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

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Showing 34461 - 34470 of 34956 results

Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Batebulast (NCO-650) is an anti-allergic drug. It significantly inhibited both the initial and secondary increases in cAMP stimulated by antigen, anti-IgE and concanavalin A (Con A) in rat peritoneal mast cells. It strongly inhibited the incorporation of the 3H-methyl moiety into phospholipid by antigen, anti-IgE and Con A during histamine release. Batebulast significantly inhibited the compound 48/80-induced bronchoconstriction in dogs. Batebulast had no effect on the bronchoconstriction induced by inhalation of acetylcholine, suggesting that NCO-650 appears to have no anti-cholinergic effect and thus no effect on the vagal reflex that occurred during the asthmatic responses. NCO-650 may be useful for the treatment of bronchial asthma as an orally active drug. Batebulast has been in phase II clinical trials for the treatment of asthma in Japan. However, this research has been discontinued.
Status:
Possibly Marketed Outside US
Source:
Schmerz. Apr 2003;17(2):110-6.: Phase 4 Human clinical trial Completed Pain, Postoperative
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

TILIDINE is a low to medium potency opioid analgesic. It is metabolized to its active metabolites, nortilidine and bisnortilidine. Its analgesic activity is largely exerted through nortilidine which is a potent agonist at Mu opioid receptors.
Status:
Possibly Marketed Outside US
Source:
NCT02986685: Phase 4 Interventional Withdrawn Refractory Reflux Esophagitis
(2016)
Source URL:

Class (Stereo):
CHEMICAL (UNKNOWN)



Trimebutine [3,4,5-trimethoxybenzoic acid 2-(dimethylamino)-2-phenylbutylester] is a noncompetitive spasmolytic agent. The actions of trimebutine on the gastrointestinal tract are mediated via (i) an agonist effect on peripheral mu, kappa and delta opiate receptors and (ii) release of gastrointestinal peptides such as motilin and modulation of the release of other peptides, including vasoactive intestinal peptide, gastrin and glucagon. Trimebutine attenuated colonic motility mainly through the inhibition of L-type Ca(2+) channels at higher concentrations, whereas, at lower concentrations, it depolarized membrane potentials by reducing BK(ca) currents, resulting in the enhancement of the muscle contractions.Trimebutine accelerates gastric emptying, induces premature phase III of the migrating motor complex in the intestine and modulates the contractile activity of the colon. It is indicated for the treatment and relief of symptoms associated with the irritable bowel syndrome (spastic colon); and in postoperative paralytic ileus in order to accelerate the resumption of the intestinal transit following abdominal surgery.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)

Proxibarbal is a non-sedative barbiturate with a specific anti-serotonin and anti-histamine effect, due to enzyme induction of serotoninase and histaminase. Its lack of unpleasant side-effects. Proxibarbal exists in ring-chain tautomeric equilibrium with the two diastereomers of valofan. Proxibarbal is metabolized to a five-membered lactone. Its only barbituric property is its ability to induce enzymes that destroy a surplus of neurohormones and rid people of their neurovegetative sufferings, including migraine and other types of vascular headache. Side effects are: dizziness, drowsiness, dyspepsia, allergic reactions. Proxibarbal enhances the effects of other depriving agents, including alcohol.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)


Cycloguanil is a dihydrofolate reductase inhibitor and is a metabolite of the antimalarial drug proguanil. The parent drug proguanil was suggested to contribute to the antimalarial activity as well, but the mechanism of action is unknown. Proguanil is a prodrug that is metabolized to its main active metabolite, cycloguanil, mostly via CYP2C19. There is significant variation in proguanil pharmacokinetics.12 CYP2C19 is the predominant enzyme catalyzing the bioactivation of proguanil to cycloguanil. Cycloguanil is one of the few antimalarial drugs that act on both the erythrocytic and on the pre-erythrocytic (hepatic) forms of the malaria parasites. Although cycloguanil is not currently in general use as an antimalarial, the continuing development of resistance to current antimalarial drugs has led to renewed interest in studying the use of cycloguanil in combination with other drugs.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Difemerine is antimuscarinic agent. It is used in the symptomatic treatment of visceral spasms. It may have anticholinergic side effects like dry mouth, dizziness, blurred vision and drowsiness. Anticholinergics must be used with caution in glaucoma and prostate hypertrophy patients.
Status:
Possibly Marketed Outside US
Source:
Schmerz. Apr 2003;17(2):110-6.: Phase 4 Human clinical trial Completed Pain, Postoperative
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

TILIDINE is a low to medium potency opioid analgesic. It is metabolized to its active metabolites, nortilidine and bisnortilidine. Its analgesic activity is largely exerted through nortilidine which is a potent agonist at Mu opioid receptors.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)


Butibufen is a non-steroidal anti-inflammatory cyclooxygenase inhibitor with analgesic and antipyretic properties. The drug was investigated for the treatment of osteoarthritis, rheumatoid artritis, and other arthroses. It was marketed under tradenames Mijal and Butilopan but now is withdrawn from the market.
Status:
Possibly Marketed Outside US
Source:
Japan:Pipemidic Acid Trihydrate
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Pipemidic Acid is a quinolone antibacterial agent. It’s used in the treatment of urinary tract infections, recidive cystitis, prolongation of the therapy of pyelonephritis (prolonged therapy at patients with tendency to recidives. It belongs to DNA Gyrase inhibitor pharmacological group on the basis of mechanism of action and also classified in Antibacterial pharmacological group. Pipemidic acid is contraindicated at conditions of proved hypersensitivity, severe renal and hepatic insufficiency, cirrhosis of the liver, porphyria, diseases of the central nervous system (epilepsy and neurological conditions with low level for convulsions). Pipemidic acid is contraindicated at children and adolescents at growing phase.
Status:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Cholinergic anthelmintic, Thenium is used against dog and cat hookworms.

Showing 34461 - 34470 of 34956 results