Description
ARC 239 dihydrochloride is a selective antagonist of α2B adrenoceptor with pKD value of 8.8 . α2B 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. ARC 239 dihydrochloride is a selective α2B adrenoceptor antagonist. In rat brain, ARC 239 inhibited the binding of 5-HTIA receptor radioligands 8-OH-DPAT and RX 821002 to cortical membranes with Ki values of 63.1 and 136 nM respectively, which suggested that ARC 239 recognized 5-HT1A receptor . Treatment human platelets with ARC 239 significantly inhibited platelet aggregation induced by adenosine diphosphate (ADP), epinephrine and arachidonic acid and increased collagen/epinephrine closure time, which suggested that α2B adrenoceptor play a critical role in platelet aggregation . In cervical samples isolated from pregnant rats, ARC 239 effectively inhibited noradrenaline-stimulated contractions . In C57BL/6 mice with gastric mucosal damage induced by acidified ethanol, ARC 239 (10.4 nM) antagonized gastroprotective effect induced by α2-adrenoceptor agonists .
Product information
CAS Number: 55974-42-0
Molecular Weight: 480.43
Formula: C24H31Cl2N3O3
Chemical Name: 2-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-4,4-dimethyl-1,2,3,4-tetrahydroisoquinoline-1,3-dione dihydrochloride
Smiles: Cl.Cl.CC1(C)C2=CC=CC=C2C(=O)N(CCN2CCN(CC2)C2=CC=CC=C2OC)C1=O
InChiKey: SAJKHRHHDGSJEZ-UHFFFAOYSA-N
InChi: InChI=1S/C24H29N3O3.2ClH/c1-24(2)19-9-5-4-8-18(19)22(28)27(23(24)29)17-14-25-12-15-26(16-13-25)20-10-6-7-11-21(20)30-3;;/h4-11H,12-17H2,1-3H3;2*1H
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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