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Azaperone, also known as Azipramide, is a chemical compound with the molecular formula C19H22FN3O. It is a white crystalline solid that is odorless and soluble in water. Azipramide is used primarily as a tranquilizer and sedative, particularly for animals such as horses and pigs. It is characterized by its low toxicity and short duration of action, making it suitable for temporary calming or restraint. Additionally, it can also be used as an organic synthesis intermediate in chemical processes. The recommended dosage for intramuscular injection varies depending on the animal's species and weight, and it is important to be cautious with the dosage to avoid potential side effects such as decreased blood pressure or temporary excitement.
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Chemical Formula |
C19H22FN3O |
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Exact Mass |
327.17 |
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Molecular Weight |
327.40 |
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m/z |
327.17 (100.0%), 328.18 (20.5%), 329.18 (2.0%), 328.17 (1.1%) |
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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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Azapirone, as a butyrylphenyl antipsychotic drug, has a core mechanism of action of dopamine D1/D2 receptor antagonism, and possesses both antihistamine and anticholinergic properties. It has shown wide application value in veterinary and special medical scenarios.
In animal husbandry, it is mainly used to control animal aggressive behavior, especially suitable for stress scenarios such as mixing, weaning, or transportation.
Pig herd management: As a systemic sedative for pigs, a dose of 2.2 mg/kg can reduce the duration of aggressive behavior from 309.8 minutes to 189.6 minutes, significantly reducing the biting frequency of mixed or weaned piglets. For aggressive sows, a single injection can encourage them to accept piglet feeding and reduce abandonment. In addition, in postpartum management of sows, a single dose injection of 320 mg can increase piglet weaning weight to 5.77 kg (control group 5.64 kg), which may be related to alleviating sow stress and promoting lactation.
Horse Sedatives: As a sedative for horses, 0.4-0.8 mg/kg intramuscular injection takes effect within 10 minutes and reaches its sedative peak within 10-70 minutes, lasting for 4 hours. It is suitable for non-invasive procedures such as transportation, hoof trimming, or basic examination.
Wildlife Baoding: When used in combination with butorphanol, it produces muscle relaxation and analgesic effects on white rhinoceros, supporting small surgical procedures such as laparoscopic examination; The "BAM regimen" consisting of 0.36 mg/kg Azapirone, 0.43 mg/kg Butorphanol, and 0.14 mg/kg Metomidine can induce controlled sedation in white tailed deer, with an average induction time of 9.8 minutes. It is suitable for wild animal capture and health check.
Often used as preoperative medication to optimize anesthesia induction conditions and reduce the dosage of general anesthetics.
Pre anesthesia administration of pigs: Intramuscular injection of 1 mg/kg can reduce the stress response of pigs to surgery. When combined with ketamine (15 mg/kg) and clonazole (1.5 mg/kg), the castration score (assessing sedation depth) of the intranasal administration group is correlated with room temperature, while the respiratory rate of the intramuscular injection group increases but walking is faster, suggesting that the administration method can be flexibly adjusted to meet different surgical needs.
Local anesthesia assistance for horses: As a preoperative medication for cesarean section or local anesthesia, a dose of 0.5 mg/kg can reduce horse struggle and lower surgical risks. Its dilating effect on peripheral blood vessels requires attention to blood pressure monitoring, but overall safety is relatively high.
Disease management: Relieve stress and improve physiological indicators
Play an auxiliary therapeutic role in specific disease scenarios.
Postpartum stress in sows: Postpartum injection can reduce the refusal and abandonment behavior of sows caused by pain or environmental changes, indirectly improving the survival rate of piglets. Research shows that the weaning weight of piglets in the treatment group increased by 2.3%, which may be related to the recovery of sow feed intake and improvement in milk quality.
Animal analgesia for chronic kidney disease: In the white rhinoceros chronic kidney disease model, the combination of azapirone (103.1 mg) and butorphanol (69.3 mg) can provide sufficient muscle relaxation, support minimally invasive surgeries such as laparoscopy, and reduce the risk of posture changes caused by pain.
Neurological disease adjuvant: Although it does not have a direct antiepileptic effect, its sedative effect can reduce the risk of self injury in epileptic animals and is often used in combination with other anticonvulsants.
Azaperone achieves efficacy superposition or side effect cancellation by being used in combination with other drugs.
Combined with opioids: When combined with butorphanol (a kappa opioid receptor agonist), it can enhance analgesic effects and reduce the risk of respiratory depression. For example, in the treatment of white rhinoceros, this combination provides stable pain relief for 4-6 hours and is suitable for chronic pain management.
Combined use with alpha 2-adrenergic agonists: When combined with metoclopramide, synergistic sedation is achieved through different mechanisms (dopamine antagonism vs. alpha 2 receptor activation), reducing the dosage of a single drug and lowering the incidence of side effects such as bradycardia.
Combination with benzodiazepines: Although azapirone does not directly act on GABA receptors, its combination with midazolam can optimize sedation depth and is suitable for preoperative preparation in high stress animals such as aggressive dogs.
The efficacy of Azapirone has been validated in unconventional treatment species.
Mink behavior management: Adding 1 mg per animal per day for one month to feed can reduce aggression and facilitate artificial feeding and breeding management. Its mechanism of action may be related to regulating dopaminergic neurotransmission and reducing anxiety related behaviors.
Zoo animal Baoding: Azapirone is often used as part of chemical Baoding protocols in primates, large felines, and other species, in combination with etomidate, fentanyl, etc., to achieve controlled sedation, support physical examinations, transportation, and other operations.
Azapirone has demonstrated irreplaceable value in animal behavior regulation, surgical assistance, disease management, and cross species therapy due to its dopamine receptor antagonistic properties. Its flexible administration method (intramuscular, intranasal), rapid onset time (10-30 minutes), and short duration (2-4 hours) make it an efficient and safe sedative choice in veterinary clinical practice.
BLOOM Tech's azaperone production stands out in the market due to its unique advantages and characteristics. Here are some key points to highlight:
Advantages
Selective Targeting: Selectively targets the 5-HT1A receptors in the brain, providing effective anti-anxiety effects without affecting other receptor systems. This ensures a more targeted and efficient treatment.
Low Addiction Potential: Unlike benzodiazepines, it does not bind to benzodiazepine receptors, thus reducing the potential for addiction and dependence. This makes it a safer long-term treatment option.
No Withdrawal Symptoms: It does not produce tolerance or withdrawal symptoms, unlike many other anti-anxiety medications. This allows patients to discontinue use gradually without experiencing unpleasant side effects.
Minimal Side Effects: Has a favorable side effect profile, with minimal cognitive and motor impairments. This means patients can maintain their daily functions and quality of life while undergoing treatment.
High Quality Production: We adhere to strict quality control standards during the production. This ensures the purity, potency, and consistency of our product, ensuring optimal therapeutic outcomes for patients.
Characteristics
Non-Benzodiazepine: It belongs to a non-benzodiazepine class of medications, which means it has a unique pharmacological profile and mechanisms of action.
Fast-Acting: It is fast-acting, providing rapid relief from anxiety symptoms. This allows patients to regain control over their emotions and functioning quickly.
Long-Lasting Effects: Has long-lasting effects, providing sustained relief from anxiety over several hours. This reduces the need for frequent dosing and improves patient compliance.
Safe for Long-Term Use: Safe for long-term use, with minimal risks of addiction, dependence, or withdrawal symptoms. This makes it a suitable treatment option for patients with chronic anxiety disorders.
Easy Administration: Available in oral formulations, making it easy to administer and convenient for patients.
In conclusion, our azaperone production offers unique advantages and characteristics that set it apart from other anti-anxiety medications. Its selective targeting, low addiction potential, no withdrawal symptoms, minimal side effects, and high-quality production ensure optimal therapeutic outcomes for patients suffering from anxiety disorders.
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