Endomorphin-1 Inhibitor

Solid. Powder

98.00%

Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent

610.67

Water: 24mg/mL (39.3mM) Need ultrasonic
(<1mg/ml refers to the product slightly soluble or insoluble)

C34H38N6O5

N[C@@H](Cc(cc1)ccc1O)C(N(CCC1)[C@@H]1C(N[C@@H](Cc1c[nH]c2c1cccc2)C(N[C@@H](Cc1ccccc1)C(N)=O)=O)=O)=O

189388-22-5

125I-Endomorphin 1 or 125I-Endomorphin 2 binding (0.2nM) is performed in potassium phosphate buffer (50mM, pH 7.4; 0.5 mL) with MgCl2 (5mM) at a tissue concentration of 10 mg wet weight/mL for brains or 0.06 mg protein/mL for MOR-1/CHO cells. Specific binding is determined in the presence and absence of either 1uM of the corresponding unlabeled peptide. The entire mixture is then incubated at 25 degree C for 1 hr and filtered over no. 32 glass fiber filters which have been presoaked for 1 hr in 0.5% polyethyleneimine and washed twice with ice-cold Tris buffer using a Brandel cell harvester. The filters are then counted on a Packard Cobra gamma counter. The other opioid receptor binding assays are performed.

Both Endomorphin 1 and Endomorphin 2 are potent analgesics with peak effects seen at 10 and 15 minutes, respectively. All subsequent studies are performed at peak effect. Both compounds are fully active supraspinally and spinally, with no indication of ceiling effects. Both Endomorphin 1 and Endomorphin 2 display a profile similar to morphine. Neither compound has analgesic activity in CXBK mice at a dose that produced over 70% analgesia in control CD-1 mice.

Endocrinology/Hormones; Opioid Receptor; Neuroscience