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Azaperone

CAS# 1649-18-9

Azaperone

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Chemical Properties of Azaperone

Cas No. 1649-18-9 SDF Download SDF
PubChem ID 15443 Appearance Powder
Formula C19H22FN3O M.Wt 327.4
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : 50 mg/mL (152.72 mM; Need ultrasonic)
H2O : < 0.1 mg/mL (insoluble)
Chemical Name 1-(4-fluorophenyl)-4-(4-pyridin-2-ylpiperazin-1-yl)butan-1-one
SMILES C1CN(CCN1CCCC(=O)C2=CC=C(C=C2)F)C3=CC=CC=N3
Standard InChIKey XTKDAFGWCDAMPY-UHFFFAOYSA-N
Standard InChI 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
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Azaperone

DescriptionAzaperone acts as a dopamine antagonist but also has some antihistaminic and anticholinergic properties. Azaperone is a pyridinylpiperazine and butyrophenone neuroleptic drug with sedative and antiemetic effects, which is used mainly as a tranquilizer in veterinary medicine.

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Preparing Stock Solutions of Azaperone

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.0544 mL 15.2718 mL 30.5437 mL 61.0874 mL 76.3592 mL
5 mM 0.6109 mL 3.0544 mL 6.1087 mL 12.2175 mL 15.2718 mL
10 mM 0.3054 mL 1.5272 mL 3.0544 mL 6.1087 mL 7.6359 mL
50 mM 0.0611 mL 0.3054 mL 0.6109 mL 1.2217 mL 1.5272 mL
100 mM 0.0305 mL 0.1527 mL 0.3054 mL 0.6109 mL 0.7636 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Azaperone

Azaperone is a pyridinylpiperazine and butyrophenone neuroleptic drug with sedative and antiemetic effects, which is used mainly as a tranquilizer in veterinary medicine.

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References on Azaperone

Evaluation of BAM (butorphanol-azaperone-medetomidine) in captive African lion (Panthera leo) immobilization.[Pubmed:28330727]

Vet Anaesth Analg. 2017 Jul;44(4):883-889.

OBJECTIVE: The combination of butorphanol, Azaperone and medetomidine (BAM) with subsequent antagonism by naltrexone-yohimbine or naltrexone-atipamezole was evaluated for reversible immobilization of captive African lions (Panthea leo). STUDY DESIGN: Prospective, clinical trial. ANIMALS: Twenty lions, 11 males and nine females, weighing 38-284 kg were immobilized in South Africa. METHODS: The BAM volume dose rate administered was 0.005-0.008 mL kg(-1) (0.6 mL 100 kg(-1)). Physiologic variables were recorded every 5 minutes. Four arterial blood samples were collected from all animals at 20, 30, 40 and 50 minutes after immobilization for analysis of blood-gases and acid-base status. RESULTS: The actual doses administered were as follows: butorphanol, 0.18+/-0.03 mg kg(-1); Azaperone, 0.07+/-0.01 mg kg(-1); and medetomidine, 0.07+/-0.01 mg kg(-1). The inductions were calm and smooth, and induction time ranged from 4 to 10 minutes (7+/-2 minutes). The amount of time needed to work with each lion was 70 minutes, and no additional drug doses were needed. Heart rate (40+/-8 beats minute(-1)) and respiratory frequency (15+/-4 breaths minute(-1)) were stable throughout immobilization. The mean arterial blood pressure of all animals was stable but elevated (142+/-16 mmHg). The rectal temperature slightly increased over time but remained within acceptable range. The recovery time was significantly shorter when using naltrexone and atipamezole (9+/-1 minutes) compared to using naltrexone and yohimbine (22+/-7 minutes). CONCLUSION AND CLINICAL RELEVANCE: The BAM combination proved to be reliable for general veterinary anaesthesia in lions. During anaesthesia, minor veterinary procedures such a blood collection, intubation, vaccination and collaring could safely be performed with no additional dosing required.

Tremors in white rhinoceroses (Ceratotherium simum) during etorphine-azaperone immobilisation.[Pubmed:28281770]

J S Afr Vet Assoc. 2017 Feb 24;88(0):e1-e10.

Little is known about the mechanisms causing tremors during immobilisation of rhinoceros and whether cardiorespiratory supportive interventions alter their intensity. Therefore, we set out to determine the possible mechanisms that lead to muscle tremors and ascertain whether cardiorespiratory supportive interventions affect tremor intensity. We studied tremors and physiological responses during etorphine-Azaperone immobilisation in eight boma-held and 14 free-living white rhinoceroses. Repeated measures analysis of variance and a Friedman test were used to determine differences in variables over time and between interventions. Spearman and Pearson correlations were used to test for associations between variables. Tremor intensity measured objectively by activity loggers correlated well (p < 0.0001; r2 = 0.9) with visual observations. Tremor intensity was greatest when animals were severely hypoxaemic and acidaemic. Tremor intensity correlated strongly and negatively with partial pressure of oxygen (PaO2 ) (p = 0.0003; r2 = 0.9995) and potential of hydrogen (pH) (p = 0.02, r2 = 0.97). It correlated strongly and positively with adrenaline concentrations (p = 0.003; r2 = 0.96), and adrenaline correlated strongly and negatively with PaO2 (p = 0.03; r2 = 0.95) and pH (p = 0.03; r2 = 0.94). Therefore, hypoxaemia and acidaemia were likely associated with the intensity of tremors through their activation of the release of tremorgenic levels of adrenaline. Tremors can be reduced if circulating adrenaline is reduced, and this can be achieved by the administration of butorphanol plus oxygen insufflation. Furthermore, to assist with reducing the risks associated with rhinoceros immobilisation, tremor intensity could be used as a clinical indicator of respiratory and metabolic compromise.

COMPARISON OF MEDETOMIDINE-KETAMINE AND BUTORPHANOL-AZAPERONE-MEDETOMIDINE IN CAPTIVE BENNETT'S WALLABIES (MACROPUS RUFOGRISEUS).[Pubmed:28080912]

J Zoo Wildl Med. 2016 Dec;47(4):1019-1024.

The objective of this study was to compare a traditional partially reversible medetomidine-ketamine sedation with a more reversible butorphanol-Azaperone-medetomidine combination in Bennett's wallabies ( Macropus rufogriseus ) maintained in a zoological collection. Fourteen animals were divided into two treatment groups. Individuals in group 1 received an intramuscular (i.m.) injection of butorphanol (0.54 +/- 0.05 mg/kg), Azaperone (0.22 +/- 0.02 mg/kg), and medetomidine (0.16 +/- 0.02 mg/kg). Individuals in group 2 received an i.m. injection of ketamine (5.43 +/-1.16 mg/kg) with medetomidine (0.05 +/- 0.014 mg/kg). For group 1, sedation was reversed with atipamezole (0.81 +/- 0.069 mg/kg i.m.) and naltrexone (1.08 +/- 0.09 mg/kg i.m.). For group 2, sedation was reversed with atipamezole (0.27 +/- 0.056 mg/kg i.m.). There were no significant differences between the groups in mean time to induction, time spent on gas anesthesia, or time to standing after reversal was administered. Animals in both groups required supplemental gas anesthesia to facilitate intubation. No adverse reactions or effects were noted with either protocol; however, the BAM protocol did not provide sufficient sedation for handling in all animals and may not be suitable for use in this species.

CAPTURE OF FREE-RANGING MULE DEER (ODOCOILEUS HEMIONUS) WITH A COMBINATION OF MEDETOMIDINE, AZAPERONE, AND ALFAXALONE.[Pubmed:28151080]

J Wildl Dis. 2017 Apr;53(2):296-303.

The combination of medetomidine, Azaperone, and alfaxalone has been successfully used to anesthetize captive white-tailed deer ( Odocoileus virginianus ). This same combination was utilized to immobilize free-ranging female mule deer ( Odocoileus hemionus ; MD) in urban and nonurban environments (14 urban MD, 14 nonurban MD) in British Columbia, Canada. Physiologic data were collected to assess the safety and reliability of this drug combination under field conditions. Each deer received estimated dosages of 0.15 mg/kg medetomidine, 0.2 mg/kg Azaperone, and 0.5 mg/kg alfaxalone intramuscularly via a remote darting system. Inductions were calm and rapid (mean time to sternal recumbency: urban MD, 6.4+/-2.2 min; nonurban MD, 8.2+/-4.1 min). Supplemental drugs were required to induce lateral recumbency in five deer, four of which had experienced initial dart failure (mean time to lateral recumbency: urban MD, 8.5+/-3.8 min; nonurban MD, 18.7+/-16.5 min). Recoveries were smooth and uneventful (time to standing: urban MD, 12.5+/-3.4 min; nonurban MD, 9.0+/-3.5 min) for all but one debilitated nonurban MD that died shortly after atipamezole administration (at five times the medetomidine dose). The major side effects of the combination were hypoxemia and hypercapnia. The combination of medetomidine, Azaperone, and alfaxalone proved suitable for the immobilization of urban and nonurban free-ranging MD.

Description

Azaperone (R-1929) acts as a dopamine antagonist but also has some antihistaminic and anticholinergic properties. Azaperone is a pyridinylpiperazine and butyrophenone neuroleptic drug with sedative and antiemetic effects, which is used mainly as a tranquilizer in veterinary medicine.

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