Akuammidine | CAS:639-36-1 | Manufacturer ChemFaces

Akuammidine

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Description:

Akuammidine shows anti-inflammatory and anti-asthmatic properties, it has opioid analgesic activity, it shows a preference for mu-opioid binding sites with Ki values of 0.6, 2.4 and 8.6 microM at mu-, delta- and kappa-opioid binding sites, respectively.

Targets:

Opioid Receptor

In vitro:

J Chromatogr B Analyt Technol Biomed Life Sci. 2012 Nov 1;908:98-104.

Microfractionation bioactivity-based ultra performance liquid chromatography/quadrupole time-of-flight mass spectrometry for the identification of nuclear factor-κB inhibitors and β2 adrenergic receptor agonists in an alkaloidal extract of the folk herb[Pubmed: 23122407 ]

This method was coupled with two dual-luciferase reporter assay systems to show nuclear factor-κB (NF-κB) inhibition and β(2) adrenergic receptor (β(2)AR) activation.
METHODS AND RESULTS:
Using UPLC-Q/TOF, 18 potential candidates were identified according to unique mass spectrometric fragmentation. After in vitro biological evaluation, several indole alkaloids with anti-inflammatory and anti-asthmatic properties were found, including Akuammidine, (E)-alstoscholarine, and (Z)-alstoscholarine. Compared with conventional fingerprints, the microfractionation based bioactivity-integrated fingerprints that contain both chemical and bioactivity details offer a more comprehensive understanding of the chemical makeup of plant materials.
CONCLUSIONS:
This strategy clearly demonstrated that dual bioactivity-integrated fingerprinting is a powerful tool for the improved screening and identification of potential dual-target lead compounds in complex herbal medicines.

Akuammidine Description

Source:	The herbs of Rauwolfia vomitoria
Solvent:	Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc.
Storage:	Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months(2-8C). Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable for up to two weeks. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please email to: service@chemfaces.com
After receiving:	The packaging of the product may have turned upside down during transportation, resulting in the natural compounds adhering to the neck or cap of the vial. take the vial out of its packaging and gently shake to let the compounds fall to the bottom of the vial. for liquid products, centrifuge at 200-500 RPM to gather the liquid at the bottom of the vial. try to avoid loss or contamination during handling.

Kinase Assay:

Eur J Pharmacol. 1998 May 29;350(1):101-8.

Opioid activity of alkaloids extracted from Picralima nitida (fam. Apocynaceae).[Pubmed: 9683021]

Extracts of the seeds of Picralima nitida (fam. Apocynaceae) have been reported to have opioid analgesic activity.
METHODS AND RESULTS:
In this investigation, isolated tissue bioassays and radioligand binding assays have been used to determine the opioid activity of five alkaloids--Akuammidine, akuammine, akuammicine, akuammigine and pseudoakuammigine--extracted from the seeds of P. nitida. Akuammidine showed a preference for mu-opioid binding sites with Ki values of 0.6, 2.4 and 8.6 microM at mu-, delta- and kappa-opioid binding sites, respectively. The agonist actions of Akuammidine in the mouse-isolated vas deferens were antagonised by naloxone and the mu-opioid receptor selective antagonist D-Phe-Cys-Tyr-D-Trp-Orn-Thr-Pen-Thr-NH2 (CTOP) confirming an action at mu-opioid receptors. In contrast, akuammine also showed highest affinity for mu-opioid binding sites (Ki 0.5 microM) but was an antagonist at mu-opioid receptors with a pK(B) of 5.7 against the selective mu-opioid receptor agonist [D-Ala2,MePhe4,Gly-ol5]enkephalin (DAMGO).
CONCLUSIONS:
Akuammicine has the highest affinity for kappa-opioid binding sites (Ki 0.2 microM) and was a full agonist at kappa-opioid receptors in the guinea pig ileum preparation but a partial kappa-opioid receptor agonist in the vasa deferentia of the mouse and the rabbit.

Product Name	Akuammidine
Price:
CAS No.:	639-36-1
Catalog No.:	CFN96242
Molecular Formula:	C₂₁H₂₄N₂O₃
Molecular Weight:	352.4 g/mol
Purity:	>=98%
Type of Compound:	Alkaloids
Physical Desc.:	Powder
Source:	The herbs of Rauwolfia vomitoria
Solvent:	Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc.
Download:	COA MSDS SDF
Similar structural:	Comparison (Web) (SDF)
Guestbook:

Size /Price /Stock	10 mM * 100 uL in DMSO / Inquiry / In-stock 10 mM * 1 mL in DMSO / Inquiry / In-stock
Related Libraries	Anti-inflammatory Compound Library Analgesia Compound Library Antiasthmatic Compound Library Alkaloids Compound Library Opioid Receptor Inhibitor Library

	1 mg	5 mg	10 mg	20 mg	25 mg
1 mM	2.8377 mL	14.1884 mL	28.3768 mL	56.7537 mL	70.9421 mL
5 mM	0.5675 mL	2.8377 mL	5.6754 mL	11.3507 mL	14.1884 mL
10 mM	0.2838 mL	1.4188 mL	2.8377 mL	5.6754 mL	7.0942 mL
50 mM	0.0568 mL	0.2838 mL	0.5675 mL	1.1351 mL	1.4188 mL
100 mM	0.0284 mL	0.1419 mL	0.2838 mL	0.5675 mL	0.7094 mL

CFN96747	Rauvotetraphylline A	1422506-49-7	342.43	C₂₀H₂₆N₂O₃
CFN96696	Rauvoyunine A	1414883-81-0	356.46	C₂₁H₂₈N₂O₃
CFN96067	Pericyclivine	975-77-9	322.4	C₂₀H₂₂N₂O₂
CFN90441	Perivine	2673-40-7	338.4	C₂₀H₂₂N₂O₃
CFN96242	Akuammidine	639-36-1	352.4	C₂₁H₂₄N₂O₃
CFN89174	Conodurine	2665-57-8	704.91	C₄₃H₅₂N₄O₅
CFN96750	Rauvotetraphylline C	1422506-51-1	510.58	C₂₈H₃₄N₂O₇
CFN96751	Rauvotetraphylline B	1422506-50-0	547.65	C₃₁H₃₇N₃O₆
CFN97884	Vellosimine	6874-98-2	292.4	C₁₉H₂₀N₂O
CFN92612	(+)-Affinisine	2912-11-0	308.4	C₂₀H₂₄N₂O