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

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Showing 391 - 400 of 408 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
Source:
Japan:Brovincamine Fumarate
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Brovincamine also known as brovincamine fumarate (BV, Sabromin) was used in Japan mainly as an improver of cerebral circulation and metabolism, and also as an inhibitor of the aggregation of platelets through the cyclic AMP pathway in patients with normal tension glaucoma. Brovincamine exerts its action via calcium channels blockade. The current drug status is unknown.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Xamoterol (ICI 118,587) is a partial agonist of beta1-adrenoceptors. Xamoterol acts on the cardiac beta 1-adrenergic receptor, modifies the response of the heart to variations in sympathetic activity. At rest, it produces modest improvements in cardiac contractility, relaxation, and filling without increase in myocardial oxygen demand. The improvements are maintained during exercise although the attendant tachycardia is attenuated. The beneficial effects of xamoterol on both systolic and diastolic function suggested that it would be effective in patients with mild-to-moderate heart failure, and this was demonstrated in small placebo-controlled studies where effort tolerance and symptoms were improved. Xamoterol produced improvements in exercise capacity, clinical signs, symptoms and quality of life with a low incidence of adverse experiences. Xamoterol is effective as monotherapy in heart failure.
Status:
Possibly Marketed Outside US
Source:
Rupall by Pediapharm Inc [Canada]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Rupatadine is characterised as a non-sedating H1 anti-histamine and platelet-activating factor (PAF) receptor antagonist. Rupatadine is indicated for the treatment of allergic rhinitis and urticaria. Rupatadine is a safe and well tolerated drug in patients over 2 years old, with no central nervous system or cardiovascular effects and it can be taken with or without foods.
Status:
Possibly Marketed Outside US
Source:
Oldagen by Purissimus [Argentina]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Homofenazine (or Pasaden) is a psycho sedative drug, developed in Germany.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)

Propiram is an orally administered analgesic with partial morphine-like agonist and weak antagonist properties. Analgesic efficacy of propiram, usually 50 or 100mg, appears comparable to that of standard dosages of other oral opioid drugs [i.e. pentazocine, pethidine (meperidine)] in patients with acute pain of moderate to severe intensity arising from various gynaecological and surgical procedures, and may be superior to codeine in gynaecological and postoperative dental pain. Propiram is a non-addictive analgesic for the relief of moderate-to-severe pain. Propiram reached Phase III clinical trials in the United States and Canada, but was discontinued. Propiram is a partial opioid mu receptor agonist.
Status:
Possibly Marketed Outside US
Source:
NCT01744236: Phase 4 Interventional Completed Type 2 Diabetes
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Tilarginine is L-N-monomethyl arginine (L -NMMA), a non-selective inhibitor of nitric oxide synthase (NOS), which has been studied in the treatment of septic shock and cardiogenic shock complicating myocardial infarction. Despite strong evidence that excessive nitric oxide (NO) production plays a pivotal role in the pathogenesis of septic shock and may contribute to the pathogenesis of cardiogenic shock complicating myocardial infarction, outcome studies in these two disorders have proved disappointing. Tilarginine therapy was associated with an excess mortality, particularly at doses > 5 mg/(kg h), in septic shock, whereas the effects of a lower dose (1 mg/(kg h)) in cardiogenic shock complicating myocardial infarction were neutral. The excess mortality in patients with septic shock was almost certainly the result of unfavorable hemodynamic changes induced by Tilarginine (decreased cardiac output, increased pulmonary vascular resistance and reduced tissue oxygen delivery) whereas the lack of benefit in patients with cardiogenic shock complicating myocardial infarction may have been because the dose of Tilarginine was too low.
Status:
Possibly Marketed Outside US
Source:
Japan:Bopindolol Malonate
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Bopindolol (4-[benzoyloxy-3-tertbutylaminopropoxy]-2-methylindole hydrogen malonate) is an indole beta-adrenoceptor antagonist bearing a benzoyl ester residue on the beta-carbon atom of the propanolamine side chain. Bopindolol is metabolized by esterase to benzoic acid and an active metabolite, 18-502 [4-(3-t-butylamino-2-hydroxypropoxy)-2-methyl indole], which is further metabolized to 20-785 [4-(3-t-butylaminopropoxy)-2-carboxyl indole]. Bopindolol produces sustained blockade of beta 1- and beta 2-adrenoceptors, has intrinsic sympathomimetic as well as membrane stabilizing actions, inhibits renin secretion, and interacts with 5-HT receptors. Bopindolol is used in the treatment of hypertension. In limited trials bopindolol has also successfully reduced symptoms in patients with angina pectoris, anxiety and essential tremor.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)


Bencyclane, a cycloheptane, is a vasodilator, antiplasmodic and a platelet aggregation inhibitor found to be effective in a variety of peripheral circulation disorders. Bencyclane has various other potentially useful pharmacological effects such as smooth muscle relaxation. Under the trade name Halidor it is used in several European countries to treat the symptoms of atherosclerosis, occlusive arterial disease. Its mechanism may involve block of calcium channels. However as was shown in vitro it does not act by a direct influence on the Ca2+ pumps of vascular smooth muscle cells. In in vitro biochemical assays related to smooth muscle excitation-contraction coupling, binding to beta 1-, beta 2-, and alpha-adrenergic receptors, inhibition of phosphodiesterase activity, and antagonism of calcium accumulation bencyclane bound to alpha- and beta-receptors. Bencyclane appeared to be a promising anti-sickling agent that can be used orally in sickle cell anaemia (SCD).
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

Azaloxan is an antidepressant drug, developed in the 1980s but never marketed.

Showing 391 - 400 of 408 results