Azatadine - CAS 3964-81-6
Catalog number: 3964-81-6
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C20H22N2
Molecular Weight:
290.40
COA:
Inquire
Targets:
Histamine Receptor
Description:
Azatadine is a new antihistamine acts as histamine for histamine H1- receptor inhibitor ( IC50 = 6.5 nM and 10 nM, respectively).
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Purity:
≥98%
Appearance:
Solid powder
Synonyms:
6,11-Dihydro-11-(1-methyl-4-piperidylidene)-5H-benzo[5,6]cyclohepta-[1,2-b]pyridine; 2-(1-methylpiperidin-4-ylidene)-4-azatricyclo[9.4.0.0³,⁸]pentadeca-1(15),3(8),4,6,11,13-hexaene;
Solubility:
Soluble in DMSO
Storage:
Store at -20 °C
MSDS:
Inquire
Application:
Antihistaminic.
Quality Standard:
Enterprise Standard
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly
Quantity:
Milligrams-Grams
Melting Point:
124-126 °C
Density:
1.127
InChIKey:
SEBMTIQKRHYNIT-UHFFFAOYSA-N
InChI:
1S/C20H22N2/c1-22-13-10-16(11-14-22)19-18-7-3-2-5-15(18)8-9-17-6-4-12-21-20(17)19/h2-7,12H,8-11,13-14H2,1H3
Canonical SMILES:
CN1CCC(CC1)=C1C2=CC=CC=C2CCC2=C1N=CC=C2
Current Developer:
Schering-Plough
1.Syntheses of molecularly imprinted polymers: Molecular recognition of cyproheptadine using original print molecules and azatadine as dummy templates.
Feás X1, Seijas JA, Vázquez-Tato MP, Regal P, Cepeda A, Fente C. Anal Chim Acta. 2009 Jan 12;631(2):237-44. doi: 10.1016/j.aca.2008.10.054. Epub 2008 Oct 31.
The use of custom-made polymeric materials with high selectivities as target molecules in solid-phase extraction (SPE), known as molecularly imprinted solid-phase extraction (MISPE), is becoming an increasingly important sample preparation technique. However, the potential risk of leakage of the imprinting molecules during the desorption phase has limited application. The use of a mimicking template, called a dummy molecular imprinting polymer (DMIP), that bears the structure of a related molecule and acts as a putative imprinting molecule may provide a useful solution to this problem. In the current study, cyproheptadine (CPH) and azatadine (AZA) were used as templates in the development of an MIP and DMIP for acrylic acid and methacrylic acid monomers. Our results indicate that DMIPs have equal recognition of CPH, avoiding the problem of leakage of original template during the desorption phase relative to MIPs synthesized in presence of the print molecule CPH.
2.Antiallergic effects of H1-receptor antagonists.
Baroody FM1, Naclerio RM. Allergy. 2000;55 Suppl 64:17-27.
The primary mechanism of antihistamine action in the treatment of allergic diseases is believed to be competitive antagonism of histamine binding to cellular receptors (specifically, the H1-receptors), which are present on nerve endings, smooth muscles, and glandular cells. This notion is supported by the fact that structurally unrelated drugs antagonize the H1-receptor and provide clinical benefit. However, H1-receptor antagonism may not be their sole mechanism of action in treating allergic rhinitis. On the basis of in vitro and animal experiments, drugs classified as H1-receptor antagonists have long been recognized to have additional pharmacological properties. Most first-generation H1-antihistamines have anticholinergic, sedative, local anaesthetic, and anti-5-HT effects, which might favourably affect the symptoms of the allergic response but also contribute to side-effects. These additional properties are not uniformly distributed among drugs classified as H1-receptor antagonists.
3.Application of dummy molecularly imprinted solid-phase extraction in the analysis of cyproheptadine in bovine urine.
Feás X1, Ye L, Regal P, Fente CA, Hosseini SV, Cepeda A. J Sep Sci. 2009 May;32(10):1740-7. doi: 10.1002/jssc.200800726.
Due to the difficulty of monitoring trace levels of cyproheptadine (CYP) residues in complicated biological matrices, specific adsorption materials for the preconcentration and clean-up of CYP are indispensable. In this work, CYP was extracted from urine using dummy molecularly imprinted SPE (DMISPE) to avoid leakage of the imprinting molecules during the desorption phase. For synthesis of DMISPE, azatadine (AZA) was employed as the dummy template, methacrylic acid (MAA) as the monomer, ethylene glycol dimethacrylate (EGDMA) as the cross-linker, 2,2'-azobis(2-methylpropionitrile) (AIBN) as the initiator, and dichloromethane as the porogen solvent. An LC-MS/MS method was used to analyze CYP. Two MRM (multiple reaction monitoring) transitions for each analyte were monitored using diphenylpyraline hydrochloride (DPP.HCl), which was used as an internal standard. The advantages of DMISPE include obtaining less complex chromatograms and reducing ion suppression in ESI.
4.Interaction between chloroquine and diverse pharmacological agents in chloroquine resistant Plasmodium yoelii nigeriensis.
Singh N1, Puri SK. Acta Trop. 2000 Nov 2;77(2):185-93.
The effect of a number of pharmacological agents on the enhancement of antimalarial activity of chloroquine was evaluated against chloroquine resistant line of Plasmodium yoelii nigeriensis (N-67). The response after combination therapy was monitored on the basis of alteration in the course of parasitaemia, the extension of mean survival time and the percent cure rate in different groups. The study was designed to compare the in vivo efficacy of a number of resistance modulating agents found effective in several in vitro studies against chloroquine resistant P. falciparum isolates. Based on their efficacy in this rodent model, the response of combination of chloroquine with agents representing diverse chemical moieties has been categorised as curative, moderately active and inactive. Out of the 22 agents evaluated, only cyproheptadine-chloroquine combination produced curative response. Ketotifen, azatadine, pheniramine, amitriptyline, fluoxetine, verapamil, penfluridol and trifluoperazine demonstrated moderate activity while loratadine, terfenadine, promethazine, ranitidine, nifedipine, diltiazem, chlorpromazine, amiodarone, tamoxifen, dipyridamol, propranolol, acyclovir and amantidine were inactive.
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CAS 3964-81-6 Azatadine

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