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Restrict the search for
methyl aminolevulinate
to a specific field?
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Napamezole [WIN 51181] is a potent alpha-2 adrenergic receptor antagonist and a selective inhibitor of 5-hydroxytryptamine re-uptake in vitro. Napamezole was at the phase I stage of development with Sanofi Winthrop (formerly known as Sterling Drug before it was purchased by Sanofi) in the USA as a treatment for depression. The alpha adrenergic antagonist activity of napamezole was determined in vitro in rat brain receptor binding assay using [3H]clonidine and [3H]prazosin for alpha-2 and alpha-1 receptors, respectively. The Ki values for napamezole were 28 nM (alpha-2) and 93 nM (alpha-1).
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Tamitinol (also known as EMD 21657), a neurotropic drug that was developed as a cognition enhancer for the treatment of diffuse cerebral disease and organic brain syndrome. Tamitinol participated in clinical trials where the therapeutic effects of the drug were shown to be statistically significant compared to placebo in the global response. However, the treatment was interrupted because of side effects (increased aggressiveness, rash) in 2 cases.
Class (Stereo):
CHEMICAL (ACHIRAL)
Fluradoline (also known as HP-494), a centrally acting antinociceptive agent with antidepressant properties. Experiments on rodents have shown that fluradoline blocked the reuptake of NE, 5-HT, and DA in the brain. Besides, fluradoline was studied for the prevention of acute and chronic postsurgical pain.
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
There is no information about biological and medical application of dorastine . It’s known, that compound possesses antihistamine properties and can be obtained from 4-chloroaniline.
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Pravadoline is the anti-nociceptive agent, which has analgesic efficacy against postoperative pain in humans. Pravadoline inhibits the enzyme cyclooxygenase, but in contrast to cyclooxygenase-inhibiting NSAIDs does not produce gastrointestinal irritation. Pravadoline inhibited the synthesis of prostaglandins in mouse brain both in vitro and ex vivo. Pravadoline demonstrated only weak anti-inflammatory activity relative to its anti-nociceptive potency. Single doses of pravadoline were safe and effective in humans, without serious adverse events. Single oral administration of pravadoline maleate induced acute tubular necrosis in male and female beagle dogs.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Doxybetasol is the corticosteroid. It is an impurity of Betamethasone, which is a glucocorticoid used as an anti-inflammatory agent. Doxybetasol also has anti-inflammatory and anti-allergic properties.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Crisnatol is a derivative of arylmethylaminopropanediol with significant antineoplastic activity in a variety of murine and human tumor models. Crisnatol functions as a DNA intercalator, with the presence of additional basic amine groups in the sidechain enhancing binding to DNA due to electrostatic interactions. Crisnatol did not show antitumor efficacy in patients with ovarian carcinoma. In another clinical study, 2 of 26 patients with glioma showed complete long-lasting responses to the drug. The dose-limiting side effect was neurotoxicity.
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.
Status:
Investigational
Source:
INN:racemethorphan [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Racemethorphan is racemic mixture of Dextromethorphan and Levomethorphan. Racemethorphan is listed under the Single Convention on Narcotic Drugs 1961 and is therefore listed in the United States as a Controlled Substance, specifically as a Narcotic in Schedule II. Dextromethorphan is a non-narcotic morphine derivative widely used as an antitussive. Dextromethorphan is a cough suppressant in many over-the-counter cold and cough medicines. In 2010, the FDA approved the combination product dextromethorphan/quinidine for the treatment of pseudobulbar affect. Dextromethorphan suppresses the cough reflex by a direct action on the cough center in the medulla of the brain. Levomethorphan is an opioid analgesic of the morphinan family that has never been marketed.
Status:
Investigational
Source:
INN:fenmetozole [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Fenmetozole is an alpha-2 adrenergic receptor antagonist which was developed for the treatment of schizophrenic and/or depressed patients, however never reached the market. It was also shown that the drug may reduce symptoms of minimal brain dysfunction in children and antagonize the effect of barbiturates and ethanol.
