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BRL 44408 (maleate)

Catalog No.
B6610
Selective α2A-AR antagonist
Grouped product items
SizePriceStock Qty
50mg
$1,386.00
Ship with 5-10 days
5mg
$120.00
Ship with 5-10 days
10mg
$210.00
Ship with 5-10 days
25mg
$465.00
Ship with 5-10 days
For scientific research use only and should not be used for diagnostic or medical purposes.

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Email: [email protected]

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Background

BRL 44408 maleate is a selective antagonist of α2A-adrenoceptor with Ki values of 1.7 and 144.5 nM for α2A- and α2B-adrenoceptors, respectively.

α2A-adrenoceptor is a G-protein coupled receptor. α2-adrenergic receptors include three subtypes: α2A, α2B and α2C, which play an important role in regulating neurotransmitter release from adrenergic neurons in the central nervous system and from sympathetic nerves.

BRL 44408 maleate is a selective α2A-adrenoceptor antagonist. In rat brain, BRL 44408 inhibited the binding of 5-HTIA receptor radioligands 8-OH-DPAT and RX 821002 to cortical membranes with Ki values of 199 and 338 nM respectively, which suggested that BRL 44408 recognized 5-HT1A receptor [1].

In wild type and monoamine oxidase-A knockout (MAO-A KO) mice, BRL 44408 (100 nM) inhibited the effect of dexmedetomidine, the α2 agonist. BRL 44408 (100 nM) increased evoked noradrenaline (NA) efflux in MAO-A KO mice. In wild type mice, BRL 44408 antagonized the agonist effect of dexmedetomidine with pKB value of 7.75, which inhibited locus coeruleus (LC) cell firing with EC50 value of 2.6 nM [2]. In the forced swim test, BRL 44408 reduced immobility time. In schedule-induced polydipsia assay, BRL 44408 increased adjunctive water intake, which suggested that BRL 44408 exhibited antidepressant-like response. In a visceral pain model, BRL 44408 exhibited analgesic activity [3].

References:
[1].  Meana JJ, Callado LF, Pazos A, et al. The subtype-selective alpha 2-adrenoceptor antagonists BRL 44408 and ARC 239 also recognize 5-HT1A receptors in the rat brain. Eur J Pharmacol, 1996, 312(3): 385-388.
[2].  Owesson CA, Seif I, McLaughlin DP, et al. Different alpha(2) adrenoceptor subtypes control noradrenaline release and cell firing in the locus coeruleus of wildtype and monoamine oxidase-A knockout mice. Eur J Neurosci, 2003, 18(1): 34-42.
[3].  Dwyer JM, Platt BJ, Rizzo SJ, et al. Preclinical characterization of BRL 44408: antidepressant- and analgesic-like activity through selective alpha2A-adrenoceptor antagonism. Int J Neuropsychopharmacol, 2010, 13(9): 1193-1205.

Chemical Properties

Physical AppearanceA crystalline solid
StorageDesiccate at -20°C
M.Wt331.4
Cas No.681806-46-2
FormulaC13H17N3·C4H4O4
Solubility<33.14mg/ml in H2O
Chemical Name2-[(4,5-dihydro-1H-imidazol-2-yl)methyl]-2,3-dihydro-1-methyl-1H-isoindole, 2Z-butenedioate
SDFDownload SDF
Canonical SMILESCC1C2=CC=CC=C2CN1CC3=NCCN3.OC(/C(C)=C\C(O)=O)=O
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Quality Control

Quality Control & MSDS

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Chemical structure

BRL 44408 (maleate)