CAS |
170098-38-1 |
Chinese Name |
爱维莫潘二水合物 |
English Name |
Alvimopan dihydrate |
Synonyms |
爱维莫潘;爱维莫潘二水合物; |
Molecular Formula |
C25H36N2O6 |
Molecular Weight |
460.56 |
Solubility |
Soluble in DMSO |
Purity |
≥98% |
Appearance |
White to off-white Solid |
Storage |
Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year |
MDL |
MFCD26142939 |
SMILES |
OC1=CC=CC([C@@]2(C)[C@@H](C)CN(C[C@H](CC3=CC=CC=C3)C(NCC(O)=O)=O)CC2)=C1.O.O |
InChIKey |
USPVLEIQIUNQGE-DBFLIVQGSA-N |
InChI |
InChI=1S/C25H32N2O4.2H2O/c1-18-16-27(12-11-25(18,2)21-9-6-10-22(28)14-21)17-20(24(31)26-15-23(29)30)13-19-7-4-3-5-8-19;;/h3-10,14,18,20,28H,11-13,15-17H2,1-2H3,(H,26,31)(H,29,30);2*1H2/t18-,20-,25+;;/m0../s1 |
PubChem CID |
5488547 |
Target Point |
Opioid Receptor |
Passage |
GPCR & G Protein;Neuronal Signaling |
Background |
Alvimopan dihydrate is a potent, relatively nonselective opioid antagonist |
Biological Activity |
Alvimopan dihydrate (ADL 8-2698 dihydrate) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC50 of 1.7 nM. Alvimopan dihydrate has selectivity for μ-opioid receptor (Ki=0.47 nM) over κ- and δ-opioid receptors (Kis=100, 12 nM, respectively). Alvimopan dihydrate can be used for the research of postoperative ileus[1-[3]. |
IC50 |
1.7nM(μ-opioid receptor)[1] |
In Vitro |
Alvimopan inhibits the loperamide-stimulated [35S]GTPγS binding to membranes containing the cloned human μ-opioid receptor,with an IC50 of 1.7 nM[1]. |
In Vivo |
Alvimopan(0.1-1.0 mg/kg; p.o.)partially antagonizes the slowing of small intestinal transit of 113Sn-labelled microspheres produced by morphine in rats.Alvimopan(3 mg/kg; p.o.)has no effect on the visceromotor behavioural responses(VMR)induced by noxious colorectal distension(CRD)in conscious rats[3]. |
Data Literature Source |
[1] Goldina Ikezuagu Erowele. P T. 2008,33(10): 574,580-583. [2] DT Beattie. Clinical Medicine: Therapeutics. 2009,1: 199-213. |
Unit |
Bottle |
Specification |
5mg 10mg 50mg |