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  4. Org 9616 bromide

Org 9616 bromide is a non-depolarizing neuromuscular blocker with a structure similar to Pancuroniam. Org 9616 bromide induces rapid-onset, short-duration neuromuscular blockade.

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Org 9616 bromide

Org 9616 bromide Chemical Structure

CAS No. : 119302-18-0

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Description

Org 9616 bromide is a non-depolarizing neuromuscular blocker with a structure similar to Pancuroniam. Org 9616 bromide induces rapid-onset, short-duration neuromuscular blockade[1].

Parmacokinetics
Species Dose Route T1/2 (Distribution) T1/2β V1 Vdss CL MRT
Cat[1] 1.2 mg/kg i.v. 2.5 min 25.9 min 149 mL/kg 346 mL/kg 28.2 mL/min/kg 11.1 min
In Vivo

Org 9616 (1.2 mg/kg; i.v.; bolus) bromide produces short-duration neuromuscular blockade in intact cats, with a duration of action of 14.6 minutes at a 1.2 mg/kg i.v. bolus dose, and is cleared via biotransformation and biliary excretion[1].
Org 9616 (1.2 mg/kg; i.v.; bolus) bromide produces short-duration neuromuscular blockade in cats with ligated renal pedicles, with a duration of action of 15.4 minutes at a 1.2 mg/kg i.v. bolus dose, and renal pedicle ligation shortens its recovery index while prolonging elimination half-life and mean residence time[1].

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

Animal Model: either sex, 2-4 kg[1]
Dosage: 1.2 mg/kg
Administration: i.v.; bolus
Result: Achieved onset time to maximum twitch depression of 0.7 minutes.
Reached duration of action (time to 25% twitch recovery) of 14.6 minutes.
Attained recovery index (25-75% twitch recovery) of 6.3 minutes.
Excreted 4.6% of the dose unchanged in urine, 20.4% unchanged in bile, and left 4.2% unchanged in the liver over 8 hours.
Excreted 1.4% of the dose as the 3-desacetyl metabolite in urine, 15.3% in bile, and left 9.8% in the liver over 8 hours.
Achieved total recovery of parent drug plus metabolite of 65% of the injected dose.\nAchieved onset time to maximum twitch depression of 0.5 minutes.
Reached duration of action (time to 25% twitch recovery) of 15.4 minutes.
Attained recovery index (25-75% twitch recovery) of 3.8 minutes, which was significantly shorter than in cats with intact renal pedicles (P < 0.05).
Showed prolonged mean elimination half-life and longer mean residence time compared to cats with intact renal pedicles.
Excreted 27.7% of the dose unchanged in bile, and left 3.6% unchanged in the liver over 8 hours.
Excreted 19.1% of the dose as the 3-desacetyl metabolite in bile, and left 14.5% in the liver over 8 hours.
Achieved total recovery of parent drug plus metabolite of 55% of the injected dose.
Molecular Weight

665.78

Formula

C36H61BrN2O4
CAS No.
SMILES

C[C@@]12[C@](C[C@H]([N+]3(CCCCC3)C)[C@H]2OC(CCC)=O)([H])[C@@]4([H])[C@]([C@@]5([C@@](C[C@@H]([C@@H](N6CCCCC6)C5)OC(C)=O)([H])CC4)C)([H])CC1.[Br-]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
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Org 9616 bromide Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Org 9616119302-18-0Org9616Org-9616Drug DerivativeDrug derivativerenal pedicle ligationneuromuscular junction nicotinic acetylcholine receptorsuccinylcholinehepatic exclusionneuromuscular blockadeneuromuscular blocking agent3-desacetyl metabolitebiliary excretioncatsvecuroniumInhibitorinhibitorinhibit

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