothesis’ (see Discussion section), morphine-conditioned mice were extinguished with 1 mg/kg of morphine and were challenged with morphine. To investigate if a ...
... with 10 mg/kg of chlordiazepoxide during the extinction phase and was challenged with morphine. To test the ‘conditioned opioid withdrawal hypothesis’ (see Discussion section), morphine-conditioned mice were extinguished with 1 mg/kg of morphine and were challenged with morphine. To investigate if a ...
Psychedelic Drugs - American College of Neuropsychopharmacology
... diastereomer of chlorobutyl LSD, is at least 50% more potent than LSD. In ligand binding at 5-HT2, 5-HT1A, D1, and D2 receptors, the (R)-2-butylamide substituent is likewise more potent. Cloning of the 5-HT-2 receptor permitted replacement of aspartate 120 in second transmembrane domain with asparag ...
... diastereomer of chlorobutyl LSD, is at least 50% more potent than LSD. In ligand binding at 5-HT2, 5-HT1A, D1, and D2 receptors, the (R)-2-butylamide substituent is likewise more potent. Cloning of the 5-HT-2 receptor permitted replacement of aspartate 120 in second transmembrane domain with asparag ...
Hallucinatory and rewarding effect of salvinorin A in zebrafish: κ
... dependent modifications of locomotor activity (Gerlai et al. 2000) and tolerance as has been observed in mammals as well as Drosophila (Scholz et al. 2000). Moreover, ethanolinduced hyperlocomotion can be blocked by the addition of a dopamine antagonist, suggesting the involvement of the brain dopam ...
... dependent modifications of locomotor activity (Gerlai et al. 2000) and tolerance as has been observed in mammals as well as Drosophila (Scholz et al. 2000). Moreover, ethanolinduced hyperlocomotion can be blocked by the addition of a dopamine antagonist, suggesting the involvement of the brain dopam ...
Immunohistochemical Analysis of Trk Receptor Activation in Epilepsy
... involvement of neurotrophins in kindling, and combined with the functional data pinpoint important sites of epileptogenesis in the brain. ...
... involvement of neurotrophins in kindling, and combined with the functional data pinpoint important sites of epileptogenesis in the brain. ...
Advances in Genetics - Department of Biology
... channel families, DEG/ENaC channels have evolved to serve many different physiological functions, acting as ionotropic receptors to diverse extracellular stimuli. Although amiloride-sensitive sodium currents from various epithelial tissues have been recorded since the early 1970s, the genes encoding ...
... channel families, DEG/ENaC channels have evolved to serve many different physiological functions, acting as ionotropic receptors to diverse extracellular stimuli. Although amiloride-sensitive sodium currents from various epithelial tissues have been recorded since the early 1970s, the genes encoding ...
Dextromethorphan (DXM)
... available in Finland include Resilar®, Redol Comp® and Sir Ephedrin®. They can only be bought at pharmacies and some are prescription-only. There are a number of English street names for preparations containing dextromethorphan, including CCC, robos and skittles. In Finland, they are known as “Ressu ...
... available in Finland include Resilar®, Redol Comp® and Sir Ephedrin®. They can only be bought at pharmacies and some are prescription-only. There are a number of English street names for preparations containing dextromethorphan, including CCC, robos and skittles. In Finland, they are known as “Ressu ...
“Robo-Tripping”: Dextromethorphan Abuse and its Anesthetic
... dextromethorphan. Respiratory depression, tachycardia, hypertension, seizures, and death may result from severe acute dextromethorphan intoxication (1, 4, 7, 8, 16) whereas chronic abuse of the drug has been associated with frank psychosis (2). These actions are very similar to those described with ...
... dextromethorphan. Respiratory depression, tachycardia, hypertension, seizures, and death may result from severe acute dextromethorphan intoxication (1, 4, 7, 8, 16) whereas chronic abuse of the drug has been associated with frank psychosis (2). These actions are very similar to those described with ...
(Nurr1, Nur77 and Nor-1) by Typical and Atypical Antipsychotics in
... atypical antipsychotic drugs. Modulation of Nur77 and Nor-1 mRNA expression by antipsychotics can be used to calculate an index that is predictive of the typical or atypical profile of antipsychotic drugs. Inductions of Nurs by antipsychotic drugs are correlated with dopamine D2 receptor in the stri ...
... atypical antipsychotic drugs. Modulation of Nur77 and Nor-1 mRNA expression by antipsychotics can be used to calculate an index that is predictive of the typical or atypical profile of antipsychotic drugs. Inductions of Nurs by antipsychotic drugs are correlated with dopamine D2 receptor in the stri ...
Disorders of Reward, Drug Abuse, and Thei r Treatment
... are key aspects to all the disorders discussed in this text. For that reason, we will discuss what is known about reward circuits in some detail. New treatments for disorders of reward circuitry are finally entering psychopharmacology and the prospects for future therapeutics that target malfunction ...
... are key aspects to all the disorders discussed in this text. For that reason, we will discuss what is known about reward circuits in some detail. New treatments for disorders of reward circuitry are finally entering psychopharmacology and the prospects for future therapeutics that target malfunction ...
The ribosome — a macromolecular machine par excellence
... proximity: the anticodon loops, which must make contact with two successive codons of the message, and the CCA ends, which must be close enough to allow transfer of the peptide bond, at the so-called peptidyltransferase center. The large (~80 Å) separation of the anticodon- and aminoacid-carrying en ...
... proximity: the anticodon loops, which must make contact with two successive codons of the message, and the CCA ends, which must be close enough to allow transfer of the peptide bond, at the so-called peptidyltransferase center. The large (~80 Å) separation of the anticodon- and aminoacid-carrying en ...
Serotonin 2A Receptors Differentially Contribute to Abuse
... self-administration and reinstatement of extinguished behavior previously maintained by drug delivery. Intravenous selfadministration is widely accepted to model ongoing drug-taking behavior, whereas reinstatement procedures are accepted to model relapse to drug taking following abstinence. Previous ...
... self-administration and reinstatement of extinguished behavior previously maintained by drug delivery. Intravenous selfadministration is widely accepted to model ongoing drug-taking behavior, whereas reinstatement procedures are accepted to model relapse to drug taking following abstinence. Previous ...
HERE - INDIGO Biosciences
... EON_ShapeTanimoto index of 0.54 (Fig. 1), and high similarity to T3 with Tanimoto Combo index of 0.52 and EON_ShapeTanimoto index of 0.42. The docking analysis was carried out using three TRβ crystal structure with three different ligands; diclofenac (Fig. 2A) could bind to active sites of all three ...
... EON_ShapeTanimoto index of 0.54 (Fig. 1), and high similarity to T3 with Tanimoto Combo index of 0.52 and EON_ShapeTanimoto index of 0.42. The docking analysis was carried out using three TRβ crystal structure with three different ligands; diclofenac (Fig. 2A) could bind to active sites of all three ...
Methadone Maintenance A Practical Guide to Pharmacotherapy
... • Each dose will have a greater effect until steady-state is achieved (potential for accumulated toxicity) • Methadone induction is a dangerous period for risk of overdose Most programs recommend at least 5 days between dose adjustments in the range of 5–10 mg. More rapid dose escalations could be a ...
... • Each dose will have a greater effect until steady-state is achieved (potential for accumulated toxicity) • Methadone induction is a dangerous period for risk of overdose Most programs recommend at least 5 days between dose adjustments in the range of 5–10 mg. More rapid dose escalations could be a ...
Piracetam and other structurally related nootropics
... Almost thirty years have now passed since the discovery of the piracetam-like nootropics. The term nootropiC92794,95 was coined by Giurgea in 1972, from Greek BOOS(~00s) (mind) and Greek tropos (T~OTOS) (turn), to describe the then netily discovered properties of these compounds: (1) enhancement of ...
... Almost thirty years have now passed since the discovery of the piracetam-like nootropics. The term nootropiC92794,95 was coined by Giurgea in 1972, from Greek BOOS(~00s) (mind) and Greek tropos (T~OTOS) (turn), to describe the then netily discovered properties of these compounds: (1) enhancement of ...
S7.Cell Signaling-β-catenin pathway homework
... 1. What are the components of the receptor complex? What is the ligand? The receptor complex is composed of LRP and Fzd. The ligand for Fzd is Wnt. 2. What is the molecular function of β-catenin itself? Apart from its role in adherens junctions, β-catenin is a transcriptional coactivator. β-catenin ...
... 1. What are the components of the receptor complex? What is the ligand? The receptor complex is composed of LRP and Fzd. The ligand for Fzd is Wnt. 2. What is the molecular function of β-catenin itself? Apart from its role in adherens junctions, β-catenin is a transcriptional coactivator. β-catenin ...
Salvinorin A, an Active Component of the Hallucinogenic Sage
... no significant activity at other receptors, including various serotonergic, dopaminergic, muscarinic, adrenergic, cannabinoid, and receptors (see Table 2 for details) We next evaluated the ability of salvinorin A and the propionate and heptanoate derivatives to activate hKORs by measuring the abil ...
... no significant activity at other receptors, including various serotonergic, dopaminergic, muscarinic, adrenergic, cannabinoid, and receptors (see Table 2 for details) We next evaluated the ability of salvinorin A and the propionate and heptanoate derivatives to activate hKORs by measuring the abil ...
Evidence that Diclofenac and Celecoxib are thyroid hormone
... acid) with Tanimoto Combo index of 0.68 and EON_ShapeTanimoto index of 0.54 (Figure 1), and high similarity to T3 with Tanimoto Combo index of 0.52 and EON_ShapeTanimoto index of 0.42. The docking analysis was carried out using three TRβ crystal structure with three different ligands; diclofenac (Fi ...
... acid) with Tanimoto Combo index of 0.68 and EON_ShapeTanimoto index of 0.54 (Figure 1), and high similarity to T3 with Tanimoto Combo index of 0.52 and EON_ShapeTanimoto index of 0.42. The docking analysis was carried out using three TRβ crystal structure with three different ligands; diclofenac (Fi ...
CURRICULUM VITAE
... absence of experimentally determined structures of cannabinoid receptors, information about their ligandbinding sites may best be obtained through the use of affinity probes coupled with mass spectrometric analysis of labeled protein. This project involves design and synthesis of: 1) Covalent and el ...
... absence of experimentally determined structures of cannabinoid receptors, information about their ligandbinding sites may best be obtained through the use of affinity probes coupled with mass spectrometric analysis of labeled protein. This project involves design and synthesis of: 1) Covalent and el ...
NMDA receptor
The N-methyl-D-aspartate receptor (also known as the NMDA receptor or NMDAR), is a glutamate receptor and ion channel protein found in nerve cells. It is activated when glutamate and glycine (or D-serine) bind to it, and when activated it allows positively charged ions to flow through the cell membrane. The NMDA receptor is very important for controlling synaptic plasticity and memory function.The NMDAR is a specific type of ionotropic glutamate receptor. The NMDA receptor is named this because the agonist molecule N-methyl-D-aspartate (NMDA) binds selectively to it, and not to other glutamate receptors. Activation of NMDA receptors results in the opening of an ion channel that is nonselective to cations with a reversal potential near 0 mV. A property of the NMDA receptor is its voltage-dependent activation, a result of ion channel block by extracellular Mg2+ & Zn2+ ions. This allows the flow of Na+ and small amounts of Ca2+ ions into the cell and K+ out of the cell to be voltage-dependent.Calcium flux through NMDARs is thought to be critical in synaptic plasticity, a cellular mechanism for learning and memory. The NMDA receptor is distinct in two ways: first, it is both ligand-gated and voltage-dependent; second, it requires co-activation by two ligands: glutamate and either D-serine or glycine.The activity of the NMDA receptor is affected by many psychoactive drugs such as phencyclidine (PCP), alcohol (ethanol) and dextromethorphan (DXM). The anaesthetic effects of the drugs ketamine and nitrous oxide are partially because of their effects on NMDA receptor activity.