U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 1 - 10 of 13 results


Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Isoflurane (1-chloro-2, 2,2-trifluoroethyl difluoromethyl ether) a nonflammable liquid administered by vaporizing, is a general inhalation anesthetic drug. Isoflurane is a clear, colorless, stable liquid containing no additives or chemical stabilizers. Similar to many general anesthetics, the exact mechanism of the action has not been clearly delineated. Isoflurane reduces pain sensitivity (analgesia) and relaxes muscles. Isoflurane likely potentiates GABA-A and glycine receptor activity, which decreases motor function, inhibits receptor activity in the NMDA glutamate receptor subtypes and binds to glutamate receptors. Isoflurane is always administered in conjunction with air and/or pure oxygen. Often nitrous oxide is also used. Although its physical properties imply that anesthesia can be induced more rapidly than with halothane, its pungency can irritate the respiratory system, negating this theoretical advantage conferred by its physical properties. It is usually used to maintain a state of general anesthesia that has been induced with another drug, such as thiopentone or propofol.
Status:
Investigational
Source:
INN:taltrimide [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Taltrimide, a taurine derivative that was developed as an anticonvulsive agent. Taltrimide strongly inhibits the sodium-independent binding of taurine to synaptic membranes of the brain and it does not appear to bind to GABAA and benzodiazepine receptor. The drug was studied in phase II clinical trial Finland as an anticonvulsant agent to treat epilepsy. However, the further development of this drug was discontinued.
Status:
Investigational
Source:
NCT02942017: Phase 3 Human clinical trial Completed Depression, Postpartum/psychology
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Eltanolone (pregnanolone) is an endogenous neuro active steroid that is biosynthesized from progesterone. It is a positive allosteric modulator of the GABAA receptor, as well as a negative allosteric modulator of the glycine receptor. There is strong evidence that it is involved in the pathophysiology of premenstrual syndrome, catamenial epilepsy, major depression, and stress-sensitive brain disorders and is known to have sedative, anxiolytic, anesthetic, and anticonvulsant effects. It was investigated for clinical use as a general (intravenous) anesthetic. It produced unwanted side effects such as convulsions on occasion, and for that reason was not marketed. Pregnanolone possesses neuroprotective and neurotrophic properties thus has been through a number of clinical trials including for treatment of traumatic brain injury (TBI), Alzheimer disease, cognitive impairment and fragile X-associated tremor/ataxia syndrome.
Enflurane (2-chloro-1,1,2,-trifluoroethyl-difluoromethyl ether) is a halogenated ether structural isomer of isoflurane. Developed by Ross Terrell in 1963, it was first used clinically in 1966. It was increasingly used for inhalational anesthesia during the 1970s and 1980s but is no longer in common use. Clinically, enflurane produces a dose-related depression of myocardial contractility with an associated decrease in myocardial oxygen consumption. Between 2% and 5% of the inhaled dose is oxidized in the liver, producing fluoride ions and difluoromethoxy-difluoroacetic acid. This is significantly higher than the metabolism of its structural isomer isoflurane. The exact mechanism of the action of general anesthetics has not been delineated. Enflurane acts as a positive allosteric modulator of the GABAA, glycine, and 5-HT3 receptors, and as a negative allosteric modulator of the AMPA, kainate, and NMDA receptors, as well as of nicotinic acetylcholine receptors.
Sarcosine, also known as N-methylglycine, is a metabolite of glycine. It shares properties with both glycine and D-serine, though its effects are weaker. Sarcosine supplementation can be used to alleviate symptoms of depression and schizophrenia, or improve cognition. It is absorbed more reliably by the body than D-serine, which can also treat similar conditions. Sarcosine is being investigated for its connection to prostate cancer. It may be a biomarker for prostate cancer, which means that if sarcosine levels in the blood are higher than normal, it could be an indicator of prostate cancer. This doesn’t mean that sarcosine itself causes cancer. More research is needed to confirm this relationship. Sarcosine’s main mechanism involves inhibiting a transporter, called GlyT1, which takes up glycine and D-serine into cells. This increases the levels of glycine and D-serine in the body and increases their effects. Sarcosine, a glycine transporter type 1 inhibitor and an N-methyl-D-aspartate (NMDA) receptor co-agonist at the glycine binding site, potentiates NMDA receptor function. Sarcosine is an inhibitory glycine receptor agonist.
Status:
Possibly Marketed Outside US
Source:
NCT02418130: Phase 4 Interventional Completed Fatigue
(2014)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Taurine is a semi-essential amino acid and is not incorporated into proteins. Taurine is considered conditionally essential because it cannot be synthesized by infants younger than 4-6 weeks, and it may not be adequately synthesized in patients receiving long-term parenteral nutrition and patients with short-term hypermetabolic conditions. In mammalian tissues, taurine is ubiquitous and is the most abundant free amino acid in the heart, retina, skeletal muscle, brain, and leukocytes. Taurin occurs naturally in fish and meat. The mean daily intake from omnivore diets was determined to be around 58 mg. Taurine is a component of energy drinks, with many contain 1000 mg per serving. In medicine, taurine supplementation demonstrated efficacy in relieving symptoms of heart failure, hepatitis, hypertension and psychotic disorder. Taurine exerts many physiological functions, including membrane stabilization, osmoregulation and cytoprotective effects, antioxidant and anti-inflammatory actions as well as modulation of intracellular calcium concentration and ion channel function. In addition taurine may control muscle metabolism and gene expression, through yet unclear mechanisms. The cellular and biochemical mechanisms mediating the actions of taurine are not fully known.
22,23-dihydro-avermectin B1a is a major form of Ivermectin mixture (more than 90%). It is a broad-spectrum anthelmintic (worms), microfilaricide (heartworms), and miticide (mites) drug, used for horses, cattle, pigs, household pets. Ivermectin used in humans, especially for river blindness. Ivermectin binds selectively and with high affinity to glutamate-gated chloride ion channels in invertebrate muscle and nerve cells of the microfilaria.
Sarcosine, also known as N-methylglycine, is a metabolite of glycine. It shares properties with both glycine and D-serine, though its effects are weaker. Sarcosine supplementation can be used to alleviate symptoms of depression and schizophrenia, or improve cognition. It is absorbed more reliably by the body than D-serine, which can also treat similar conditions. Sarcosine is being investigated for its connection to prostate cancer. It may be a biomarker for prostate cancer, which means that if sarcosine levels in the blood are higher than normal, it could be an indicator of prostate cancer. This doesn’t mean that sarcosine itself causes cancer. More research is needed to confirm this relationship. Sarcosine’s main mechanism involves inhibiting a transporter, called GlyT1, which takes up glycine and D-serine into cells. This increases the levels of glycine and D-serine in the body and increases their effects. Sarcosine, a glycine transporter type 1 inhibitor and an N-methyl-D-aspartate (NMDA) receptor co-agonist at the glycine binding site, potentiates NMDA receptor function. Sarcosine is an inhibitory glycine receptor agonist.
Sarcosine, also known as N-methylglycine, is a metabolite of glycine. It shares properties with both glycine and D-serine, though its effects are weaker. Sarcosine supplementation can be used to alleviate symptoms of depression and schizophrenia, or improve cognition. It is absorbed more reliably by the body than D-serine, which can also treat similar conditions. Sarcosine is being investigated for its connection to prostate cancer. It may be a biomarker for prostate cancer, which means that if sarcosine levels in the blood are higher than normal, it could be an indicator of prostate cancer. This doesn’t mean that sarcosine itself causes cancer. More research is needed to confirm this relationship. Sarcosine’s main mechanism involves inhibiting a transporter, called GlyT1, which takes up glycine and D-serine into cells. This increases the levels of glycine and D-serine in the body and increases their effects. Sarcosine, a glycine transporter type 1 inhibitor and an N-methyl-D-aspartate (NMDA) receptor co-agonist at the glycine binding site, potentiates NMDA receptor function. Sarcosine is an inhibitory glycine receptor agonist.
Status:
Possibly Marketed Outside US
Source:
NCT02418130: Phase 4 Interventional Completed Fatigue
(2014)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Taurine is a semi-essential amino acid and is not incorporated into proteins. Taurine is considered conditionally essential because it cannot be synthesized by infants younger than 4-6 weeks, and it may not be adequately synthesized in patients receiving long-term parenteral nutrition and patients with short-term hypermetabolic conditions. In mammalian tissues, taurine is ubiquitous and is the most abundant free amino acid in the heart, retina, skeletal muscle, brain, and leukocytes. Taurin occurs naturally in fish and meat. The mean daily intake from omnivore diets was determined to be around 58 mg. Taurine is a component of energy drinks, with many contain 1000 mg per serving. In medicine, taurine supplementation demonstrated efficacy in relieving symptoms of heart failure, hepatitis, hypertension and psychotic disorder. Taurine exerts many physiological functions, including membrane stabilization, osmoregulation and cytoprotective effects, antioxidant and anti-inflammatory actions as well as modulation of intracellular calcium concentration and ion channel function. In addition taurine may control muscle metabolism and gene expression, through yet unclear mechanisms. The cellular and biochemical mechanisms mediating the actions of taurine are not fully known.

Showing 1 - 10 of 13 results