Bromocriptine mesylate

Bromocriptine mesylate 속성

Bromocriptine mesylate C화학적 특성, 용도, 생산

개요

Bromocriptine is a dopamine receptor agonist (K_is = 1,659, 12.2, 12.2, 59.7, and 1,691 nM for dopamine D₁, D₂, D₃, D₄, and D₅ receptors, respectively). It also binds to the serotonin (5-HT) receptor subtypes 5-HT_1A and 5-HT_1D (K_is = 12.9 and 10.7 nM, respectively), as well as α₁-adrenergic receptors (K_is = 1.12-4.17 nM). Bromocriptine (5 mg/kg) restores locomotor activity, without inducing dyskinesia, in a macaque model of Parkinson’s disease induced by MPTP. Formulations containing bromocriptine have been used in the treatment of Parkinson''s disease, hyperprolactinemia-associated dysfunctions, and acromegaly.

화학적 성질

Solid

용도

Dopamine receptor agonist; derivative of the ergotoxin group of ergot alkaloids. Prolactin inhibitor; antiparkinsonian.

일반 설명

Bromocriptine mesylate,(6aR,9R)-5-bromo-N-((2R,5S,10aS,10bS)-10b-hydroxy-5-isobutyl-2-isopropyl-3,6-dioxooctahydro-2H-oxazolo[3,2-a]pyrrolo[2,1c]pyrazin-2-yl)-7-methyl-4,6,6a,7,8,9-hexahydroindolo[4,3-fg]quinoline-9-carboxamide methanesulfonate(Parlodel), is a white solid soluble in ethanol and slightly solublein water (pK_a’s＝6.6 and 15). Bromocriptine is rapidlyabsorbed after oral administration and it has low systemicbioavailability because of its extensive first-pass metabolism.Bromocriptine enters the brain quickly with a half-lifefor uptake into the brain of approximately 0.3 hours; 8% ofthe drug crosses the BBB.The metabolites are excreted primarilyin the bile and feces. The high first-pass hepatic metabolismimplies an increased risk of drug interactions.Concomitant administration with the DA antagonists, metoclopramide,or domperidone may aggravate parkinsoniansymptoms and induce extrapyramidal side effects (EPS).Other drugs that may interact with bromocriptine are highlyplasma protein–bound drugs (e.g., warfarin, increased dyskinesiacaused by bromocriptine); macrolides antibacterials(enhanced dopaminergic effects); and caffeine (elevation inplasma bromocriptine concentrations). The combination oflevodopa/AADC inhibitors with bromocriptine permits a reductionof the dose of levodopa. Thus, the side effects oflevodopa are decreased, resulting in a more continuous stimulationof DA receptors.

생물학적 활성

Selective D 2 -like dopamine receptor agonist (K i values are ~ 8, ~ 5, ~ 290, ~ 440 and ~ 450 nM for D 2 , D 3 , D 4 , D 1 and D 5 receptors respectively).

Bromocriptine mesylate 준비 용품 및 원자재

원자재

준비 용품

Bromocriptine mesylate 공급 업체

공급자	전화	이메일	국가	제품 수	이점
Hebei Yanxi Chemical Co., Ltd.	+8617531190177	peter@yan-xi.com	China	5993	58
Henan Tianfu Chemical Co.,Ltd.	+86-0371-55170693 +86-19937530512	info@tianfuchem.com	China	21691	55
Shanxi Naipu Import and Export Co.,Ltd	+86-13734021967 +8613734021967	kaia@neputrading.com	China	1011	58
SHANDONG ZHI SHANG CHEMICAL CO.LTD	+86 18953170293	sales@sdzschem.com	China	2931	58
BOC Sciences	+1-631-485-4226	inquiry@bocsci.com	United States	19553	58
CONIER CHEM AND PHARMA LIMITED	+8618523575427	sales@conier.com	China	47465	58
Hubei Ipure Biology Co., Ltd	+8613367258412	ada@ipurechemical.com	China	10326	58
Career Henan Chemica Co	+86-0371-86658258 15093356674;	laboratory@coreychem.com	China	30255	58
Shanxi Xuanran Import and Export Trade Co., Ltd.	+8617735180244	mike_yan@xuanranglobal.com	CHINA	4022	58
Dideu Industries Group Limited	+86-29-89586680 +86-15129568250	1026@dideu.com	China	29271	58

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