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

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Showing 1 - 10 of 22 results

Status:

Class (Stereo):
CHEMICAL (ACHIRAL)



Pimozide (Orap) is a diphenylbutylpiperidine that is effective as an antipsychotic agent and as an alternative to haloperidol for the suppression of vocal and motor tics in patients with Tourette syndrome. It is not intended as a treatment of first choice nor is it intended for the treatment of tics that are merely annoying or cosmetically troublesome. It should be reserved for use in Tourette’s Disorder patients whose development and/or daily life function is severely compromised by the presence of motor and phonic tics. Evidence supporting approval of pimozide for use in Tourette’s Disorder was obtained in two controlled clinical investigations, which enrolled patients between the ages of 8 and 53 years. Most subjects in the two trials were 12 or older. Pimozide is an orally active antipsychotic drug product, which shares with other antipsychotics the ability to blockade dopaminergic receptors on neurons in the central nervous system. Although its exact mode of action has not been established, the ability of pimozide to suppress motor and phonic tics in Tourette’s Disorder is thought to be a function of its dopaminergic blocking activity. However, receptor blockade is often accompanied by a series of secondary alterations in central dopamine metabolism and function which may contribute to both pimozide’s therapeutic and untoward effects. In addition, pimozide, in common with other antipsychotic drugs, has various effects on other central nervous system receptor systems which are not fully characterized.
Fluphenazine is a trifluoro-methyl phenothiazine derivative intended for the management of schizophrenia and other psychotic disorders. Fluphenazine has not been shown effective in the management of behaviorial complications in patients with mental retardation. Fluphenazine blocks postsynaptic mesolimbic dopaminergic D1 and D2 receptors in the brain; depresses the release of hypothalamic and hypophyseal hormones and is believed to depress the reticular activating system thus affecting basal metabolism, body temperature, wakefulness, vasomotor tone, and emesis.
Status:
First marketed in 1937
Source:
Oreton-F by Schering
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Testosterone is a steroid sex hormone found in both men and women. In men, testosterone is produced primarily by the Leydig (interstitial) cells of the testes when stimulated by luteinizing hormone (LH). It functions to stimulate spermatogenesis, promote physical and functional maturation of spermatozoa, maintain accessory organs of the male reproductive tract, support development of secondary sexual characteristics, stimulate growth and metabolism throughout the body and influence brain development by stimulating sexual behaviors and sexual drive. In women, testosterone is produced by the ovaries (25%), adrenals (25%) and via peripheral conversion from androstenedione (50%). Testerone in women functions to maintain libido and general wellbeing. Testosterone exerts a negative feedback mechanism on pituitary release of LH and follicle-stimulating hormone (FSH). Testosterone may be further converted to dihydrotestosterone or estradiol depending on the tissue. The effects of testosterone in humans and other vertebrates occur by way of two main mechanisms: by activation of the androgen receptor (directly or as DHT), and by conversion to estradiol and activation of certain estrogen receptors. Free testosterone (T) is transported into the cytoplasm of target tissue cells, where it can bind to the androgen receptor, or can be reduced to 5α-dihydrotestosterone (DHT) by the cytoplasmic enzyme 5α-reductase. DHT binds to the same androgen receptor even more strongly than T, so that its androgenic potency is about 2.5 times that of T. The T-receptor or DHT-receptor complex undergoes a structural change that allows it to move into the cell nucleus and bind directly to specific nucleotide sequences of the chromosomal DNA. The areas of binding are called hormone response elements (HREs), and influence transcriptional activity of certain genes, producing the androgen effects. Testosterone is used as hormone replacement or substitution of diminished or absent endogenous testosterone. Use in males: For management of congenital or acquired hypogonadism, hypogonadism associated with HIV infection, and male climacteric (andopause). Use in females: For palliative treatment of androgen-responsive, advanced, inoperable, metastatis (skeletal) carcinoma of the breast in women who are 1-5 years postmenopausal; testosterone esters may be used in combination with estrogens in the management of moderate to severe vasomotor symptoms associated with menopause in women who do not respond to adequately to estrogen therapy alone.
Status:
Investigational
Source:
INN:acoltremon [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



WS-12 is a cooling agent and potent TRPM8 agonist. It activates TRPM8 but not related TRP channels like TRPM3 and TRPV6. WS-12 seems to activate TRPM8 mediated cation currents by shifting the voltage dependence of the activation curves to the left toward more physiological membrane potentials. Highly selective TRPM8 activators may be useful for prostate cancer imaging and/or therapy and for therapy in chronic neuropathic pain states.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)

Conditions:

There is no much available information in the literature around nandrolone cyclohexanecarboxylate (brand name Nor-Durandron, Norlongandron). It is known, that this compound is a synthetic androgen and anabolic steroid, which belongs to the strong acting chemical compounds.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Nandrolone hexyloxyphenylpropionate (brand names Anador, Anadur, Anadurine) is a synthetic androgen and anabolic steroid is marketed in some countries. Nandrolone, in general, is more anabolic than testosterone and has a very low androgenic expression. It is reported to have an anabolic to androgenic ratio of 37:125. Typically, males would take a dosage range of 200-600mg/wk with higher doses sometimes found in more advanced users. This compound normally would not be recommended for women due to the virilization effects this compound may cause such as increased body hair, deepened voice. Anadur has a high affinity towards the androgen receptor while having a lower androgenic expression, it is usually not recommended to be taken without testosterone. Without a high androgenic expression and having a strong bond to the AR, side effects of low testosterone are possible such as the infamous "Deca-Dick" (impotence), lethargy, and low sex drive.
Status:
Possibly Marketed Outside US
Source:
Japan:Nandrolone Cyclohexylpropionate
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Nandrolone cyclohexylpropionate (a derivative of Nandrolone, which is approved by FDA) is an anabolic steroid. Nandrolone cyclohexylpropionate is reported as an ingredient of Sanabolicum in Austria. Sanabolicum is a rarely found version of the anabolic androgenic steroid nandrolone, with a CycloHexylPropionate ester. This modification makes nandrolone more anabolic (muscle building) and less androgenic. Nandrolone cyclohexylpropionate is an androgen receptor agonist.