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Carboxamides

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cx516
CX-516 is an ampakine and nootropic that acts as an AMPA receptor positive allosteric modulator and had been undergoing development by a collaboration between Cortex, Shire, and Servier. It was studied as a potential treatment for Alzheimer's disease under the brand name Ampalex, and was also being examined as a treatment for ADHD.
otenabant
Otenabant (CP-945,598) is a drug that acts as a potent and highly selective CB1 antagonist. It was developed by Pfizer for the treatment of obesity, but development for this application has been discontinued following the problems seen during clinical use of the similar drug rimonabant.
cerulenin
Cerulenin is an antifungal antibiotic that inhibits fatty acid and steroid biosynthesis. It was the first natural product antibiotic known to inhibit lipid synthesis. In fatty acid synthesis, it has been reported to bind in equimolar ratio to b-keto-acyl-ACP synthase, one of the seven moieties of fatty acid synthase, blocking the interaction of malonyl-CoA. It also has the related activity of stimulating fatty acid oxidation through the activation of CPT1, another enzyme normally inhibited by malonyl-CoA. Inhibition involves covalent thioacylation that permanently inactivates the enzymes. Thes
tiracizine
Tiracizine is an antiarrhythmic agent.
SB-277,011-A
SB-277,011A is a drug which acts as a potent and selective dopamine D3 receptor antagonist, which is around 80–100times selective for D3 over D2, and lacks any partial agonist activity.
4-nonanoylmorpholine
4-Nonanoylmorpholine [pelargonic acid morpholide, N-nonanoylmorpholine, MPK or МПК (for '), or MPA'] is an amide of pelargonic acid and morpholine. It is an ingredient of tear gas.
α-ergocryptine
Ergocryptine is an ergopeptine and one of the ergoline alkaloids. It is isolated from ergot or fermentation broth and it serves as starting material for the production of bromocriptine. Two isomers of ergocryptine exist, α-ergocryptine and β-ergocryptine. The beta differs from the alpha form only in the position of a single methyl group, which is a consequence of the biosynthesis in which the proteinogenic amino acid leucine is replaced by isoleucine. β-Ergocryptine was first identified in 1967 by Albert Hofmann. Ergot from different sources have different ratios of the two isomers.
sb-216641
SB-216641 is a drug which is a selective antagonist for the serotonin receptor 5-HT1B, with around 25x selectivity over the closely related 5-HT1D receptor. It is used in scientific research, and has demonstrated anxiolytic effects in animal studies.
quinaprilat
Quinaprilat is the active metabolite of quinapril.
LP-12
LP-12 is a drug which acts as a potent agonist at the 5HT7 serotonin receptor, with very high selectivity over other tested receptor subtypes such as the serotonin 5-HT1A and 5-HT2A, and the dopamine D2 receptor. It has been used to research the involvement of the 5-HT7 receptor in as yet poorly understood processes such as allodynia and hyperalgesia.
tomopenem
Tomopenem (formerly CS-023) is a carbapenem β-lactam antibiotic.
fenoverine
Fenoverine (INN) is an antispasmodic [also known as spasmolytics] drug, which acts by inhibiting calcium channels [much in the same way as traditional calcium channel blockers, which are used as antianginal drugs]. In the case of Fenoverine, the relaxation occurs in abdominal / intestinal smooth muscles, while in case of antianginal drugs, the relaxation occurs in coronary vessels. Notably Fenoverine does not act as an antianginal agent. ==Toxicity== Fenoverine is known to cause rhabdomyolysis. ==References==
BU-LAD
BU-LAD, also known as 6-butyl-6-nor-LSD or '6-butyl-6-nor-lysergic acid diethylamide', is a psychedelic drug and analogue of lysergic acid diethylamide (LSD) first described by David E. Nichols and colleagues in the 1980s.
carboxyamidotriazole
Carboxyamidotriazole is a calcium channel blocker that blocks voltage-gated and ligand-gated calcium channels and has been investigated as an anti-cancer drug in vitro.
bucladesine
Bucladesine is a cyclic nucleotide derivative which mimics the action of endogenous cAMP and is a phosphodiesterase inhibitor.
Cellocidin
Cellocidin (2-butynediamide) is an organic chemical compound with the molecular formula C4H4O2N2. This compound was isolated from Streptomyces chibaensis, Streptomyces reticuli and Streptomyces sp. SF-536.
esaxerenone
Esaxerenone () (brand name Minnebro; developmental code names CS-3150, XL-550) is a nonsteroidal antimineralocorticoid which was discovered by Exelixis and developed by Daiichi Sankyo Company and is approved in Japan for the treatment of hypertension. It acts as a highly selective silent antagonist of the mineralocorticoid receptor (MR), the receptor for aldosterone, with greater than 1,000-fold selectivity for this receptor over other steroid hormone receptors, and 4-fold and 76-fold higher affinity for the MR relative to the existing antimineralocorticoids spironolactone and eplerenone.
ibodutant
Ibodutant was a candidate drug for irritable bowel syndrome diarrhea, developed by The Menarini Group. , it underwent a multicentre double blind efficacy clinical study. Ibodutant selectively blocks the tachykinin receptor NK2, with blockade practically complete in nanomolar concentrations. A phase 2 trial in Europe (the IRIS-2 trial) completed in May 2012 with positive results. A 52-week phase 3 study was terminated as of 2015 because of low response and negative results of study NAK-06.
posizolid
Posizolid is an oxazolidinone antibiotic under investigation by AstraZeneca for the treatment of bacterial infections. At a concentration of 2 mg/L it inhibited 98% of all Gram-positive bacteria tested in vitro.