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Status:
Possibly Marketed Outside US
Source:
Calblock by Daiichi Sankyo|Ube Industries
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Azelnidipine is a dihydropyridine calcium channel antagonist being jointly developed by Daiichi Sankyo Inc (formerly Sankyo) and Ube Industries. Azelnidipine is a L-type calcium channel antagonist. Azelnidipine was approved by Pharmaceuticals and Medicals Devices Agency of Japan (PMDA) on Jan 31, 2003. Azelnidipine is indicated for the treatment of hypertension. Its trend name is Calblock. Azelnidipine has two enantiomers (R-(−)- and S-( )-enantiomers) due to an asymmetric carbon at the 4-position, and the (R)-(−) enantiomer of dihydropyridine calcium antagonists is considered to possess intrinsic pharmacological activity. The
pharmacological action of azelnidipine resides in the (R)-enantiomer. This is in marked contrast to other calcium channel blocker (CCB) in which the (S)-enantiomer is responsible for the biological activity. There were no
significant differences in the inhibitory effects on TGF-b1-induced expression of COL1A1 mRNA among vitamin E - pretreated LX-2 cells
treated with azelnidipine (racemate), (R)-(-)-azelnidipine
or (S)-( )-azelnidipine, although the L-type
voltage-operated calcium channel blocking activity of (R)-(-)-
enantiomer was more potent than that of the (S)-( )-
enantiomer.
Status:
Possibly Marketed Outside US
Source:
Calblock by Daiichi Sankyo|Ube Industries
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Azelnidipine is a dihydropyridine calcium channel antagonist being jointly developed by Daiichi Sankyo Inc (formerly Sankyo) and Ube Industries. Azelnidipine is a L-type calcium channel antagonist. Azelnidipine was approved by Pharmaceuticals and Medicals Devices Agency of Japan (PMDA) on Jan 31, 2003. Azelnidipine is indicated for the treatment of hypertension. Its trend name is Calblock. Azelnidipine has two enantiomers (R-(−)- and S-( )-enantiomers) due to an asymmetric carbon at the 4-position, and the (R)-(−) enantiomer of dihydropyridine calcium antagonists is considered to possess intrinsic pharmacological activity. The
pharmacological action of azelnidipine resides in the (R)-enantiomer. This is in marked contrast to other calcium channel blocker (CCB) in which the (S)-enantiomer is responsible for the biological activity. There were no
significant differences in the inhibitory effects on TGF-b1-induced expression of COL1A1 mRNA among vitamin E - pretreated LX-2 cells
treated with azelnidipine (racemate), (R)-(-)-azelnidipine
or (S)-( )-azelnidipine, although the L-type
voltage-operated calcium channel blocking activity of (R)-(-)-
enantiomer was more potent than that of the (S)-( )-
enantiomer.
Status:
Possibly Marketed Outside US
Source:
Valerian by Bos, R. et al.
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Valerian is on the FDA’s list of substances that are generally recognised to be safe (GRAS). The root oil and extracts may be used as spice or seasoning. Valerian is most commonly used for sleep disorders. The essential oil of valerian contains a variety of compounds including valerenic acid and its derivatives, hydroxyvalerenic acid, acetoxyvalerenic acid and valerenal.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Betamipron (BP) is an amino acid derivative that has benzoyl and carboxyl groups in its structure, and it also has very low toxicity in mammals (LD50 in the rat, more than 3,000 mg/kg, i.v.). BP is a renal anionic transport inhibitor and decreases nephrotoxicity caused by high doses of carbapenems, anionic drugs, by inhibiting the drug accumulation in the renal cortex. BP significantly inhibited organic anion uptake by human organic anion transporter 1 (human-OAT1) and human-OAT3 in a dose-dependent manner. Panipenem-betamipron is marketed as Carbenin® (Sankyo Company, Tokyo, Japan).
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ABSOLUTE)
Zinc lactate is used to eliminate halitosis. Halitosis (commonly
known as bad breath) is a condition affecting many people and one of the most usual reasons why people go look for a dentist’s advice. The main
origin of halitosis is related to the volatile sulphur compounds (VSC) produced by the different bacterial colonies found on the tongue and in the
gingival crevices. Zinc lactate is a very effective solution to neutralize the VSC and an excellent ingredient for mouthwashes and toothpastes.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (RACEMIC)
HA-242, a benzodioxan derivative, is a muscle relaxant. It can be used for the treatment of central nervous muscular spasticity. Was marketed under the name Quiloflex. Quiloflex (HA-242) is a reflex inhibitor used in human medicine for the symptomatic treatment of spasticity due to pyramidal tract lesions. Quiloflex was also used for casting cattle and horses, and although well tolerated at a dosage of 1-8 mg/kg body wt. in cattle, it was unsuitable for use in this species as the onset of relaxation was slow and the sedation prolonged. A dosage of 6 mg/kg i/m in horses gave relaxation suitable for surgery in 30 min.
Status:
Possibly Marketed Outside US
Source:
S-Adchnon by Yasuhito Yamanishi|Shiraimatsu Shinyaku
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Adrenochrome monoaminoguanidine (S-Adchnon) is a hemostatic capillary-stabilizing agent demonstrating pharmacological effects against radiation injury by reducing side effects of radiation therapy on hematopoietic organ. Synthesized by a dehydrating reaction of adrenochrome and aminoguanidine it has superior properties than adrenochrome, an oxidation product of adrenalin remarkable for its efficiency as a haemostatic agent at very small doses and for its more rapid and equally intense action than that of adrenalin. Adrenochrome does not alter the cardiac rhythm and does not cause any hypertension or internal haemorrhages and would be suitable for therapeutic applications, however, its instability, in aqueous or alcoholic solution, makes its use substantially impossible. S-Adchnon was devised, approved by the Japanese Ministry of Health, Labor and Welfare in 1962 and used widely in Japan. Adrenochrome monoaminoguanidine has negligible toxicity, stable and could be made into salts for aqueous dosage, especially for injection. Adrenochrome monoaminoguanidine methanesulfonate (AMM) enhances the recovery from radiation-induced leukopenia in rabbits and in humans, and inhibits the increases in chromosome aberrations in peripheral lymphocytes of patients with cervical carcinoma under radiotherapy. It has been shown that the radiation-induced initial decrease in number of peripheral blood leukocytes (PBL) is not affected by AMM, but recovery from the decrease is enhanced, shortening the period of leukopenia. This suggests that AMM may not exert its effects by protecting PBL directly but by protecting stem and/or progenitor cells in hematogenesis which proliferate and differentiate to PBL after irradiation. In in vitro colony formation method AMM demonstrated a protective effect on the survival of GM-CFC, a hematopoietic progenitor cells. Differential action on cancer and normal tissue by AMM and cytochrome C combined with radiotherapy was demonstrated. AMM in combination with cytochrome C augumented natural killer (NK) cells activity in KSN nude mice, protected potent NK cells in patients with lung cancer against radiotherapy and sensitized the human lung cancer xenografts to radiotherapy. Thus, AMM and cytochrome C may have the potential as a differential modulator of radiosensitivity of normal tissues and of tumors.
Status:
Possibly Marketed Outside US
Source:
NCT02380053: Phase 4 Interventional Completed Chronic Obstructive Pulmonary Disease
(2016)
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Celiprolol is beta blocker, used to treat high blood pressure. Celiprolol is a selective β1 receptor antagonist, β2 receptor partial agonist. Celiprolol is not approved by the FDA, but is available worldwide under brand names Cardem, Selectol, Celipres, Celipro, Celol, Cordiax, Dilanorm. It is used to treat mild to moderate hypertension and angina prectoris. In 2010 celiprolol has demonstrated positive results in the prevention of vascular complications of Ehlers-Danlos syndrome. Celiprolol has fewer CNS-related side effects than other beta blockers presumably because of limited penetration through blood-brain barrier because of its solubility.
Status:
Possibly Marketed Outside US
Source:
Cordanum by Eckardt, R.|Carstens, E.|Femmer, K.
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Talinolol (brand name Cordanurn) is the cardioselective beta-receptor antagonist which has been used for a long time in the treatment of various cardiovascular diseases and in tachyarrhythmia. The mean dosage is 10-20 mg intravenously administered over a period of 3-5 minutes, while the chronic oral dosage for this patient group amounts to 300mg/day. Cordanum eliminates the stimulating effect of catecholamines on the heart for physical and psychoemotional stress. The hypotensive effect is stabilized by the end of 2 weeks of course treatment. Reduces the frequency and severity of angina attacks; Contributes to the limitation of the heart attack zone and reduces the risk of arrhythmia in the presence of myocardial infarction, resulting in a decrease in mortality and the frequency of relapses. In average therapeutic doses, it has a less pronounced effect on the smooth muscles of the bronchi, myometrium, and peripheral arteries compared to non-selective beta-blockers. Talinolol is used in supraventricular (atrial fibrillation and flutter with high ventricular rate, paroxysmal supraventricular 1 tachycardia, sinus tachycardia) as well as ventricular extrasystoles and ventricular tachyarrhythmias. Patients with an increased tonus of the sympathetic nervous system related to sinus tachycardia, exercise-induced arrhythmias, hypertension, hyperthyroidism and coronary heart disease show a particularly positive reaction.
Status:
Possibly Marketed Outside US
Source:
Unknown
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
8-Hydroxyquinoline is is a heterocyclic phenol, exhibiting antiseptic, disinfectant and pesticide properties. It is used to prevent and treat vaginal bacterial infections, but the efficacy was not proven in clinical trial. 8-Hydroxyquinoline is used in over-the-counter remedies for diaper rash and oral health care. Its use for veterinary treatment of bacterial an skin infections is not approved by FDA. 8-Hydroxyquinoline acts by inhibition of RNA synthesis and DNA replication by chelating the dissociable cations Mn2 and Mg2 .