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

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Showing 81 - 90 of 186 results

Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Androstenol (5α-androst-16-en-3α-ol), a pheromone that acts as a potent positive allosteric modulator of the GABA-A receptor. Androstenol was first isolated from boar testes, and several animal experiments suggest that androstenol is capable of reducing anxiety, as well as hippocampal epileptogenic activity. It was subsequently detected in humans, (primarily in males), in sweat, urine, plasma, and saliva. Androstenol is also shown to affect hormonal, behavioral and social responses in humans. In animals, androstenol has been found to produce anxiolytic-like, antidepressant-like and anticonvulsant effects.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Pimpinellin is a furocoumarin and mevalonic acid derivative, that was isolated from Heracleum laciniatum and Toddalia asiatica. Pimpinellin, isopimpinellin and phellopterin are three major coumarins present in Toddalia asiatica extract which demonstrated activities like anticancer, vasodilative and antioxidant etc Pimpinellin is well known photoreactive compound and it is used in Brazil in some pharmaceutical and cosmetic products because of their UV-light absorbing properties
CX614 (2H,3H,6aH-pyrrolidino(2,1-3',2')1,3-oxazino(6',5'-5,4)benzo(e)1,4-dioxan-10-one) is a positive allosteric modulator of the AMPA receptor. Chronic treatment of rat hippocampal slices with CX614 gradually reduced levels of glutamate receptor (GluR)1 and GluR2/3 AMPA subunits and of their anchoring proteins synapse-associated protein 97 (SAP97) and glutamate receptor interacting protein 1 (GRIP1). The physiological and toxicological properties of this compound have not been evaluated in humans.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)



LY-450108 had been in phase I clinical trial by Lilly, where was shown, that this drug safe and well tolerated in healthy subjects. This drug in the preclinical studies on animal models for the treatment of depression and Parkinson's disease.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Tribromoethanol is a popular injectable anesthetic agent commonly used for embryo-transfer surgery for the generation of transgenic mice and sometimes rats. In humans and animals, Tribromoethanol produces a generalized CNS depression, including both the respiratory and cardiovascular centers. It undergoes conjugation with glucuronic acid during metabolism in the liver, followed by excretion in the urine as TBE glucuronate. Tribromoethanol causes rapid and deep anesthesia followed by rapid and full postoperative recovery, but the margin of safety between anesthetic and the lethal dose is narrow. Depression of respiration and circulation, together with its general unpredictability, eventually discouraged its use. Although Tribromoethanol solutions are often referred to as Avertin, this is a misnomer. Avertin was the trade name for Winthrop Laboratories’ proprietary Tribromoethanol formulation, which is no longer available. Marketing of pharmaceutical-grade Tribromoethanol took place under several proprietary names, including Avertin, Bromethol, Ethobrom, and Narkolan, each as a 66.7% (w/w) solution of Tribromoethanol in tertiary-amyl alcohol, wherein each milliliter contained 1 g of Tribromoethanol. Although pharmaceutical-grade TBE has not been commercially available or routinely used for human or veterinary anesthesia for several years, the agent has received widespread acceptance for use in the various manipulations required for the production of genetically engineered mice and rats. Tribromoethanol is an attractive anesthetic choice for many researchers because it is easy and inexpensive to make in the laboratory from readily available reagents, requires no special equipment for its administration, and is not subject to federal or state drug enforcement agency storage or accountability regulations. More importantly, the i.p. injection of TBE results in the simple and rapid induction of short-term surgical anesthesia sufficient for the vasectomy, embryo transfer, and tail amputation for Southern blot analysis—all necessary elements in the production of genetically engineered animals.
Status:
US Previously Marketed
First approved in 2019

Class (Stereo):
CHEMICAL (ABSOLUTE)



Allopregnanolone is a neurosteroid metabolite of progesterone. It is an allosteric modulator of inhibitory γ-aminobutyric acid (GABA-A) receptors on neural stem cells and other cell types in the brain. Allopregnanolone has effects similar to those of other positive allosteric modulators of the GABA action at GABAA receptor such as the benzodiazepines, including anxiolytic, sedative, and anticonvulsant activity. A solution of allopregnanolone, SAGE-547 is an intravenous allosteric modulator of both synaptic and extrasynaptic γ-aminobutyric acid type A (GABAA)receptors. It's believed that allopregnanolone is effective as an anticonvulsant when prolonged seizure activity has become resistant to benzodiazepine treatment. Under the names brexanolone and SAGE-547, allopregnanolone is under development by SAGE Therapeutics as an intravenously administered drug for the treatment of super-refractory status epilepticus, postpartum depression, and essential tremor. Allopregnanolone is in phase III trials for the treatment of super-refractory status epilepticus (SRSE) and postpartum depression.
Status:
US Previously Marketed
First approved in 1981

Class (Stereo):
CHEMICAL (ACHIRAL)



Halazepam is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. Halazepam is used to relieve anxiety, nervousness, and tension associated with anxiety disorders. Halazepam (Paxipam) is no longer commercially available in the United States. Common adverse effects are: hypotension, nausea, xerostomia, confusion, headache. Alcohol should be avoided while taking Paxipam as it causes drowsiness as well. Medications that also cause drowsiness should not be taken along with Paxipam. These include: Antidepressants, Pain relievers, Seizure medications, Muscle relaxants, Antihistamines, Sleeping pills and sedatives.