Carbazole scaffold in medicinal chemistry and natural products: a review from 2010-2015
LS Tsutsumi, D Gündisch, D Sun - Current Topics in Medicinal …, 2016 - ingentaconnect.com
… However, lower MIC values were observed with dibenzo[b,d]furan and dibenzo[b,d]thiophene
triazole conjugates in the series (MICs = 0.78 to 25 µg/mL) in comparison to those …
triazole conjugates in the series (MICs = 0.78 to 25 µg/mL) in comparison to those …
Nicotine decreases food intake through activation of POMC neurons
… Food intake was not significantly affected by nicotine or cytisine in POMC KO mice at two
different doses (D). Furthermore, knockdown of Mc4r by AAV-shRNAs in the PVN [detected by …
different doses (D). Furthermore, knockdown of Mc4r by AAV-shRNAs in the PVN [detected by …
Bispidine as a privileged scaffold
I Tomassoli, D Gündisch - Current topics in medicinal chemistry, 2016 - ingentaconnect.com
… D. A flattened (c,c) conformation will increase the dipole moment to 1.90 D, whereas the dipole
moment is 1.84 D … However, the experimental value obtained was 2.02 D, which excluded …
moment is 1.84 D … However, the experimental value obtained was 2.02 D, which excluded …
5-Iodo-A-85380, an α4β2 subtype-selective ligand for nicotinic acetylcholine receptors
AG Mukhin, D Gündisch, AG Horti, AO Koren… - Molecular …, 2000 - ASPET
In an effort to develop selective radioligands for in vivo imaging of neuronal nicotinic
acetylcholine receptors (nAChRs), we synthesized 5-iodo-3-(2(S)-azetidinylmethoxy)pyridine (5-…
acetylcholine receptors (nAChRs), we synthesized 5-iodo-3-(2(S)-azetidinylmethoxy)pyridine (5-…
Nicotinic acetylcholine receptor ligands, a patent review (2006–2011)
D Gündisch, C Eibl - Expert opinion on therapeutic patents, 2011 - Taylor & Francis
… be less than 1 μM to the receptor; ii) agonist activity (E max ) less than 10% of the E max of
an agonist; iii) the inhibiting receptor activation by an agonist via desensitization (IC 50(D) ) …
an agonist; iii) the inhibiting receptor activation by an agonist via desensitization (IC 50(D) ) …
Syntheses and evaluation of halogenated cytisine derivatives and of bioisosteric thiocytisine as potent and selective nAChR ligands
…, P Klaperski, MT Stubbs, G Seitz, D Gündisch - European journal of …, 2001 - Elsevier
… based on the measured IC 50 values and K d =10 pM for binding of (±)-[ 3 H]epibatidine
and K d =1 nM for [ 3 H]MLA. The K d values were obtained from five independent experiments …
and K d =1 nM for [ 3 H]MLA. The K d values were obtained from five independent experiments …
2-, 5-, and 6-Halo-3-(2(S)-azetidinylmethoxy)pyridines: Synthesis, Affinity for Nicotinic Acetylcholine Receptors, and Molecular Modeling
…, AG Horti, AG Mukhin, D Gündisch… - Journal of medicinal …, 1998 - ACS Publications
3-(2(S)-Azetidinylmethoxy)pyridine (A-85380) has been identified recently as a ligand with
high affinity for nicotinic acetylcholine receptors (nAChRs). Here we report the synthesis and …
high affinity for nicotinic acetylcholine receptors (nAChRs). Here we report the synthesis and …
Smoking upregulates α4β2* nicotinic acetylcholine receptors in the human brain
U Wüllner, D Gündisch, H Herzog, M Minnerop… - Neuroscience …, 2008 - Elsevier
… 2D). No region with reduced tracer uptake was found. … (D) Statistical parametric mapping
analysis using proportional scaling; the depicted areas exceed a voxelbased statistical …
analysis using proportional scaling; the depicted areas exceed a voxelbased statistical …
Cytisine-based nicotinic partial agonists as novel antidepressant compounds
…, G Young, C Kochevar, RL Papke, D Gündisch… - … of Pharmacology and …, 2009 - ASPET
Nicotine and other nicotinic agents are thought to regulate mood in human subjects and have
antidepressant-like properties in animal models. Recent studies have demonstrated that …
antidepressant-like properties in animal models. Recent studies have demonstrated that …
Synthesis and nicotinic binding studies on enantiopure diazine analogues of the novel (2-chloro-5-pyridyl)-9-azabicyclo [4.2. 1] non-2-ene UB-165
H Gohlke, D Gündisch, S Schwarz, G Seitz… - Journal of medicinal …, 2002 - ACS Publications
As part of our program aimed at optimizing therapeutic effects over toxic effects (as
observed in the naturally occurring nicotinic acetylcholine receptor modulators (−)-nicotine, (−)-…
observed in the naturally occurring nicotinic acetylcholine receptor modulators (−)-nicotine, (−)-…