β-育亨宾

beta-Yohimbine

	产品编号	CFN98921
	CAS编号	549-84-8
	分子式 = 分子量	C₂₁H₂₆N₂O₃ = 354.5
	产品纯度	>=98%
	物理属性	Powder
	化合物类型	Alkaloids
	植物来源	The peels of Corynante yohimbe
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产品名称	产品编号	CAS编号	包装	QQ客服
β-育亨宾	CFN98921	549-84-8	1mg	QQ客服：1413575084
β-育亨宾	CFN98921	549-84-8	5mg	QQ客服：1413575084
β-育亨宾	CFN98921	549-84-8	10mg	QQ客服：1413575084
β-育亨宾	CFN98921	549-84-8	20mg	QQ客服：1413575084

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Description:

Beta-Yohimbine has approximately twice as toxic as yohimbine and corynanthine about one fifth as toxic. Beta-yohimbine has alpha-1 and alpha-2 adrenoceptor blocking activities, it has cardiovascular effects. Beta-Yohimbine has anti-plasmodial and anti-malarial activity.

Targets:

Adrenergic Receptor | Antifection

In vitro:

Molecules. 2013 May 29;18(6):6281-97.

Chemical composition of Aspidosperma ulei Markgr. and antiplasmodial activity of selected indole alkaloids.[Pubmed: 23760029]

METHODS AND RESULTS:
A new indole alkaloid, 12-hydroxy-N-acetyl-21(N)-dehydroplumeran-18-oic acid (13), and 11 known indole alkaloids: 3,4,5,6-tetradehydro-β-yohimbine (3), 19(E)-hunteracine (4), beta-Yohimbine(5), yohimbine (6), 19,20-dehydro-17-α-yohimbine (7), uleine (10), 20-epi-dasycarpidone (11), olivacine (8), 20-epi-N-nor-dasycarpidone (14), N-demethyluleine (15) and 20(E)-nor-subincanadine E (12) and a boonein δ-lactone 9, ursolic acid (1) and 1D,1O-methyl-chiro-inositol (2) were isolated from the EtOH extracts of different parts of Aspidosperma ulei Markgr. (Apocynaceae). Identification and structural elucidation were based on IR, MS, ¹H- and ¹³C-NMR spectral data and comparison to literature data. The antiplasmodial and antimalarial activity of 1, 5, 6, 8, 10 and 15 has been previously evaluated and 1 and 10 have important in vitro and in vivo antimalarial properties according to patent and/or scientific literature. With the aim of discovering new antiplasmodial indole alkaloids, 3, 4, 11, 12 and 13 were evaluated for in vitro inhibition against the multi-drug resistant K1 strain of the human malaria parasite Plasmodium falciparum. IC₅₀ values of 14.0 (39.9), 4.5 (16.7) and 14.5 (54.3) mg/mL (mM) were determined for 3, 11 and 12, respectively. Inhibitory activity of 3, 4, 11, 12 and 13 was evaluated against NIH3T3 murine fibroblasts.
CONCLUSIONS:
None of these compounds exhibited toxicity to fibroblasts (IC₅₀ > 50 mg/mL). Of the five compounds screened for in vitro antiplasmodial activity, only 11 was active.

In vivo:

Psychopharmacology (Berl). 1977 Jan 31;51(2):209-12.

Interaction between yohimbine alkaloids and amphetamine in mice.[Pubmed: 402675]

METHODS AND RESULTS:
The toxicity (LD50) of the isomers yohimbine, beta-Yohimbine, and corynanthine was determined in mice. The LD50 of amphetamine in the presence of a constant dose of a yohimbine isomer and that of the isomer in the presence of a constant dose of amphetamine were determined in aggregated mice. Isobolograms were constructed from these data and used to evaluate the interaction of the yohimbine alkaloids and amphetamine. beta-Yohimbine was found to be approximately twice as toxic as yohimbine and corynanthine about one fifth as toxic. There was a mutual potentiation between the toxicities of yohimbine and amphetamine. Potentiation of the toxicity of amphetamine occurred with beta-Yohimbine but the effect was not as marked as with yohimbine. In contrast, corynanthine antagonized the toxicity of amphetamine.
CONCLUSIONS:
The interaction between yohimbine and amphetamine is unlikely to be due to noradrenergic mechanisms but could conceivably involve serotonergic or dopaminergic mechanisms.

Chem Pharm Bull (Tokyo). 1990 Jun;38(6):1702-6.

Structure-activity relationship of yohimbine and its related analogs in blocking alpha-1 and alpha-2 adrenoceptors: a comparative study of cardiovascular activities.[Pubmed: 1976443]

We investigated the selectivities and structure requirements for alpha-1 and alpha-2 adrenoceptor blocking activities of yohimbine (YO) and its 12 related analogs, such as beta-Yohimbine (beta-YO), dihydrocorynantheine (DHC) and (-)indoloquinolizidine ((-)IQ).
METHODS AND RESULTS:
The affinity of YO analogs to alpha-adrenoceptor was assessed by measuring their blockade of pressor responses to epinephrine in pithed rats. Among YO structure groups, the potency order was YO greater than DHC = beta-YO greater than geissoschizine methylether greater than 14 beta-hydroxy YO greater than 14 beta-benzoyloxy YO (inactive). (-)IQ was slightly less potent than YO, but much stronger than (+)IQ. Among (+/-)IQ structure groups, the potency order was (+/-)IQ greater than (+/-)1,12b-trans-1-hydroxy IQ much greater than (+/-)1,12b-cis-1-hydroxy IQ (inactive). (+/-)Borrerine was active, but (+/-)desmethylborrerine was inactive. The alpha-1 blocking activities of the four compounds YO, beta-YO, DHC and (-)IQ, were assessed in experiments of pressor responses to methoxamine in pithed rats and contractile responses to methoxamine in the rat vas deferens. The potency order was (-)IQ greater than YO greater than DHC greater than beta-YO. Furthermore, the alpha-2 blocking activities of the four analogs were assessed in experiments of pressor responses to clonidine and inhibition of electrically driven cardioacceleration by clonidine, in pithed rats. The potency order was YO greater than beta-YO greater than (-)IQ greater than DHC.
CONCLUSIONS:
Based on the potency ratio between alpha-1 and alpha-2 blocking activities, DHC or YO was most selective for alpha-1 or alpha-2 subtype, respectively, among the four YO analogs.

产品名称	产品编号	CAS编号	分子式 = 分子量	位单	联系QQ
别育享宾; Allo-Yohimbine	CFN92577	522-94-1	C₂₁H₂₆N₂O₃ = 354.5	5mg	QQ客服：1457312923
利血平酸甲酯; Methyl reserpate	CFN92579	2901-66-8	C₂₃H₃₀N₂O₅ = 414.5	5mg	QQ客服：1413575084
利血那明; Reserpinine	CFN92580	24815-24-5	C₃₅H₄₂N₂O₉ = 634.7	5mg	QQ客服：2159513211
利血平氮氧化物; Reserpin N-oxide	CFN92583	474-48-6	C₃₃H₄₀N₂O₁₀ = 624.7	5mg	QQ客服：1457312923
18-β-羟基-3-表-α-育亨宾; 18-Beta-hydroxy-3-epi-alpha-yohimbine	CFN92610	81703-06-2	C₂₁H₂₆N₂O₄ = 370.5	5mg	QQ客服：2056216494
利血平; Reserpine	CFN98112	50-55-5	C₃₃H₄₀N₂O₉ = 608.69	20mg	QQ客服：3257982914
羧酯利血平; Syrosingopine	CFN98542	84-36-6	C₃₅H₄₂N₂O₁₁ = 666.71	5mg	QQ客服：2159513211
异柯楠碱; Isorauhimbine	CFN98762	483-09-0	C₂₁H₂₆N₂O₃ = 354.5	5mg	QQ客服：3257982914
β-育亨宾; beta-Yohimbine	CFN98921	549-84-8	C₂₁H₂₆N₂O₃ = 354.5	5mg	QQ客服：2056216494
α-育亨宾; alpha-Yohimbine	CFN99400	131-03-3	C₂₁H₂₆N₂O₃ = 354.5	5mg	QQ客服：215959384

	1 mg	5 mg	10 mg	20 mg	25 mg
1 mM	2.8209 mL	14.1044 mL	28.2087 mL	56.4175 mL	70.5219 mL
5 mM	0.5642 mL	2.8209 mL	5.6417 mL	11.2835 mL	14.1044 mL
10 mM	0.2821 mL	1.4104 mL	2.8209 mL	5.6417 mL	7.0522 mL
50 mM	0.0564 mL	0.2821 mL	0.5642 mL	1.1283 mL	1.4104 mL
100 mM	0.0282 mL	0.141 mL	0.2821 mL	0.5642 mL	0.7052 mL

β-育亨宾

beta-Yohimbine

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