Azaperone

Catalog No.S4219 Synonyms: NSC 170976

For research use only.

Azaperone (NSC 170976,Ketamine) crosses the blood-brain barrier and binds to both DI and D2 receptors, being an antagonist of Dopamine receptors with sedative and antiemetic effects, which is used mainly as a tranquilizer in veterinary medicine.

Azaperone Chemical Structure

CAS No. 1649-18-9

Selleck's Azaperone has been cited by 1 Publication

Purity & Quality Control

Choose Selective Dopamine Receptor Inhibitors

Other Dopamine Receptor Products

Biological Activity

Description Azaperone (NSC 170976,Ketamine) crosses the blood-brain barrier and binds to both DI and D2 receptors, being an antagonist of Dopamine receptors with sedative and antiemetic effects, which is used mainly as a tranquilizer in veterinary medicine.
Targets
Dopamine receptor [6]
In vivo

Azaperone eliminates fighting only for a few hours after it is administered, after which the behaviour of pigs treated with it is not different from that of non-tranquillized mixed pigs. [1] Azaperone (2.2 mg/kg i.m.) reduces total fighting from 309.8 min for saline to 189.6 min in pigs. [2] Azaperone (103.1 mg) combined with Butorphanol (69.3 mg) produces adequate muscle relaxation and apparently adequate analgesia for minor surgical interferences, including abdominal laparoscopy, in a white rhinoceros with chronic renal disease. [3] Azaperone combined with Butorphanol and Medetomidine (BAM: 0.43 mg/kg Butorphanol, 0.36 mg/kg Azaperone, 0.14 mg/kg Medetomidine) results in a predictable onset of sedation, with a mean induction time to lateral recumbency of 9.8 min, in white-tailed deer. Azaperone combined with Butorphanol and Medetomidine (BAM: 0.43 mg/kg Butorphanol, 0.36 mg/kg Azaperone, 0.14 mg/kg Medetomidine) results in decreased heart rate and increased arterial partial pressure of carbon dioxide (PaCO2) in white-tailed deer. [4] Azaperone (1.0 mg/kg) combined with Ketamine (15 mg/kg) and Climazolam (1.5 mg/kg) results in a significantly higher castration score, when administrated intranasally (IN) compared with intramuscularly (IM) in piglets, there is an association between castration score and room temperature in the IN group. Azaperone (1.0 mg/kg) combined with Ketamine (15 mg/kg) and Climazolam (1.5 mg/kg) results in higher heart rate in the IN group of piglets. Azaperone (1.0 mg/kg) combined with Ketamine (15 mg/kg) and Climazolam (1.5 mg/kg) results in higher respiratory rate and walking significantly faster in the IM group of piglets. [5]

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 327.4
Formula

C19H22FN3O

CAS No. 1649-18-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CN(CCN1CCCC(=O)C2=CC=C(C=C2)F)C3=CC=CC=N3

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05571176 Not yet recruiting Drug: S-ketamine The Effect of S-ketamine on Pharmacokinetics of Morphine Hydromorphone and Buprenorphine Elina Brinck|Helsinki University Central Hospital January 2023 Phase 1
NCT05506462 Not yet recruiting Drug: Ketamine Hydrochloride Major Depressive Disorder Ehave Inc.|Tristar Wellness January 2023 Phase 4
NCT05451095 Withdrawn Drug: BI 474121|Drug: Placebo|Drug: Ketamine hydrochloride Healthy Boehringer Ingelheim November 7 2022 Phase 1
NCT04877977 Recruiting -- Depression|Suicide Risk National Institute of Mental Health (NIMH)|National Institutes of Health Clinical Center (CC) November 29 2022 --
NCT05086250 Recruiting Drug: Ketamine|Drug: Placebo Anxiety|Pancreatic Cancer Cedars-Sinai Medical Center October 20 2022 Early Phase 1

(data from https://clinicaltrials.gov, updated on 2022-11-29)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Azaperone | Azaperone ic50 | Azaperone price | Azaperone cost | Azaperone solubility dmso | Azaperone purchase | Azaperone manufacturer | Azaperone research buy | Azaperone order | Azaperone mouse | Azaperone chemical structure | Azaperone mw | Azaperone molecular weight | Azaperone datasheet | Azaperone supplier | Azaperone in vitro | Azaperone cell line | Azaperone concentration | Azaperone nmr