Endomorphin 2, a high affinity, highly selective agonist of the μ-opioid receptor, displays reasonable affinities for kappa₃ binding sites, with K_i value between 20 and 30 nM.

Ki: 20-30 nM (kappa₃ opioid receptor)^[1]

Endomorphin 2 is an endogenous opioid peptide and one of the two Endomorphins. It is a high affinity, highly selective agonist of the μ-opioid receptor, and along with Endomorphin 1 (EM-2). The two Endomorphins display reasonable affinities for kappa₃ binding sites, with K_i values between 20 and 30 nM. Endomorphin 1 and Endomorphin 2 compete both μ₁ and μ₂ receptor sites quite potently. Endomorphins have little appreciable affinity for either delta or kappa₁ binding sites, with K_i values greater than 500 nM^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Both Endomorphin 1 and Endomorphin 2 are potent analgesics with peak effects seen at 10 and 15 min, respectively. All subsequent studies are performed at peak effect. Both compounds are fully active supraspinally and spinally, with no indication of ceiling effects. Endomorphin 1 is significantly more potent spinally than supraspinally and, at the spinal level, it is significantly more potent than Endomorphin 2. The response of both agents are readily reversed by naloxone. β-FNA, a highly selective μ antagonist, effectively reverses the actions of both Endomorphins. Both Endomorphin 1 and Endomorphin 2 display a profile similar to morphine. Neither compound have analgesic activity in CXBK mice at a dose which produced over 70% analgesia in control CD-1 mice^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

571.67

C₃₂H₃₇N₅O₅

141801-26-5

Tyr-Pro-Phe-Phe-NH2

YPFF-NH2

内吗啡肽 2

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

H₂O

Peptide Solubility and Storage Guidelines:

1.;;Calculate the length of the peptide.

2.;;Calculate the overall charge of the entire peptide according to the following table:

3.;;Recommended solution:

• [1]. Goldberg IE, et al. Pharmacological characterization of endomorphin-1 and endomorphin-2 in mouse brain. J Pharmacol Exp Ther. 1998 Aug;286(2):1007-13.

¹²⁵I-Endomorphin 1 or ¹²⁵I-Endomorphin 2 binding (0.2 nM) is performed in potassium phosphate buffer (50 mM, pH 7.4; 0.5 mL) with MgCl₂ (5 mM) 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 1 μM of the corresponding unlabeled peptide. The entire mixture is then incubated at 25°C for 1 hr and filtered over no. 32 glass fiber filters which have been presoaked for 1 hr in 0.5% polyethylenimine 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^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Mice^[1]
Groups of mice are treated i.c.v. with Endomorphin 1 (12 μg) or Endomorphin 2 (3 μg) 15 min before a 0.5-cc charcoal meal (2.5% gum tragacanth,10% activated charcoal in water). The mice are killed 30 min later and the distance the charcoal traveled is measured.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

• [1]. Goldberg IE, et al. Pharmacological characterization of endomorphin-1 and endomorphin-2 in mouse brain. J Pharmacol Exp Ther. 1998 Aug;286(2):1007-13.