BRL 44408 maleate


Catalog No. Size PriceQuantity
M22725-C Contact sales@xcessbio.com for quotation $100Unavailable

Description

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 . 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 . 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 .

Product information

CAS Number: 118343-19-4

Molecular Weight: 331.37

Formula: C17H21N3O4

Chemical Name: (2Z)-but-2-enedioic acid; 2-[(4,5-dihydro-1H-imidazol-2-yl)methyl]-1-methyl-2,3-dihydro-1H-isoindole

Smiles: CC1C2=CC=CC=C2CN1CC1NCCN=1.OC(=O)/C=C\C(O)=O

InChiKey: DDIQGSUEJOOQQQ-BTJKTKAUSA-N

InChi: InChI=1S/C13H17N3.C4H4O4/c1-10-12-5-3-2-4-11(12)8-16(10)9-13-14-6-7-15-13;5-3(6)1-2-4(7)8/h2-5,10H,6-9H2,1H3,(H,14,15);1-2H,(H,5,6)(H,7,8)/b;2-1-

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

Products are for research use only. Not for human use.

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