아목사핀

아목사핀
아목사핀 구조식 이미지
카스 번호:
14028-44-5
한글명:
아목사핀
동의어(한글):
아목사핀;아목사핀(AMOXAPINE)
상품명:
Amoxapine
동의어(영문):
amoxan;Defanyl;Moxadil;Asendin;Asendis;cl67772;Demolox;Ascendin;CL 67772;AMOXAPINE
CBNumber:
CB5375947
분자식:
C17H16ClN3O
포뮬러 무게:
313.78
MOL 파일:
14028-44-5.mol
MSDS 파일:
SDS

아목사핀 속성

녹는점
175-1760C
끓는 점
469.9±55.0 °C(Predicted)
밀도
1.2613 (rough estimate)
굴절률
1.5800 (estimate)
인화점
9℃
저장 조건
Keep in dark place,Inert atmosphere,Room temperature
용해도
메탄올 에 용해됨
물리적 상태
고체
물리적 상태
단단한 모양
산도 계수 (pKa)
pKa 7.6 (Uncertain)
색상
벤젠/애완동물 에테르에서 침전된 결정
Merck
14,576
안정성
Stable under recommended storage conditions., Stable Under Recommended Storage C
CAS 데이터베이스
14028-44-5(CAS DataBase Reference)
NIST
Amoxapine(14028-44-5)
안전
  • 위험 및 안전 성명
  • 위험 및 사전주의 사항 (GHS)
위험품 표기 Xn
위험 카페고리 넘버 22
안전지침서 36
유엔번호(UN No.) 3249
WGK 독일 3
RTECS 번호 HQ4025500
위험 등급 6.1(b)
포장분류 III
HS 번호 2934990002
독성 LD50 in mice (mg/kg): 122 i.p.; 112 orally (Howell, 1972)
그림문자(GHS): GHS hazard pictograms
신호 어: Warning
유해·위험 문구:
암호 유해·위험 문구 위험 등급 범주 신호 어 그림 문자 P- 코드
H302 삼키면 유해함 급성 독성 물질 - 경구 구분 4 경고 GHS hazard pictograms P264, P270, P301+P312, P330, P501
예방조치문구:
P264 취급 후에는 손을 철저히 씻으시오.
P264 취급 후에는 손을 철저히 씻으시오.
P270 이 제품을 사용할 때에는 먹거나, 마시거나 흡연하지 마시오.
P301+P312 삼켜서 불편함을 느끼면 의료기관(의사)의 진찰을 받으시오.
P501 ...에 내용물 / 용기를 폐기 하시오.

아목사핀 MSDS


Amoxapine

아목사핀 C화학적 특성, 용도, 생산

개요

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.

화학적 성질

Crystalline Solid

용도

Amoxapine is intended more for relieving symptoms in patients with neurotic or situational depression. It has a number of serious side effects.

정의

ChEBI: A dibenzooxazepine compound having a chloro substituent at the 2-position and a piperazin-1-yl group at the 11-position.

일반 설명

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

신진 대사

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."

아목사핀 준비 용품 및 원자재

원자재

준비 용품


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