| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| 500mg |
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| Other Sizes |
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| Targets |
DR/Dopamine receptor
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|---|---|
| ln Vivo |
We describe induction time in six white rhinoceros (Ceratotherium simum) when they received etorphine intramuscularly (IM) or etorphine plus azaperone IM. The median induction time was reduced from 8.9 min for etorphine alone to 6.25 min with azaperone; however, there was no difference in immobilization quality between treatments[1].
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| Animal Protocol |
Six male white rhinoceros (5–6 y old) were captured in the Kruger National Park (23°49′60 S, 31°30′0 E; altitude 317 m), South Africa, and habituated over 4 mo to captivity in holding pens. These animals were part of a multifaceted crossover study with two randomly allocated (computer-generated) interventions separated by a minimum 2-wk washout period between treatments (Buss et al. 2016, 2018). The rhinoceros were administered the following treatments, which included hyaluronidase (5000 IU); etorphine hydrochloride (9.8 mg/mL IM, M99), or etorphine and azaperone (40 mg/mL IM). Total doses were 2.5 mg etorphine, 37.5 mg azaperone (for a 1,000–1,250-kg rhinoceros), and 3.0 mg etorphine, 45 mg azaperone (for a 1,250–1,500-kg rhinoceros), giving etorphine 0.002–0.0025 mg/kg and azaperone 0.03–0.0375 mg/kg (Haw et al. 2014; Buss et al. 2016). At the end of each trial, the rhinoceros was weighed; its body mass was used to determine treatment drug doses and to monitor the animal's health.[1]
We administered immobilization drugs into the nuchal hump using a 3.0-mL plastic dart with a 60-mm uncollared needle propelled from a compressed air rifle. Induction time was measured from the time of dart placement to when the animal could be safely placed in sternal recumbency. Immobilization quality score was subjectively assessed as 1–4 by the same observer using established criteria (Table 1) at 10 min after a rhinoceros became recumbent (t=0). At the end of each trial, a rhinoceros was administered naltrexone (40 mg/mL) intravenously at 20 times the etorphine dose (milligrams) and observed until fully recovered.[1] |
| References |
[1]. Effect of Azaperone on Induction Times in Etorphine-Immobilized White Rhinoceros (Ceratotherium simum). J Wildl Dis. 2022 Jan 1;58(1):245-247.
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| Additional Infomation |
Azaperone is an N-arylpiperazine that is 2-(piperazin-1-yl)pyridine in which the amino hydrogen is replaced by a 3-(4-fluobenzoyl)propyl group. Used mainly as a tranquiliser for pigs and elephants. It has a role as an antipsychotic agent and a dopaminergic antagonist. It is a N-arylpiperazine, a N-alkylpiperazine, an aminopyridine, a tertiary amino compound, a member of monofluorobenzenes and an aromatic ketone.
Azaperone is a pyridinylpiperazine and butyrophenone agent that is capable of eliciting neuroleptic sedative and antiemetic effects. It is subsequently employed predominantly as a veterinary tranquilizer and mainly for pigs and elephants. At the same time, the agent generally does not see equine use as particular adverse reactions may happen. More rarely it may be used in humans as an antipsychotic drug, but this is uncommon. A butyrophenone used in the treatment of PSYCHOSES. |
| Molecular Formula |
C19H22FN3O
|
|---|---|
| Molecular Weight |
327.3959
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| Exact Mass |
327.174
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| Elemental Analysis |
C, 69.70; H, 6.77; F, 5.80; N, 12.83; O, 4.89
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| CAS # |
1649-18-9
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| Related CAS # |
Azaperone-d4;1173021-72-1; 1649-18-9; 59698-53-2 (dimaleate)
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| PubChem CID |
15443
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| Appearance |
Typically exists as Light yellow to yellow solids at room temperature
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
499.5±45.0 °C at 760 mmHg
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| Melting Point |
92-95ºC
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| Flash Point |
255.9±28.7 °C
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| Vapour Pressure |
0.0±1.3 mmHg at 25°C
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| Index of Refraction |
1.568
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| LogP |
2.5
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
24
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| Complexity |
390
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC1C([H])=C([H])C(=C([H])C=1[H])C(C([H])([H])C([H])([H])C([H])([H])N1C([H])([H])C([H])([H])N(C2=C([H])C([H])=C([H])C([H])=N2)C([H])([H])C1([H])[H])=O
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| InChi Key |
XTKDAFGWCDAMPY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H22FN3O/c20-17-8-6-16(7-9-17)18(24)4-3-11-22-12-14-23(15-13-22)19-5-1-2-10-21-19/h1-2,5-10H,3-4,11-15H2
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| Chemical Name |
1-(4-fluorophenyl)-4-(4-pyridin-2-ylpiperazin-1-yl)butan-1-one
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| Synonyms |
Azaperone; 1649-18-9; Stresnil; Azaperon; Fluoperidol; Suicalm; Eucalmyl; Fluoperidol; Eucalmyl; Azeperone;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~152.72 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.64 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.64 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.64 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0544 mL | 15.2718 mL | 30.5437 mL | |
| 5 mM | 0.6109 mL | 3.0544 mL | 6.1087 mL | |
| 10 mM | 0.3054 mL | 1.5272 mL | 3.0544 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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