Dihydro-β-erythroidine hydrobromide

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Dihydro-β-erythroidine hydrobromide | CAS No. 29734-68-7 | Additional Nicotinic Receptor Antagonists
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Description: α4β2, muscle type and Torpedo nAChR antagonist
Alternative Names: DHβE

Chemical Name: (2S,13bS)-2-Methoxy-2,3,5,6,8,9,10,13-octahydro-1H,12H-benzo[i]pyrano[3,4-g]indolizin-12-one hydrobromide

Purity: ≥98%

Product Details
Citations (30)
Supplemental Products
Reviews

Biological Activity

Dihydro-β-erythroidine hydrobromide is a member of the Erythrina alkaloids, it is a competitive nicotinic acetylcholine receptor antagonist with moderate selectivity for the neuronal α4 receptor subunit (IC50 values are 0.19 and 0.37 μM for α4β4 and α4β2 receptors, respectively). Antagonizes behavioral effects of nicotine in vivo. Dihydro-β-erythroidine blocks excitation of striatal GABAergic neurons, which completely suppress polysynaptic inhibition between striatal cholinergic interneurons. Dihydro-β-erythroidine hydrobromide has antidepressive-like effects in mice (forced swim and mouse suspension). Orally bioavailable.

Technical Data

M.Wt:
356.26
Formula:
C16H21NO3.HBr
Solubility:
Soluble to 100 mM in water and to 25 mM in DMSO
Purity:
≥98%
Storage:
Desiccate at RT
CAS No:
29734-68-7

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. Greater ethanol inhibition of presynaptic dopamine release in C57BL/6J than DBA/2J mice: Role of nicotinic acetylcholine receptors.
    Yorgason J, Rose J, McIntosh J, Ferris M, Jones S
    Neuroscience, 2015;284(0):854-64.
  2. TRPV1 regulates excitatory innervation of OLM neurons in the hippocampus
    JI Hurtado-Za, B Ramachandr, S Ahmed, R Halder, C Bolleyer, A Awasthi, MA Stahlberg, RJ Wagener, K Anderson, RM Drenan, HA Lester, JM Miwa, JF Staiger, A Fischer, C Dean
    Nat Commun, 2017;8(0):15878.
  3. Administration of nicotinic receptor antagonists during the period of memory consolidation affects passive avoidance learning and modulates synaptic efficiency in the CA1 region in vivo.
    Dobryakova Y, Gurskaya O, Markevich V
    Neuroscience, 2015;284(0):865-71.
  4. Binding of the nicotinic cholinergic antagonist, dihydro-β-erythroidine, to rat brain tissue.
    Williams and Robinson
    J.Neurosci., 1984;4:2906
  5. In vivo pharmacological effects of dihydro-β-erythroidine, a nicotinic antagonist, in mice.
    Damaj et al.
    Psychopharmacology, 1995;117:67
  6. Multiple determinants of dihydro-β-erythroidine sensitivity on rat neuronal nicotinic receptor α subunits.
    Harvey et al.
    J.Neurochem., 1996;67:1953
  7. Nicotinic acetylcholine receptors: Ex-vivo expression of functional, non-hybrid, heteropentameric receptors from a marine arthropod, Lepeophtheirus salmonis
    L Rufener, K Kaur, A Sarr, SM Aaen, TE Horsberg
    PLoS Pathog., 2020;16(7):e1008715.

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Citations for Dihydro-β-erythroidine hydrobromide

The citations listed below are publications that use Tocris products. Selected citations for Dihydro-β-erythroidine hydrobromide include:

30 Citations: Showing 1 - 10

  1. GABAergic inhibition in dual-transmission cholinergic and GABAergic striatal interneurons is abolished in Parkinson disease.
    Authors: Lozovaya Et al.
    Nat Commun  2349;9(1):1422
  2. Polysynaptic inhibition between striatal cholinergic interneurons shapes their network activity patterns in a dopamine-dependent manner.
    Authors: Dorst Et al.
    Nat Commun  2020;11:5113
  3. Neural mechanisms of contextual modulation in the retinal direction selective circuit.
    Authors: Huang Et al.
    Nat Commun  2019;10:2431
  4. Pauses in Cholinergic Interneuron Activity Are Driven by Excitatory Input and Delayed Rectification, with DA Modulation.
    Authors: Zhang Et al.
    Neuron  2018;98:918
  5. Differential effects of α4β2 nicotinic receptor antagonists and partial-agonists on contextual fear extinction in male C57BL/6 mice.
    Authors: Kutlu Et al.
    Psychopharmacology (Berl)  2018;235:1211
  6. Local GABAA receptor mediated suppression of DA release within the nucleus accumbens.
    Authors: Brodnik Et al.
    ACS Chem Neurosci  2018;17:1978
  7. Inhibition of peripheral macrophages by nicotinic acetylcholine receptor agonists suppresses spinal microglial activation and neuropathic pain in mice with peripheral nerve injury.
    Authors: Kiguchi
    J Neuroinflammation  2018;15(1):96
  8. Differential processing of thalamic information via distinct striatal interneuron circuits.
    Authors: Assous
    Nat Commun  2017;8:15860
  9. Selective and regulated trapping of nicotinic receptor weak base ligands and relevance to smoking cessation.
    Authors: Govind Et al.
    Elife  2017;6
  10. Speed and segmentation control mechanisms characterized in rhythmically-active circuits created from spinal neurons produced from genetically-tagged embryonic stem cells.
    Authors: Sternfeld Et al.
    Elife  2017;6
  11. Plasticity in Brainstem Mechanisms of Pain Modulation by Nicotinic Acetylcholine Receptors in the Rat.
    Authors: Jareczek Et al.
    Eneuro  2017;4
  12. Spontaneous Release Regulates Synaptic Scaling in the Embryonic Spinal Network In Vivo
    Authors: Miguel Angel Garcia-Bereguiain Et al.
    The Journal of Neuroscience  2016;6:7268
  13. Nicotinic and opioid receptor regulation of striatal DA D2-receptor mediated transmission
    Authors: Mamaligas Et al.
    Scientific Reports  2016;6:37834
  14. A cholinergic basal forebrain feeding circuit modulates appetite suppression
    Authors: Herman Et al.
    Nature  2016;538:253
  15. Nicotine evokes kinetic tremor by activating the inferior olive via α7 nicotinic acetylcholine receptors.
    Authors: Kunisawa Et al.
    Behav.Brain Res.  2016;314:173
  16. Acetylcholine induces GABA release onto rod bipolar cells through heteromeric nicotinic receptors expressed in A17 amacrine cells.
    Authors: Elgueta Et al.
    PLoS One  2015;9:6
  17. Ins enhances striatal DA release by activating cholinergic interneurons and thereby signals reward.
    Authors: Stouffer Et al.
    Nat Commun  2015;6:8543
  18. Corelease of acetylcholine and GABA from cholinergic forebrain neurons.
    Authors: Saunders Et al.
    J Neurosci  2015;4
  19. Novel aspects of cholinergic regulation of colonic ion transport.
    Authors: Bader and Diener
    Elife  2015;3:e00139
  20. An Asymmetric Increase in Inhibitory Synapse Number Underlies the Development of a Direction Selective Circuit in the Retina.
    Authors: Morrie and Feller
    Neuroscience  2015;35:9281
  21. Functional Upregulation of α4* Nicotinic Acetylcholine Receptors in VTA GABAergic Neurons Increases Sensitivity to Nicotine Reward.
    Authors: Ngolab Et al.
    J Neurosci  2015;35:8570
  22. Absence of plateau potentials in dLGN cells leads to a breakdown in retinogeniculate refinement.
    Authors: Dilger Et al.
    J Neurosci  2015;35:3652
  23. Greater ethanol inhibition of presynaptic DA release in C57BL/6J than DBA/2J mice: Role of nicotinic acetylcholine receptors.
    Authors: Yorgason Et al.
    Front Cell Neurosci  2015;284:854
  24. Nicotinic acetylcholine receptors containing the α7-like subunit mediate contractions of muscles responsible for space positioning of the snail, Helix pomatia L. tentacle.
    Authors: Kiss Et al.
    PLoS One  2014;9:e109538
  25. Nicotine elicits prolonged calcium signaling along ventral hippocampal axons.
    Authors: Zhong Et al.
    Pharmacol Res Perspect  2013;8:e82719
  26. Striatal DA transmission is subtly modified in human A53Tα-synuclein overexpressing mice.
    Authors: Platt Et al.
    PLoS One  2012;7:e36397
  27. Gamma oscillations are generated locally in an attention-related midbrain network.
    Authors: Goddard Et al.
    Neuron  2012;73:567
  28. Developmental regulation of CB1-mediated spike-time dependent depression at immature mossy fiber-CA3 synapses.
    Authors: Caiati Et al.
    Sci Rep  2012;2:285
  29. Cytisine induces autonomic cardiovascular responses via activations of different nicotinic receptors.
    Authors: Li Et al.
    Auton Neurosci  2010;154:14
  30. Specific subtypes of nicotinic cholinergic receptors involved in sympathetic and parasympathetic cardiovascular responses.
    Authors: Li Et al.
    Neurosci Lett  2009;462:20

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