Search Results - "Buschmann, Helmut"

Bioactive sulfoximines: Syntheses and properties of Vioxx® analogs by Park, Seong Jun, Buschmann, Helmut, Bolm, Carsten

“…The syntheses and biological profiles of sulfoximine-based Vioxx® analogs 2 are described. Interesting data have been obtained for 2a, which shows a selective…”
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Synthesis and Biological Evaluation of the 1‑Arylpyrazole Class of σ1 Receptor Antagonists: Identification of 4‑{2-[5-Methyl-1-(naphthalen-2-yl)‑1H‑pyrazol-3-yloxy]ethyl}morpholine (S1RA, E‑52862) by Díaz, José Luis, Cuberes, Rosa, Berrocal, Joana, Contijoch, Montserrat, Christmann, Ute, Fernández, Ariadna, Port, Adriana, Holenz, Jörg, Buschmann, Helmut, Laggner, Christian, Serafini, Maria Teresa, Burgueño, Javier, Zamanillo, Daniel, Merlos, Manuel, Vela, José Miguel, Almansa, Carmen

“…The synthesis and pharmacological activity of a new series of 1-arylpyrazoles as potent σ1 receptor (σ1R) antagonists are reported. The new compounds were…”
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N-Cyano Sulfoximines: COX Inhibition, Anticancer Activity, Cellular Toxicity, and Mutagenicity by Park, Seong Jun, Baars, Hannah, Mersmann, Stefanie, Buschmann, Helmut, Baron, Jens Malte, Amann, Philipp M., Czaja, Katharina, Hollert, Henner, Bluhm, Kerstin, Redelstein, Regine, Bolm, Carsten

“…From insects to cancer: N‐Cyano sulfoximines were evaluated for COX inhibition and antiproliferative activity against a panel of cancer cell lines. The most…”
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Syntheses and biological activities of sulfoximine-based acyclic triaryl olefins by Chen, Xiao Yun, Park, Seong Jun, Buschmann, Helmut, De Rosa, Maria, Bolm, Carsten

“…Sulfoximine-based acyclic triaryl olefins 8 and 9 have been prepared and initial studies have been performed to determine their biological profiles. In…”
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5-HT7 receptor activation inhibits mechanical hypersensitivity secondary to capsaicin sensitization in mice by Brenchat, Alex, Romero, Luz, García, Mónica, Pujol, Marta, Burgueño, Javier, Torrens, Antoni, Hamon, Michel, Baeyens, José Manuel, Buschmann, Helmut, Zamanillo, Daniel, Vela, José Miguel

“…This work aimed to evaluate the potential role of the 5-HT(7) receptor in nociception secondary to a sensitizing stimulus in mice. For this purpose, the…”
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Mechanistic and functional differentiation of tapentadol and tramadol by Raffa, Robert B, Buschmann, Helmut, Christoph, Thomas, Eichenbaum, Gary, Englberger, Werner, Flores, Christopher M, Hertrampf, Torsten, Kögel, Babette, Schiene, Klaus, Straßburger, Wolfgang, Terlinden, Rolf, Tzschentke, Thomas M

“…Many opioid analgesics share common structural elements; however, minor differences in structure can result in major differences in pharmacological activity,…”
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Sigma-1 receptor antagonism as opioid adjuvant strategy: Enhancement of opioid antinociception without increasing adverse effects by Vidal-Torres, Alba, de la Puente, Beatriz, Rocasalbas, Maria, Touriño, Clara, Andreea Bura, Simona, Fernández-Pastor, Begoña, Romero, Luz, Codony, Xavier, Zamanillo, Daniel, Buschmann, Helmut, Merlos, Manuel, Manuel Baeyens, José, Maldonado, Rafael, Vela, José Miguel

“…While opioids are potent analgesics widely used in the management of pain, a number of well-known adverse effects limit their use. The sigma-1 receptor is a…”
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New Developments in the Origins of the Homochirality of Biologically Relevant Molecules by Buschmann, Helmut, Thede, Richard, Heller, Detlef

“…Perhaps it is the intrinsic chirality at the level of elementary particles that accounts for why relevant biomolecules (proteinogenic amino acids and sugar…”
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Differential anti-neuropathic pain effects of tetrodotoxin in sciatic nerve- versus infraorbital nerve-ligated rats – Behavioral, pharmacological and immunohistochemical investigations by Kayser, Valérie, Viguier, Florent, Ioannidi, Myrto, Bernard, Jean-François, Latrémolière, Alban, Michot, Benoît, Vela, José-Miguel, Buschmann, Helmut, Hamon, Michel, Bourgoin, Sylvie

“…Several voltage-gated sodium channels are expressed in primary sensory neurons where they control excitability and participate in the generation and…”
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Functional and Molecular Characterization of Voltage-Gated Sodium Channels in Uteri from Nonpregnant Rats by SEDA, Marian, PINTO, Francisco M, WRAY, Susan, CINTADO, Cristina G, NOHEDA, Pedro, BUSCHMANN, Helmut, CANDENAS, Luz

“…We investigated the function and expression of voltage-gated Na + channels (VGSC) in the uteri of nonpregnant rats using organ bath techniques, intracellular…”
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The quality of drugs and drug products - Always guaranteed? by Buschmann, Helmut, Handler, Norbert, Holzgrabe, Ulrike

“…To ensure the efficacy, safety, and quality of drugs, several national and international guidelines and regulatory requirements exist. The most important…”
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Functional and Molecular Characterization of Voltage-Gated Sodium Channels in Uteri from Nonpregnant Rats1 by Seda, Marian, Pinto, Francisco M, Wray, Susan, Cintado, Cristina G, Noheda, Pedro, Buschmann, Helmut, Candenas, Luz

“…We investigated the function and expression of voltage-gated Na+ channels (VGSC) in the uteri of nonpregnant rats using organ bath techniques, intracellular…”
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Different solid forms for optimizing route of administration of the herpes drug Pritelivir by Ruebsamen-Schaeff, Helga, Buschmann, Helmut

“…Pritelivir (AIC316, BAY 57-1293) was discovered as a highly potent drug against herpes simplex viruses with a novel mode of action, i.e. inhibition of the…”
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Stereoselective and efficient synthesis of ( S)-pregabalin from d-mannitol by Izquierdo, Sandra, Aguilera, Jordi, Buschmann, Helmut H., García, Mónica, Torrens, Antoni, Ortuño, Rosa M.

“…A straightforward synthesis of ( S)-pregabalin in 28% overall yield starting from d-mannitol acetonide, as a primary source of chirality, is presented. The…”
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Application of advanced high resolution mass spectrometric techniques for the analysis of losartan potassium regarding known and unknown impurities by Backer, Laura, Buschmann, Helmut, Kinzig, Martina, Sörgel, Fritz, Scherf-Clavel, Oliver, Holzgrabe, Ulrike

“…Recalls of medicinal products can cause supply bottlenecks. This is often due to the findings of unexpected impurities that pose a health risk to patients. A…”
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Prediction of Degradation Profiles for Various Sartans under Solvent-Free Mechanochemical Conditions by Amer, Mostafa M., Backer, Laura, Buschmann, Helmut, Handler, Norbert, Scherf-Clavel, Oliver, Holzgrabe, Ulrike, Bolm, Carsten

“…For the approval of a drug, the stability data must be submitted to regulatory authorities. Such analyses are often time-consuming and cost-intensive. Forced…”
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Strategy to Assess and Control Nitrosamine Formation in API during Storage: A Sitagliptin Case Study by Badia, Laura, Camps, Helena, Lloveras, Isabel, Handler, Norbert, Buschmann, Helmut, Valls, Jordi, Poznik, Michal

“…A new strategy to identify, assess, and mitigate the nitrosamine formation in APIs during storage was developed and demonstrated on sitagliptin hydrochloride…”
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Discovery, Chemistry, and Preclinical Development of Pritelivir, a Novel Treatment Option for Acyclovir-Resistant Herpes Simplex Virus Infections by Birkmann, Alexander, Bonsmann, Susanne, Kropeit, Dirk, Pfaff, Tamara, Rangaraju, Manickam, Sumner, Melanie, Timmler, Burkhard, Zimmermann, Holger, Buschmann, Helmut, Ruebsamen-Schaeff, Helga

“…When the nucleoside analogue acyclovir was introduced in the early 1980s, it presented a game-changing treatment modality for herpes simplex virus infections…”
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New approaches to treating pain by Wolkerstorfer, Andrea, Handler, Norbert, Buschmann, Helmut

“…After 100years of pain research—old scaffolds, minor improvements? [Display omitted] Pain is the most common reason for patients seeking medical care resulting…”
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Ball milling - a new concept for predicting degradation profiles in active pharmaceutical ingredients by Kaiser, Reinhard P, Krake, Everaldo F, Backer, Laura, Urlaub, Jonas, Baumann, Wolfgang, Handler, Norbert, Buschmann, Helmut, Beweries, Torsten, Holzgrabe, Ulrike, Bolm, Carsten

“…A method for forced oxidative mechanochemical degradation of active pharmaceutical ingredients (APIs) using clopidogrel hydrogensulfate as a model compound is…”
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