Amoxapine
- CAS No.
- 14028-44-5
- Chemical Name:
- Amoxapine
- Synonyms
- amoxan;Defanyl;Moxadil;Asendin;Asendis;cl67772;Demolox;Ascendin;CL 67772;AMOXAPINE
- CBNumber:
- CB5375947
- Molecular Formula:
- C17H16ClN3O
- Molecular Weight:
- 313.78
- MOL File:
- 14028-44-5.mol
- Modify Date:
- 2023/9/20 16:43:00
Melting point | 175-1760C |
---|---|
Boiling point | 469.9±55.0 °C(Predicted) |
Density | 1.2613 (rough estimate) |
refractive index | 1.5800 (estimate) |
Flash point | 9℃ |
storage temp. | Keep in dark place,Inert atmosphere,Room temperature |
solubility | methanol: soluble |
form | Solid |
pka | pKa 7.6 (Uncertain) |
color | Crystals from benzene/pet ether |
Merck | 14,576 |
Stability | Stable under recommended storage conditions., Stable Under Recommended Storage C |
CAS DataBase Reference | 14028-44-5(CAS DataBase Reference) |
NIST Chemistry Reference | Amoxapine(14028-44-5) |
SAFETY
Risk and Safety Statements
Symbol(GHS) | GHS07 |
---|---|
Signal word | Warning |
Hazard statements | H302 |
Precautionary statements | P264-P270-P301+P312-P501 |
Hazard Codes | Xn |
Risk Statements | 22 |
Safety Statements | 36 |
RIDADR | 3249 |
WGK Germany | 3 |
RTECS | HQ4025500 |
HazardClass | 6.1(b) |
PackingGroup | III |
HS Code | 2934990002 |
Toxicity | LD50 in mice (mg/kg): 122 i.p.; 112 orally (Howell, 1972) |
Amoxapine price More Price(5)
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
Sigma-Aldrich(India) | A129 | Amoxapine | 14028-44-5 | 100MG | ₹4708.88 | 2022-06-14 | Buy |
Sigma-Aldrich(India) | A129 | Amoxapine | 14028-44-5 | 500MG | ₹14635.4 | 2022-06-14 | Buy |
Sigma-Aldrich(India) | PHR1841 | Amoxapine Pharmaceutical Secondary Standard; Certified Reference Material | 14028-44-5 | 500MG | ₹23739.23 | 2022-06-14 | Buy |
Sigma-Aldrich(India) | A129 | Amoxapine | 14028-44-5 | 5G | ₹87801.58 | 2022-06-14 | Buy |
TCI Chemicals (India) | A2499 | Amoxapine min. 97.0 % | 14028-44-5 | 1G | ₹6200 | 2022-05-26 | Buy |
Amoxapine Chemical Properties,Uses,Production
Description
Amoxapine is a tetracyclic antidepressant with a wide range of pharmacological effects. It inhibits norepinephrine and serotonin reuptake, binding the respective transporters with Kd values of 16 and 58 nM. It has also been shown to act as either an antagonist or inverse agonist at serotonin 5-HT2A, 2B, 2C, 3, 6, 7 (Kis = 1 and 2 nM for 5-HT2A and 5-HT2C, respectively), dopamine D2, 3, 4 (Kd = 160 nM for D2), α1-adrenergic (Kd = 50 nM), and histamine H1 (Kd = 25 nM) receptors.
Chemical Properties
Crystalline Solid
Uses
Amoxapine is intended more for relieving symptoms in patients with neurotic or situational depression. It has a number of serious side effects.
Definition
ChEBI: A dibenzooxazepine compound having a chloro substituent at the 2-position and a piperazin-1-yl group at the 11-position.
General Description
Consideration of the structure of amoxapine, 2-chloro-11-(1-piperazinyl)dibenz-[b,f] [1,4]oxazepine (Asendin), reinforcesthe fact that many antidepressants are very closelyrelated to antipsychotics. Indeed, some, including amoxapine,have significant effects at D2 receptors. The Nmethyl–substituted relative of amoxapine is the antipsychoticloxapine (Loxitane). The 8-hydroxy metabolite ofamoxapine is reportedly active as an antidepressant and asa D2 receptor blocker.
Mechanism of action
Additionally, it is the N-desmethyl metabolite of the antipsychotic loxapine. Amoxapine differs structurally from the other secondary TCAs in that it has both a nitrogen and an oxygen atom in its 7-membered central ring and a piperazinyl ring rather than a propylamino side chain attached to the central ring.Amoxapine is a less potent inhibitor of neuronal NE reuptake compared with the other secondary TCAs, with a mechanism of action similar to that of desipramine.
Pharmacology
The antidepressant action of amoxapine is comparable to that of imipramine and amitriptyline. It exhibits antagonistic activity on dopamine (D2) receptors.
Pharmacokinetics
Amoxapine shares the toxic potentials of the TCAs, and the usual precautions of TCA administration should be observed. Amoxapine resembles the atypical antipsychotic drugs in its intermediate affinity as an antagonist of dopamine-2 and of 5-HT2 receptors. Amoxapine is rapidly and almost completely absorbed from the gastrointestinal (GI) tract. Amoxapine and its 8-hydroxyamoxapine metabolite have been detected in human milk at concentrations below steady-state therapeutic concentrations.
Clinical Use
Amoxapine is a dibenzoxazepine TCA with antidepressant and antipsychotic effects that has shown therapeutic effectiveness in patients with delusional depression.
Safety Profile
Poison by ingestion andintraperitoneal routes. Human systemic effects byingestion: acute renal failure, acute tubular necrosis, BPlowering, coma, convulsions, decreased body temperature,EKG changes, excitement, fasciculations, heart ratechanges, hype
Metabolism
Amoxapine has the shortest elimination time (~8 hours) of the secondary TCAs. It is metabolized in the liver principally to 8-hydroxyamoxapine and to 7-hydroxyamoxapine. Both of these metabolites are pharmacologically active and have half-lives of 30 and 6.5 hours, respectively. The hydroxylation of amoxapine is inhibited by ketoconazole, suggesting the involvement of CYP3A4."
Amoxapine Preparation Products And Raw materials
Raw materials
Preparation Products
Supplier | Tel | Country | ProdList | Advantage | Inquiry |
---|---|---|---|---|---|
Mehta Pharmaceutical Industries | +91-8390068777 +91-8390068777 | Mumbai, India | 30 | 58 | Inquiry |
Global Pharma | +91-9819994077 +91-9819994077 | Maharashtra, India | 34 | 58 | Inquiry |
Anlon Healthcare Pvt Ltd | +91-2812562538 +91-7069690081 | Gujarat, India | 54 | 58 | Inquiry |
AKASH PHARMA EXPORTS | +91-9388123451 +91-9846039283 | Kerela, India | 470 | 58 | Inquiry |
A.J Chemicals | 91-9810153283 | New Delhi, India | 6124 | 58 | Inquiry |
CLEARSYNTH LABS LTD. | +91-22-45045900 | Hyderabad, India | 6351 | 58 | Inquiry |
TCI Chemicals (India) Pvt. Ltd. | 1800 425 7889 | New Delhi, India | 6778 | 58 | Inquiry |
Pharmaffiliates Analytics and Synthetics P. Ltd | +91-172-5066494 | Haryana, India | 6773 | 58 | Inquiry |
Di Bombay Pharma | 08047627138 | Nagpur, India | 8 | 58 | Inquiry |
SynZeal Research Pvt Ltd | +1 226-802-2078 | Gujarat, India | 6522 | 58 | Inquiry |
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