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Restrict the search for
phenyl aminosalicylate
to a specific field?
Class (Stereo):
CHEMICAL (ACHIRAL)
FETOXYLATE, a phenoxyethyl ester of diphenoxylate, is an opioid receptor agonist. It is used as antidiarrheal.
Status:
Investigational
Source:
INN:esoxybutynin [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Esoxybutynin is (S)-enantiomer of oxybutynin. Esoxybutynin exerts antimuscarinic properties. Racemic oxybutynin is used clinically to treat urinary incontinence. Sepracor was developing (S)-oxybutynin, a single-isomer version of Alza's Ditropan (racemic oxybutynin), a muscarinic acetylcholine receptor antagonist, as a potential treatment for urinary incontinence.
Class (Stereo):
CHEMICAL (UNKNOWN)
Prodilidine is an arylpyrrolidine derivative patented by Mead Johnson & Co.as moderately potent analgesic. By comparison with other drugs, including morphine, Prodilidine has a prompt and unusually sustained antinociceptive action in rodents by all routes. Prodilidine substantially lacks antipyretic, anti-inflammatory, antitussive, constipating, respiratory depressant, and cardiovascular effects. Prodilidine resembles meperidine in excitatory properties and body-temperature lowering action at high dosage. The d-isomer is about twice as potent and toxic as the l-isomer parenterally; by the gastric route, the difference is markedly less.
Status:
Investigational
Class (Stereo):
CHEMICAL (RACEMIC)
Denzimol is a new imidazole derivative with anticonvulsant properties. Denzimol suppressed electrically and chemically induced tonic seizures but did not prevent the clonic ones. Denzimol prolongs pentobarbitone sleeping times indicating that drug binds to rat liver microsomes and are potent inhibitors in the rat of mixed function monooxygense activities both in‐vitro and in‐vivo. The antiepileptic activity of the denzimol has been evaluated in patients with poorly controlled partial epilepsy by adding on the drug to the current therapy. Although denzimol increased blood concentrations of carbamazepine, correlation analysis indicated that the improvement was more likely due to intrinsic properties of denzimol. No severe side effects were reported, although several patients experienced nausea and vomiting, which caused 2 patients to drop out. The drug did not show any mutagenic activity when compared with mutagenic standards.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Fanetizole is a derivative of 2-aminothiazole. It is an anti-inflammatory agent. This drug is reported to have some cyclooxygenase inhibiting activity. Production of superoxide in response to the chemotactic factor formyl-methionyl-leucyl-phenylalanine (f-Met-Leu-Phe) was markedly inhibited by fanetizole. Suppression of neutrophil production of toxic oxygen metabolites may partially explain the antiarthritic effect of fanetizole. Fanetizole was shown to restore depressed E-rosetting activity in adult thymectomized mice, as well as enhance in in vitro proliferation of murine thymic cells to mitogen and synergistically acted with the monokine interleukin-1. It displays anti-arthritic activity in viva in the rat adjuvant arthritis model, inhibiting the development of disease in the non-infected foot. This drug has less side effects than levamisole in animals.
Class (Stereo):
CHEMICAL (ACHIRAL)
Seperidol (also known as clofluperol or R9298), a butyrophenone derivative that was developed as an antipsychotic agent. This compound was studied as a long-acting neuroleptic. However, information about the current use of seperidol is not available.
Status:
Investigational
Source:
NCT03739125: Phase 3 Interventional Completed Type2 Diabetes
(2017)
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Lobeglitazone (trade name Duvie; Chong Kun Dang Pharmaceutical Corporation) was developed as effective and safe antidiabetic TZD drug. Lobeglitazone is a peroxisome proliferator-activated receptor-γ agonist. Lobeglitazone was conceptually designed by modification of the rosiglitazone structure with a substituted pyrimidine. Lobeglitazone has a p-methoxyphenoxy group at the 4-position of the pyrimidine moiety. Lobeglitazone showed more potent activity than the reference compounds (pioglitazone and rosiglitazone) with an EC50 value of 0.018 uM in a type 2 diabetes animal model, which is 16 times lower than pioglitazone (EC50 0.30 uM). Lobeglitazone exhibited similar efficacy profiles in glycemic control and lipid modulation to pioglitazone, but with a 30 times smaller dose in clinical studies. Lobeglitazone displays 12 times higher affinity to PPARγ than rosiglitazone and pioglitazone. Lobeglitazone acts as an insulin sensitizer by binding and activating Peroxisome Proliferator-Activated Receptors (PPAR) gamma within fat cells. By promoting the binding of insulin at fat cells, lobeglitazone has been shown to reduce blood sugar levels, lower hemoglobain A1C (HbA1C) levels, and improve lipid and liver profiles. Lobeglitazone was approved by the Ministry of Food and Drug Safety (Korea) in 2013. Lobeglitazone is not approved for use by either the Food and Drug Administration (USA), Health Canada, or by the European Medicines Agency for use in the management of diabetes.
Class (Stereo):
CHEMICAL (RACEMIC)
Diacetolol is the major metabolite of the β-adrenoceptor blocking agent, acebutolol. In vitro, the β-adrenoceptor blocking potency of diacetolol was less than that of acebutolol but its cardioselectivity (atrial relative to tracheal tissue) was greater. Diacetolol had weak intrinsic sympathomimetic activity, and no significant membrane-stabilizing activity. It did not restore sinus rhythm to anaesthetized dogs with ouabain-induced arrhythmias but was similar to acebutolol in preventing arrhythmia induced by adrenaline/methylchloroform in anaesthetized cats. Study of diacetolol pharmacokinetics and bioavailability suggests either a first-pass effect or incomplete absorption of diacetolol after oral administration. Diacetolol plasma half-life after oral administration is about 12 h and is not dose-dependent. Diacetolol possesses significant antihypertensive action against moderate essential hypertension in man. Its antihypertensive effect is associated with a reduction in the heart rate and a decrease in plasma renin activity.
Status:
Class (Stereo):
CHEMICAL (ACHIRAL)
Stilbazium is a pyridinium derivative with considerable anthelminthic activity against some animal nematodes, including Syphacia obvelata, Ancylostoma caninum, Uncinaria stenocephala and Toxocara cati.
Status:
Class (Stereo):
CHEMICAL (MIXED)
Hexopyrronium is an antihistaminic agent. Its gastric antisecretory action was studied in human. Information about the current use of this drug is not available.
