FK 33-824
FK 33-824 is a μ-opioid receptor agonist. FK 33-824 binds μ/δ opioid receptors to an equal extent, increases hippocampal CA1 population spikes, and inhibits basal and vasopressin-stimulated pituitary ACTH release and Oestradiol secretion. FK 33-824 inhibits sensory-evoked dorsal horn responses accompanied by chronic tolerance/cross-tolerance, produces analgesic effects, and abolishes estradiol responses.
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- CAS No.: 64854-64-4
- Formule: C29H41N5O7S
- Masse moléculaire:603.73
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
Description
IC50 & Target
[1]|
μ Opioid Receptor/MOR |
δ Opioid Receptor/DOR |
In Vitro
FK 33-824 (0.1 µM; 3 h) does not directly affect basal or dopamine-inhibited PRL release from the anterior pituitary of female Wistar rats in vitro[1].
FK 33-824 increases the population spike response evoked in rat hippocampal CA1 slices, with an EC50 of 13 nM[2].
FK 33-824 (1 nM; up to 30 min) does not significantly affect phospholipase C-mediated inositol phosphate accumulation in porcine granulosa cells from large follicles[4].
FK 33-824 (1 nM; 4 h) maintains the inhibition of E2 secretion in PKC-deficient porcine granulosa cells[4].
FK 33-824 (1 nM; 4 h) inhibits E2 secretion in porcine granulosa cells, and PMA at 10 and 100 nM abolishes this inhibition[4].
FK 33-824 (1 nM) completely eliminates hCG-stimulated progesterone secretion in porcine small luteal cells, but does not affect basal progesterone secretion in SLCs or LLCs[7].
FK 33-824 (1 nM; 12 h) increases cAMP release in porcine large luteal cells and decreases cGMP release in porcine small luteal cells within 12 hours[7].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CD-COBS (male, Charles River Italy, 180-200 g, overnight fasted)[5]
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Dosage:Various dosages
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Administration:i.p.; single administration; 5 min before charcoal test meal
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Result:Dose-dependently inhibited gastrointestinal transit of the charcoal test meal.
The dose reducing test meal progression to 50% of controls (ID50) was 1.0 µg/kg alone.
In the presence of N-methyl naloxone, the FK 33-824 ID50 was 3.6 µg/kg at 75 µg/kg antagonist, 7.3 µg/kg at 150 µg/kg antagonist, and 26.5 µg/kg at 450 µg/kg antagonist.
The apparent pA2 for N-methyl naloxone against FK 33-824 was 7.10.
Near-maximal inhibition of transit by FK 33-824 was virtually fully prevented at the highest doses of N-methyl naloxone.
Chemical Information
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CAS No. 64854-64-4
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Masse moléculaire 603.73
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Formule C29H41N5O7S
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Sequence
Tyr-dAla-Gly-MePhe-Met(O)-ol
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Sequence Shortening
Y-dAla-G-N-Me-FM(O)-ol
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)