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Status:
Possibly Marketed Outside US
Source:
Unknown by Takeda Chemical Industries
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Manidipine, (S)- is enantiomer of Manidipine a lipophilic, third-generation dihydropyridine calcium channel antagonist with a high degree of selectivity for the vasculature, thereby inducing marked peripheral vasodilation with negligible cardiodepression. Manidipine has different pharmacological effects and (S)-manidipine is shown to be about 30–80 times more potent than (R)-manidipine in its antihypertensive action and in the radioligand binding assay. Patch-clamp experiments revealed that the S-enantiomers of manidipine displayed a faster onset of action and produced a greater blockade than the R-enantiomer. Also, manidipine enantiomers have markedly different pharmacokinetics and the S/R ratio for (S)- and (R)-enantiomer concentrations is 2.0
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (UNKNOWN)
Targets:
Perhexiline, 2-(2,2-dicyclohexylethyl)piperidine, is an anti-anginal drug. Perhexiline reduces fatty acid metabolism through the inhibition of carnitine palmitoyltransferase, the enzyme responsible for mitochondrial uptake of long-chain fatty acids. Perhexiline is used for reducing the frequency of moderate to severe attacks of angina pectoris due to coronary artery disease in patients who have not responded to other conventional therapy or in whom such therapy may be contraindicated. Heart Metabolics Limited is developing perhexiline for the treatment of hypertrophic cardiomyopathy
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (UNKNOWN)
Targets:
Perhexiline, 2-(2,2-dicyclohexylethyl)piperidine, is an anti-anginal drug. Perhexiline reduces fatty acid metabolism through the inhibition of carnitine palmitoyltransferase, the enzyme responsible for mitochondrial uptake of long-chain fatty acids. Perhexiline is used for reducing the frequency of moderate to severe attacks of angina pectoris due to coronary artery disease in patients who have not responded to other conventional therapy or in whom such therapy may be contraindicated. Heart Metabolics Limited is developing perhexiline for the treatment of hypertrophic cardiomyopathy
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Lappaconitine is an alkaloid isolated from the root of Aconltitum sinomantanum Nakai. It has a strong analgesic activity that does not involve the opioid receptor. It was shown to have class-I antiarrhythmic action and irreversibly blocks cloned human heart (hH1) channels by binding to the site 2 receptor.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Fomocaine is a local anesthetic used in the gel formulations for the relief of pain associated with burns and wounds. Fomocaine blocks both sodium and calcium voltage-gated ion cahnnel currents.
Status:
Possibly Marketed Outside US
Source:
JAMA Netw Open. May 2024;7(5):e248661.: Phase 4 Human clinical trial Completed Vaginosis, Bacterial
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Dequalinium is a quaternary ammonium cation commonly available as the dichloride salt. Dequalinium chloride has an antiseptic effect against a wide range of bacteria, yeasts, and some fungi and viruses. It kills the micro-organisms associated with various mild infections of the mouth and throat. Also, Dequalinium chloride is active against the bacteria which cause bacterial vaginosis. Dequalinium Chloride (DECA) is a PKC inhibitor and high-affinity blocker CNGA1 channel, and nearly as effective on heteromeric CNGA1+CNGB1 channels. Common side effects are: vaginal discharge; vaginal itching or vaginal burning; vaginal yeast infection (thrush); tender tongue.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Watanidipine (AE0047) had been NDA filed for the treatment of hypertension in Japan. Watanidipine (as Calbren®) was awaiting registration with Mitsubishi Pharma Corporation in Japan. However, Mitsubishi Pharma Corporation has discontinued the development of this drug. Watanidipine had also been in phase II clinical trials for the treatment of stroke and preclinical trials for atherosclerosis. However, no recent development has been reported. Watanidipine (AE0047) has being shown to be a calcium antagonist with protective effects against cerebral ischaemia and the occurrence of stroke in several animal models.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
Pirmenol is an antiarrhythmic agent, which exhibits effects on the fast action potential similar to other class 1 membrane active antiarrhythmic agents. Pirmenol depresses not only the fast Na+ channel, but also others, such as the slow Ca2+ and K+ channels. Pirmenol had sevenfold lower affinity for glandular-type muscarinic receptors (M3) than for cardiac-type muscarinic receptors (M2). This medicine regulates disturbed pulse by acting on the cardiac muscle. Usually, used for treatment of tachyarrhythmia (ventricular). The most commonly reported adverse reactions include constipation, discomfort in stomach, difficulty in urination (urinary retention), headache, insomnia, bitterness in the mouth, nausea, dry mouth and palpitation. Lidocaine, procainamide and quinidine a greater degree of arrhythmia conversion occurred when dosed 15 min after pirmenol than when these agents were dosed alone.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Ipidacrine (Neiromidin) is a drug first synthesized by the National Research Center for Biologically Active Compounds in the Russian Federation. Neuromidin has a direct stimulating effect on the conduct of the pulse along the nerve fibers, interneuronal and neuromuscular synapses of the CNS and peripheral nervous system. Pharmacological action neuromidin is based on a combination of two mechanisms of action: blockade of potassium channels of the membrane of neurons and muscle cells; reversible inhibition of cholinesterase in synapses. Neuromidin enhances the effect on smooth muscle acetylcholine not only, but epinephrine, serotonin, histamine and oxytocin. It has the following pharmacological effects: - Improve and stimulate impulse conduction in the nervous system and neuromuscular transmission; - Enhances contractility of smooth muscle organs under the influence of acetylcholine agonists, adrenaline, serotonin, histamine and oxytocin receptors, with the exception of potassium chloride; - Improves memory, slows progressive course of dementia. In preclinical studies Neuromidin is not teratogenic, embryotoxic, mutagenic, carcinogenic and immunotoxic action, had no effect on the endocrine system
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Ipidacrine (Neiromidin) is a drug first synthesized by the National Research Center for Biologically Active Compounds in the Russian Federation. Neuromidin has a direct stimulating effect on the conduct of the pulse along the nerve fibers, interneuronal and neuromuscular synapses of the CNS and peripheral nervous system. Pharmacological action neuromidin is based on a combination of two mechanisms of action: blockade of potassium channels of the membrane of neurons and muscle cells; reversible inhibition of cholinesterase in synapses. Neuromidin enhances the effect on smooth muscle acetylcholine not only, but epinephrine, serotonin, histamine and oxytocin. It has the following pharmacological effects: - Improve and stimulate impulse conduction in the nervous system and neuromuscular transmission; - Enhances contractility of smooth muscle organs under the influence of acetylcholine agonists, adrenaline, serotonin, histamine and oxytocin receptors, with the exception of potassium chloride; - Improves memory, slows progressive course of dementia. In preclinical studies Neuromidin is not teratogenic, embryotoxic, mutagenic, carcinogenic and immunotoxic action, had no effect on the endocrine system