Pharmacological characterization of nipecotic acid ethyl ester: A novel cholinergic muscarinic agonist

The aim of this dissertation was to examine the hypothesis that (R)-nipecotic acid ethyl ester ((R)-NAEE) is a cholinergic agonist that is selective for a particular subclass (M$\sb1$ or M$\sb2$) of muscarinic receptors.^ Ligand binding studies indicated that like cholinergic agonists (R)-NAEE selectively interacts with rat heart (M$\sb2$) and brain (M$\sb1$) muscarinic binding sites. Physiological studies revealed that unlike cholinergic agonists (R)-NAEE stimulated only those responses coupled to M$\sb2$ muscarinic receptors (acid secretion, negative inotropic response, smooth muscle contraction). Moreover, in rat brain (R)-NAEE differentiated between M$\sb2$ receptors negatively coupled to adenylate cyclase activity and M$\sb1$ receptors mediating PI turnover, being a weak competitive antagonist at these latter sites. In isolated rat gastric mucosal cells (R)-NAEE also differentiated between two M$\sb2$ coupled responses where it potentiated acid secretion but could not stimulate PI turnover. Atropine, a selective antimuscarinic agent, competitively antagonized all agonist effects of (R)-NAEE.^ Unlike (R)-NAEE, the muscarinic agonist arecoline, which is structurally similar to (R)-NAEE, stimulates both M$\sb1$ and M$\sb2$ receptors. Structure activity studies revealed that saturation of the piperidine ring and the length of the ester side chain of (R)-NAEE are the most important determinants for both M$\sb2$ efficacy and selectivity.^ The results of this dissertation establish that (R)-NAEE is a cholinergic muscarinic receptor agonist that displays greater efficacy at M$\sb2$ than at M$\sb1$ receptors, being a weak antagonist at the M$\sb1$ site. With such selectivity, (R)-NAEE may be regarded as a prototype for a unique class of cholinergic muscarinic M$\sb2$ receptor agonists. Because of these unique properties, (R)-NAEE should be useful in the further characterization of muscarinic receptors, and could lead to the development of a new class of therapeutic agents. ^

Deoxynucleoside triphosphates bearing histamine, carboxylic acid, and hydroxyl residues--synthesis and biochemical characterization.

Modified nucleoside triphosphates (dA(Hs)TP, dU(POH)TP, and dC(Val)TP) bearing imidazole, hydroxyl, and carboxylic acid residues connected to the purine and pyrimidine bases through alkyne linkers were prepared. These modified dN*TPs were excellent substrates for various DNA polymerases in primer extension reactions. Moreover, the combined use of terminal deoxynucleotidyl transferase (TdT) and the modified dNTPs led to efficient tailing reactions that rival those of natural counterparts. Finally, the triphosphates were tolerated by polymerases under PCR conditions, and the ensuing modified oligonucleotides served as templates for the regeneration of unmodified DNA. Thus, these modified dN*TPs are fully compatible with in vitro selection methods and can be used to develop artificial peptidases based on DNA.

Tor Ester : Mittel gegen die falschen Blutbeschuldigungen

von M. Duschak

Discorso accademico del Rabbi Tranquillo Vita Corcos fatto recitare dalli giovani della sua Accdemia in occasione della festività degli Ebrei per l'historia d'Ester, e Mordacheo nell'anno 5470. dalla creazione del mondo

Im Freimann-Katalog Teil der Sammelmappe "Schriften zur Geschichte der Juden in Rom, 1697-1890"

Erreṭung der judn durch Ester und Mordechai : troier špihl und freidliches ende in 5 teihlin ...

in der reine oif richṭige ṭaiṭš šprache ... Ja'akov Ben-... Jeḥzki'el mip-Puzn

Sēfer Mēṣaḥ Ahārôn : ʿal megillôt Estēr, targûm rîšôn we-targûm šēnî ; dś iz warn gmachṭ oif megiles Ester un ali guṭ ṭaiṭš gšṭelṭ

[Aharon Ben-Mordechai aus Rödelheim]

Ester oder di belohnṭe ṭugend : eine pozze in fier abšniṭṭen nebzṭ einigen noch nichṭ gedrukṭen gedichṭen in jidiš-daiṭšer mundarṭ

fon Josef Hertz

Sēfer Mēṣaḥ Ahārôn : ʿal megillôt Estēr, targûm rîšôn we-targûm šēnî ; dś iz war gimachṭ oif megiles Ester ... alz guṭ ṭaiṭš gšṭelt ...

[Aharon Ben-Mordechai aus Rödelheim]

Ester oder di belohnṭe ṭugend : in 4 abšniṭṭen in jidiš-ṭaiṭšer mundorṭ

fon Josef Herz

Ester oder di belohnṭe ṭugend : eine posse in fier abšniṭṭen jidiš daiṭšer mundarṭ als beilage tzum mišloaḥ-manos an purim

fon Josef Hertz

Aḥashṿerosh shpil : gshprekh fun Haman un Mordechai un al geṭigi fragn un anṭṿorṭn fun di malkah Vashti un Ester un ali datsu geherigi bedinṭn ...

Digitalisat der Ausgabe Lemberg, 1848