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

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Showing 1301 - 1310 of 2849 results

Dibenzepin is a tricyclic antidepressant of the dibenzo-epine group. It is a selective noradrenaline uptake inhibitor, which exhibits in vitro and in vivo imipramine-like effects. It binds strongly to histamine H1 receptors in the brain and, to a lesser extent, to cholinergic receptors. The pharmacological profile of dibenzepin corresponds widely to its biochemical properties: histamine antagonism, tetrabenazine antagonism, potentiation of various noradrenergic effects and anticholinergic effects. Dibenzepin is only available in European countries for the treatment of depression.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)


Metapramine is a tetracyclic antidepressant available in tablet and injectable form. It is claimed to have an antidepressant effect and is useful in all types of depression. Metapramine is a low-affinity antagonist of the NMDA receptor complex channel. Its acting as a norepinephrine reuptake inhibitor without affecting the reuptake of serotonin and dopamine. Quick acting, metapramine has a very interesting peculiarity: its large tolerance, which seems to be related to a no-anticholinergic effect. Metapramine could be indicated for correction of extra-pyramidal side effects induced by neuroleptics or observed in parkinsonism.
Status:
Possibly Marketed Outside US
Source:
Parmidin tablets 0,25 g by Anan, F.K.|Hosaki, S.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Parmidin (pyridinol carbamate) is a Soviet drug, has anti-arteriosclerotic (increased vascular resistance) activity, reduces the permeability of blood vessels, it helps to restore disturbed microcirculation in pathological processes. This is mainly due to the influence on kinin system, especially with a decrease in the activity of bradykinin receptors. It also reduces the aggregation of platelets. It’s used to treat: the brain vascular atherosclerosis, heart, limbs; diabetic retinopathy (non-inflammatory lesion of the retina associated with increased levels of sugar in the blood); thrombosis (violation of patency) retinal vein; occlusive disease (inflammation of the inner lining of arteries with a decrease in their lumen); trophic leg ulcers (slow-healing skin defects caused by malnutrition). Ointment is used in neurodermatitis (skin disease caused by disturbance of the central nervous system), Lichen sclerosus (teardrop scleroderma) genital organs of children, as well as a prophylactic and therapeutic agent against radiation skin lesions.
Status:
Possibly Marketed Outside US
Source:
NCT00272532: Phase 4 Interventional Completed Myofascial Pain Syndromes
(2005)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Thiocolchicoside is a muscle relaxant that has been authorised by national procedures in several EU Member States for use by mouth or injection into the muscles in the treatment of painful muscular disorders. Thiocolchicoside is marketed under the brand name Muscoril among others. Thiocolchicoside (TCC) is used clinically for its muscle relaxant, anti-inflammatory, and analgesic properties, and it has been shown to interact with gamma-aminobutyric acid (GABA) type A receptors (GABAARs) and strychnine-sensitive glycine receptors in the rat central nervous system.
Status:
Possibly Marketed Outside US

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
Source:
Zacopride hydrochloride by ZYF Pharm Chemical
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Zacopride is a potent antagonist at the 5-HT3 receptor and an agonist at the 5-HT4 receptor with antiemetic, anxiolytic and nootropic effects in animal models. Zacopride also has pro-respiratory effects, both reducing sleep apnea and reversing opioid-induced respiratory depression in animal studies. Zacopride has been tested in clinical trials for the treatment of schizophrenia but was found unsuccessful.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)


Fenpiverinium is a quaternary ammonium compound, it is an anticholinergic and antispasmodic agent. It is a constituent of Baralgin. The effects of the constituents of Baralgin (metamizole , fenpiverinium, and pitofenone ) on mechanical activity were studied in isolated human preparations of the upper urinary tract. Fenpiverinium blocked the increase in frequency of phasic-rhythmic contractions and the tonic tension development induced by acetylcholine. Fenpiverinium did influence neither spontaneous phasic activity nor activation by high potassium or norepinephrine. Fenpiverinium has exclusively anticholinergic properties. Fenpiverinium is a muscarinic acetylcholine receptor antagonist.
Status:
Possibly Marketed Outside US
Source:
Japan:Bevantolol Hydrochloride
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Bevantolol (INN) was a drug candidate for angina and hypertension that acted as both a beta blocker and a calcium channel blocker. Animal experiments confirm both agonist and antagonist effects on alpha-receptors, in addition to antagonist activity at beta-1 receptors. By binding and antagonizing beta-1 receptors Bevantolol inhibits the normal normal epinephrine-mediated sympathetic actions such as increased heart rate. This has the effect of decreasing preload and blood pressure. Bevantolol was discovered and developed by Warner-Lambert but in January 1989 the company announced that it had withdrawn the New Drug Application. As of 2016 it wasn't marketed in the US, UK, or Europe.
Ifenprodil (marketed under the brands Vadilex; Dilvax; Creocral; Cerocral) is a selective NMDA receptor (glutamate) antagonist. Additionally, ifenprodil inhibits GIRK channels, and interacts with alpha1 adrenergic, serotonin, and sigma receptors. Ifenprodil acts as a vasodilator. Ifenprodil is a medicine available in a number of countries worldwide, but not in US.
Benzilonium is an antispasmodic and antimuscarinic drug. Benzilonium bromide is a quarternary antimuscarinic agent with minimal passage of the blood-brain barrier.

Showing 1301 - 1310 of 2849 results