• We specialize in small molecule inhibitors, agonists, antagonists and screening libraries!
Search Site
Home >> Signaling Pathways >> Neuroscience >> Nicotinic Receptor >> Dihydro-β-erythroidine hydrobromide
Related Products
Dihydro-β-erythroidine hydrobromideantagonist of nAChRs

Dihydro-β-erythroidine hydrobromide

Catalog No. B7030
Size Price Stock Qty
10mg $193.00 Ship Within 7 Days
50mg $809.00 Ship Within 7 Days

Tel: +1-832-696-8203

Email: sales@apexbt.com

Worldwide Distributors

Sample solution is provided at 25 µL, 10mM.

Quality Control

Quality Control & MSDS

View current batch:

Chemical structure

Dihydro-β-erythroidine hydrobromide

Protocol

Cell experiment [1]:

Cell lines

Xenopus oocytes

Preparation method

The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

300nM or 1 μM

Applications

At the concentration of 1 μM, Dihydro-β-erythroidine Hydrobromide almost completely blocked the α4β4 subunit but showed little effect on the α3β4 subunit. However, the blockade effect of Dihydro-β-erythroidine Hydrobromide on the α4β4 subunit could be reversed by increasing the agonist concentration. In the presence of 300 nM Dihydro-β-erythroidine Hydrobromide, the current response of α4β4-expressing oocytes to 5 μM and 500 μM ACh were 36.0 ± 9.0 % and 97.1 ± 9.6 % of the response to ACh alone, respectively.

Animal experiment [2]:

Animal models

A nicotine-induced hypothermia mouse model

Dosage form

0, 1.8, 3.6, 7.2 or 10.8 μmol/kg; s.c.

Applications

In a nicotine-induced hypothermia mouse model, Dihydro-β-erythroidine Hydrobromide dose-dependently attenuated hypothermia, with the AD50 value of 6.2 μmol/kg. But it did not have a significant effect on the non-nicotine-induced increase in body temperature at the inducated doses.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Harvey SC, Maddox FN, Luetje CW. Multiple determinants of dihydro-beta-erythroidine sensitivity on rat neuronal nicotinic receptor alpha subunits. J Neurochem. 1996 Nov;67(5):1953-9.

[2]. Damaj MI, Welch SP, Martin BR. In vivo pharmacological effects of dihydro-beta-erythroidine, a nicotinic antagonist, in mice. Psychopharmacology (Berl). 1995 Jan;117(1):67-73.

Dihydro-β-erythroidine hydrobromide Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

Dihydro-β-erythroidine hydrobromide Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Chemical Properties

Cas No. 29734-68-7 SDF Download SDF
Chemical Name (2R,4aS,7R,13bS)-2-methoxy-12-oxo-2,4a,5,6,7,8,9,10,12,13-decahydro-1H-pyrano[4',3':3,4]pyrido[2,1-i]indol-7-ium bromide
Canonical SMILES O=C1OCC2=C(C1)[C@@]3(C4)[N@@H+](CC2)CC[C@H]3C=C[C@@H]4OC.[Br-]
Formula C16H21NO3.HBr M.Wt 356.26
Solubility Soluble in DMSO > 10 mM Storage Desiccate at RT
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

IC50: 1.3 μM for α2β2, 2.3 μM for α2β4, 0.41 μM for α3β2, 23.1 μM for α3β4, 0.37 μM for α4β2, and 0.19 μM for α4β4 [1]

Dihydro-β-erythroidine hydrobromide (DHβE), the hydrogenated derivative of erythroidine, is a competitive antagonist of neuronal nicotinic acetyicholine receptors (or nAChRs). Nicotinic acetyicholine receptors are neuron receptor proteins which respond to the neurotransmitter acetylcholine.

In vitro: DHβE has been shown to be a purely competitive antagonist of the neuronal nicotinic receptor [1].

In vivo: DHβE is able to block some of the central actions of nicotine after systemic and intrathecal administration. The mechanism of blockade is different from that of mecamylamine, a classical ganglionic antagonist, and may involve a direct action of DHβE on nicotine receptor [2].

Clinical trial: DHβE can be given orally and may cross the blood-brain barriers. At 200 mg/kg, the effects were bradycardia and visual difficulty most often described as blurring of vision or double vision; at 6 mg/kg, produced aforementioned effects plus hypotension and reduction in grip strength with accompanying feelings of sedation [3].

References:
[1] Harvey SC, Maddox FN, Luetje CW.  Multiple determinants of dihydro-beta-erythroidine sensitivity on rat neuronal nicotinic receptor alpha subunits. J Neurochem. 1996 Nov;67(5):1953-9.
[2] Damaj MI, Welch SP, Martin BR.  In vivo pharmacological effects of dihydro-beta-erythroidine, a nicotinic antagonist, in mice. Psychopharmacology (Berl). 1995 Jan;117(1):67-73.
[3] MURPHREE HB.  Effects in human volunteers of subparalytic doses of dihydro-beta-erythroidine. Clin Pharmacol Ther. 1963 May-Jun;4:304-10.