Hydroxyzine-d8 is intended for use as an internal standard for the quantification of hydroxyzine (Item No. 24039) by GC- or LC-MS. Hydroxyzine is a histamine H1 receptor antagonist (Ki = 1.9 nM).{39568} It binds competitively with the H1 receptor inverse agonist mepyramine (Item No. 20978) with an IC50 value of 80 µM in polymorphonuclear leukocytes.{39569} In vivo, it is metabolized to the H1 receptor antagonist cetirizine (Item No. 19686).{40229} In situ, hydroxyzine (10 µM) prevents recruitment of rolling leukocytes induced by histamine in rat mesentery post-capillary venules.{39570} Hydroxyzine also decreases anxiety-like behavior in mice, increasing the time spent in the open arms of the elevated plus maze and in the light side of the light-dark exploration test.{39571} Formulations containing hydroxyzine have been used in the treatment of anxiety and as antihistamines in the treatment of allergic rhinitis.
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An internal standard for the quantification of hydroxyzine by GC- or LC-MS
Formal name: 2-[2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl-d8]ethoxy]-ethanol, dihydrochloride
Synonyms:
Molecular weight: 455.9
CAS: 1808202-93-8
Purity: ≥99% deuterated forms (d1-d8)
Formulation: A solid
The tetracycline repressor (TetR) is a transcriptional regulator which normally binds tightly to its palindromic tetO operator DNA, blocking gene expression.{17508} Tet causes the repressor to dissociate from the DNA, allowing transcription to occur. A novel reverse TetR (revTetR) requires tetracycline as a co-repressor to bind tetO and block transcription.{17509,17510} Anhydrotetracycline (hydrochloride) is a powerful effector in both the tetracycline repressor (TetR) and reverse TetR (revTetR) systems, binding the Tet repressor 35-fold more strongly than Tet.{17508,17511} Moreover, anhydrotetracycline poorly binds the 30S ribosomal subunit, compared to Tet,{17512} so it does not act as a general inhibitor of translation and is a poor antibiotic. Perhaps related to this, the concentration of anhydrotetracycline that inhibits eukaryotic cell growth is more than a 1,000-fold above the dose that alters transcription through TetR.{17508}
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The nuclear factor-κB (NF-κB) regulates the expression of numerous genes involved in immunity and inflammation, cellular stress responses, growth, and apoptosis. Resveratrol, a polyphenolic trans-stilbene, is a known inhibitor of the activation of NF-κB and exhibits activity against a wide variety of cancer cells. CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}
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1,2-Dipalmitoyl-sn-glycero-3-PC (DPPC) is a zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers, bilayers, and liposomes for use in a variety of applications.{14480,24261,14478,14479} It has been used in the formation of proteoliposomes for implantation of γ-glutamyl transpeptidase into human erythrocyte membranes.{14478} Incorporation of glycosphingolipid antigens into DPPC-containing liposomes increases the immunogenicity of the antigens in mice.{14479}
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1,2-Dipalmitoyl-sn-glycero-3-PC (DPPC) is a zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers, bilayers, and liposomes for use in a variety of applications.{14480,24261,14478,14479} It has been used in the formation of proteoliposomes for implantation of γ-glutamyl transpeptidase into human erythrocyte membranes.{14478} Incorporation of glycosphingolipid antigens into DPPC-containing liposomes increases the immunogenicity of the antigens in mice.{14479}
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