Nortilidine

Nortilidine

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Nortilidine
Drug
Nortilidine is the major active metabolite of tilidine. It is formed from tilidine by demethylation in the liver. The racemate has opioid analgesic effects roughly equivalent in potency to that of morphine but virtually all of the opioid activity resides in the (1S,2R) isomer.

Nortilidine – Wikipediaen.wikipedia.org › wiki › Nortilidine
Description
Formula: C16H21NO2
Molar mass: 259.3434 g/mol
ChemSpider ID: 142535
ChEMBL Id: 1614654
ChemSpider ID: 142535
PubChem CID: 162321

Description

Description

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Buy Nortilidine online
Drug
Nortilidine is the major active metabolite of tilidine. It is formed from tilidine by demethylation in the liver. The racemate has opioid analgesic effects roughly equivalent in potency to that of morphine but virtually all of the opioid activity resides in the (1S,2R) isomer.

Nortilidine – Wikipediaen.wikipedia.org › wiki › Nortilidine
Description
Formula: C16H21NO2
Molar mass: 259.3434 g/mol
ChemSpider ID: 142535
ChEMBL Id: 1614654
ChemSpider ID: 142535
PubChem CID: 162321

 

Abstract

Tilidine, alone or combined with naloxone to prevent drug abuse, is used as an oral opioid analgesic. Although the analgesic action of tilidine and its active metabolite nortilidine is reversed by naloxone and therefore believed to involve the activation of the Mu opioid (MOP, OP3, mu) receptor, this has never been studied in recombinant systems. We have measured the selectivity of tilidine and nortilidine for human opioid and opioid-like receptors stably expressed in CHO-K1 cells, using the inhibition of the forskolin (FK)-induced accumulation of cAMP as endpoint. In cells expressing the MOP receptor, tilidine and nortilidine inhibited cAMP accumulation with IC50 of 11 microM and 110 nM, respectively. The agonist effects of nortilidine and [D-Ala2-MePhe4-Gly5-ol]enkephalin (DAMGO) on the MOP receptor were reversed by naloxone with very similar IC50 (1.2 versus 1.8 nM). At concentrations up to 100 microM, tilidine and nortilidine had no agonist effect on the DOP, KOP and NOP receptors. In conclusion, this study on cloned human receptors demonstrates that nortilidine is a selective agonist of the MOP receptor.

 

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Nortilidine is the primary, active metabolite of tilidine, a synthetic opioid analgesic used mainly in Germany, Switzerland and Belgium for treatment of moderate to severe pain, both acute and chronic.

Properties
Related Categories Additional Standards, Analgesics (non-opiates), Analytical Standards, Analytical/Chromatography, Certified Reference Materials (CRMs),
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Quality Level 100
grade certified reference material
feature Snap-N-Spike®/Snap-N-Shoot®
packaging ampule of 1 mL
mfr. no. Cerilliant®
concentration 1.0 mg/mL in methanol (as free base)
Featured Industry Pharmaceutical (small molecule)
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Description
General description
Nortilidine is the primary, active metabolite of tilidine, a synthetic opioid analgesic used mainly in Germany, Switzerland and Belgium for treatment of moderate to severe pain, both acute and chronic. This new Snap-N-Spike® solution standard is suitable for numerous GC/MS and LC/MS applications from clinical toxicology and forensic analysis to calibrator preparation and urine drug testing.

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Legal Information
CERILLIANT is a registered trademark of Cerilliant Corporation

Snap-N-Shoot is a registered trademark of Cerilliant Corporation

Snap-N-Spike is a registered trademark of Cerilliant Corporation

Buy Nortilidine Online to be used for treatment of moderate to severe pain, both acute and chronic.

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