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

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Showing 12471 - 12480 of 12951 results

Ormeloxifene (also known as centchroman) is a selective estrogen receptor modulator. It is a once-a-week non-steroidal oral contraceptive agent marketed in India and other countries under the brand names Novex-DS, Centron, and Sevista. Ormeloxifene has been investigated in the management of benign breast diseases such as mastalgia. The l-isomer, levormeloxifene, which has oestrogenic effects, has been investigated in the management of postmenopausal osteoporosis, but development appears to have been discontinued because of adverse effects. Recent studies have shown Ormeloxifene`s potent anti-cancer activities in breast, head and neck, and chronic myeloid leukemia cells. Several in vivo and clinical studies have reported that ormeloxifene possesses an excellent therapeutic index and has been well-tolerated, without any haematological, biochemical or histopathological toxicity, even with chronic administration. In India, ormeloxifene has been available as birth control since the early 1990s, and it is currently marketed there under the trade name Saheli. Ormeloxifene has also been licensed under the trade names Centron and Sevista. Ormeloxifene acts on oestrogen receptors. It has a weak estrogenic and potent antiestrogenic actions. It is expected to exert a contraceptive effect and normalise the bleeding from uterine cavity by regularising the expression of oestrogen receptors on the endometrium. As a contraceptive, it prevents proliferation and decidualisation of the endometrium, enhances blastocyst formation and slightly increases embryo transport through the oviducts.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)

Guanazodine is a new antihypertensive drug. Guanazodine caused a sustained decrease in the systemic blood pressure of spontaneously hypertensive rats, renal hypertensive dogs and normal cats. No tachyphylaxis developed when the drug was administered orally. The heart rate decreased. Guanazodine relaxed the cat nictitating membrane, attenuated the positive chronotropic response to sympathetic nerve stimulation in anesthetized dogs and in isolated rabbit aorta to transmural electrical stimulation. Guanazodine potentiated the pressor response to noradrenaline but attenuated the response to tyramine in anesthetized cats. It may be concluded that the hypotensive effect of guanazodine is related to adrenergic neuron blocking action, the noradrenaline-depleting action in peripheral tissues is similar to the effect of guanethidine and bethanidine. However, this drug is less potent than guanethidine. Toxicity and side effects appear to be less with guanazodine than with guanethidine and bethanidine.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)



Acedoben (4-acetamidobenzoic acid) is a benzoic acid derivative and a metabolite of benzocaine. It is a component of immunomodulatory drug inosine pranobex, which is used to treat mucocutaneous infections due to herpes simplex virus (type 1 and/or type II), genital warts as adjunctive therapy to podophyllin or carbon dioxide laser, and subacute sclerosing panencephalitis.
Status:
Possibly Marketed Outside US
Source:
CAMTOBELL by Chong Kun Dang Research Institute
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Belotecan is a semisynthetic analogue of camptothecin containing a 2-(N-isopropylamino) ethyl group linkage at position C-7 of the camptothecin ring. It stabilizes the complex formed between topoisomerase I and DNA, thereby preventing the religation of DNA breaks. This leads to an inhibition of DNA replication and triggers apoptotic cell death. Belotecan was approved in Korea under the name Camtobell for the treatment of patients with ovarian and small cell lung cancers.
Dimebon (latrepirdine) is an orally available, small molecule, gamma carboline derivative that was developed and used in Russia as an over-the-counter oral antihistamine for allergy treatment since 1980s. In 1990s it was shown that Dimebon has promising potential in treating neurodegenerative diseases. In 2003, Medivation Inc acquired the rights to Dimebon. Medivation went public in December 2004, with Dimebon as the only drug in its pipeline. The product was being developed by Medivation and Pfizer as a treatment for early-stage Alzheimer's disease and Huntington's disease. However, development was discontinued by Medivation and Pfizer in early 2012. Dimebon inhibits alpha-Adrenergic receptors (alpha1A, alpha1B, alpha1D, and alpha2A), Histamine H1 and H2 receptors and Serotonin 5-HT2c, 5-HT5A, 5-HT6 receptors with high affinity. Dimebon may act by blocking NMDA receptors or voltage-gated Ca2+ channels and by preventing mitochondrial permeability pore transition.
Status:
Possibly Marketed Outside US
Source:
Japan:Dimethylaminoethyl Reserpilinate Dihydrochloride
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Conditions:

Dimethylaminoethyl reserpilinate is reserpilinate derivative with hypotensive activity. Given subcutaneously to rats in doses 200 mg/kg dimethylaminoethane reserpilinate increased very slightly the gastric motility but showed no ulcerogenic effect.
Status:
Possibly Marketed Outside US
Source:
Japan:Diponium Bromide
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Diponium bromide ((2-[alpha,alpha-dicyclopentylacetoxy)- ethyl] triethylammonium bromide) is a muscarinic cholinergic receptor antagonist. It exerts antispasmodic action.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Tedisamil is an antiarrhythmic with additional anti-ischaemic properties, which acts via potassium channel blockade. This drug can be categorised as a class III antiarrhythmic agent due to its effects of action potential and QT interval prolongation in these patients. Although tedisamil has been shown to be an effective anti-ischaemic agent, with Phase III trials for angina pectoris now completed, the company are now pursuing the use of tedisamil for the treatment of atrial fibrillation, for which tedisamil is still in Phase II/III clinical trials. The FDA’s Cardiovascular and Renal Drugs Advisory Committee voted not to recommend approval for Solvay Pharmaceuticals’ investigational anti-arrhythmic drug Pulzium (Tedisamil) and asked the company to give the FDA more information.
Timepidium bromide is a quaternary ammonium antimuscarinic used for the symptomatic treatment of visceral spasms. It is a muscarinic antagonist.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)


Obidoxime is an antidote for organophosphorous nerve agent poisoning including chlorosarin, cyclosarin (GF), R-33 (VR), R-VX, sarin (GB), tabun (GA), VX, chlorosoman, soman (GD), and organophosphorous pesticides. It acts as an acetylcholinesterase (AChE) reactivator. In combination with atropine obidoxime can be used to treat super toxic organophosphate poisoning by relieving the symptoms of skeletal neuromuscular blocking that occurs during a cholinergic crisis.

Showing 12471 - 12480 of 12951 results