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Restrict the search for
nonoxynol-9
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Class (Stereo):
CHEMICAL (RACEMIC)
Picenadol is a 4-phenylpiperidine derivative and a racemic mixture whose mixed agonist-antagonist properties are a consequence of the d-isomer being a potent opiate agonist, whereas the I-isomer is an opioid antagonist. In the mouse writhing and rat tail heat tests, the analgesic potency of picenadol is estimated to be 1/3 that of morphine. Picenadol itself has weak antagonist activity, whereas the antagonist potency of the l-isomer is approx. 1/10 that of nalorphine. Picenadol has high affinity for both the mu and delta receptors but a markedly lower affinity for the kappa receptor. Extensive pharmacological investigations show picenadol to have a low potential to produce opiate-like side effects, including a low liability for abuse and physical dependence. Antinociceptive properties of picenadol arise from mu agonist actions of the dextrorotatory isomer and that the levorotatory isomer acts to limit the efficacy of the racemate.
Status:
Class (Stereo):
CHEMICAL (ACHIRAL)
Nolinium bromide (NB) is a nonanticholinergic, gastric acid antisecretory agent and a gastrointestinal tract antispasmodic agent. The gastrointestinal antispasmodic action of NB has been demonstrated in a variety of test systems. The compound inhibited electrically induced contractions of rabbit ileum and nicotine-induced contractions of rat ileum in vitro, gastric emptying in fasted rats, and intestinal transport of a charcoal meal in mice. In the anesthetized dog, NB antagonized colonic contractions induced by acetylcholine, histamine, serotonin, and pelvic nerve stimulation, and duodenal contractions due to vagal stimulation and acetylcholine. In the unanesthetized dog, feeding induced colonic and duodenal motilities were inhibited by NB. The antisecretory action of NB may involve inhibition of enzymes of gastric acid secretion, specifically histamine-stimulated adenylate cyclase and potassium-stimulated ATPase. NB has no direct histamine-H2 receptor blocking properties. Nolinium bromide inhibits in a dose-dependent manner both the gastric H+, K+-ATPase activity and H+ uptake ability of the gastric microsomes. Increasing concentrations of K+ could reverse the nolinium bromide inhibition of both the H+, K+-ATPase activity and vesicular H+ transport. Nolinium bromide interferes primarily with the K+-dependent phosphatase step and thereby reduces the turnover of the enzyme. The drug acts as a K+ antagonist in the gastric H+ +K+-dependent ATPase reaction.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Rosamaricin is a macrolide antibiotic similar to erythromycin. This compound is more effective against Gram-negative bacteria than erythromycin, especially in the prostate where rosamaricin was shown to be more concentrated than erythromycin in dogs. Rosamaricin has antibiotic activity against Neisseria gonorrhoeae, Chlamydia trachomatis, Ureaplasma urealyticum and Mycoplasma hominis. When the drug was compared with penicillin G in the treatment of pneumococcal meningitis in rabbits it was found to be less effective than penicillin G, as measured by bacterial clearance from cerebrospinal fluid and by treatment outcome. No information on the current use of this compound is available.
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Tomelukast (previously known as LY171883), an orally active antagonist of the CysLT1 receptor (leukotriene D4), which was investigated to treat asthma, but this study was discontinued because of adverse gastrointestinal effect.
Status:
Investigational
Source:
NCT04227756: Phase 1 Interventional Completed Healthy
(2020)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Class (Stereo):
CHEMICAL (ACHIRAL)
Tampramine (also known as AHR-9377) is a potent and selective, noncompetitive inhibitor of norepinephrine reuptake possesses antidepressant activity. This drug was studied for the treatment of the major depressive disorder; however, this study was discontinued.
Status:
Investigational
Class (Stereo):
CHEMICAL (RACEMIC)
Tandamine was developed as a selective serotonin reuptake inhibitor for the treatment of depression. Tandamine participated in clinical trials in hospitalized depressed patients, where it showed that the well-tolerated drug could be of some benefit for retarded depressions. In addition, was found in human volunteers, that tandamine possessed significant anticholinergic activity, to reduce appetite and to produce sedation. However, this drug has never been marketed.
Status:
Investigational
Source:
INN:dezaguanine [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Dezaguanine is a broad spectrum guanine antimetabolite. This compound differs from guanine only in the substitution of a carbon for the 3-nitrogen of guanine. Dezaguanine must be converted to its nucleotides to be active. Dezaguanine nucleotides inhibit synthesis of guanine nucleotides, and can be incorporated into nucleic acids in place of guanine nucleotides; incorporation into DNA may be particularly important in the cytotoxicity of this compound. Addition of certain purines or purine nucleosides can prevent dezaguanine cytotoxicity in vitro. It has exhibited sufficient preclinical antitumor activity, particularly against rat and mouse mammary adenocarcinomas, slow and fast growing mammary tumors in mice and the human breast xenograft subrenal capsule implant system. It has completed one phase I trial.
Status:
Investigational
Source:
INN:milipertine [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Milipertine was studied in patients with severe schizophrenia. Information about the current use of the drug is not available.
Status:
Investigational
Source:
Cancer Treat Rep. 1981;65(7-8):689-92.: Phase 3 Human clinical trial Completed Kidney Neoplasms/pathology
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Nafoxidine is a nonsteroidal antiestrogen available as an investigational agent from the Investigational Drug Branch of the National Cancer Institute. It has been used effectively in the treatment of breast cancer patients. Nafoxidine competes with endogenous estrogen for binding to specific estrogen receptors. This agent also inhibits angiogenesis in some tissues by blocking the effects of fibroblast growth factor (FGF) and vascular endothelial growth factor (VEGF); paradoxically, it may enhance angiogenesis in uterine tissue. Nafoxidine also induces oxidative stress, protein kinase C and calcium signaling.
