A G-protein biased μ-opioid receptor agonist (Ki= 1 nM in HEK293 cell membranes expressing the mouse receptor); selective for the μ-opioid receptor over the nociceptin receptor and δ- and κ-opioid receptors

TRV-130 (hydrochloride) – 5 mg

Brand:
Cayman
CAS:
1401031-39-7
Storage:
-20
UN-No:
Non-Hazardous - /

TRV-130 is a G-protein biased μ-opioid receptor agonist (Ki = 1 nM in HEK293 cell membranes expressing the mouse receptor).{61001} It is selective for the μ-opioid receptor over the nociceptin receptor and δ- and κ-opioid receptors, as well as a panel of 120 additional receptors, channels, and enzymes at 10 μM. TRV-130 inhibits forskolin-induced cAMP accumulation, a marker of G-protein signaling, with an EC50 value of 0.4 nM, but has limited effects on β-arrestin-2 recruitment (EC50s = 12.6 nM). TRV-130 increases the latency to paw withdrawal in the hot plate test in rats with an ED50 value of 0.32 mg/kg, which is 10-fold more potent than morphine. It exhibits reduced increases in blood peak partial pressure of carbon dioxide (pCO2) levels, a marker of respiratory depression, compared with morphine when administered at equianalgesic doses in rats.  

 

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SKU: 30624 - 5 mg Category:

Description

A G-protein biased μ-opioid receptor agonist (Ki= 1 nM in HEK293 cell membranes expressing the mouse receptor); selective for the μ-opioid receptor over the nociceptin receptor and δ- and κ-opioid receptors, as well as a panel of 120 additional receptors, channels, and enzymes at 10 μM; inhibits forskolin-induced cAMP accumulation (EC50 = 0.4 nM), but has limited effects on β-arrestin-2 recruitment (EC50 = 12.6 nM); increases the latency to paw withdrawal in the hot plate test in rats (ED50 = 0.32 mg/kg); exhibits reduced increases in blood peak pCO2 levels compared with morphine at equianalgesic doses in rats

Formal name: (9R)-N-[(3-methoxy-2-thienyl)methyl]-9-(2-pyridinyl)-6-oxaspiro[4.5]decane-9-ethanamine, monohydrochloride

Synonyms: 

Molecular weight: 423

CAS: 1401031-39-7

Purity: ≥95%

Formulation: A crystalline solid

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