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

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Showing 10041 - 10050 of 10251 results

Butamisole is an injectable imidazothiazoles anthelmintic. In dogs it is used for the treatment of infections with whipworms (Trichuris vulpis ), and the hookworm (Ancylostoma caninum ). Nicotinic acetylcholine receptor agonist. Acts as agonist at nicotinic Ach receptor of nematode à ganglionic stimulation causes sustained muscle contraction initially followed by depolarising neuro muscular blockade which in turn leads to spastic paralysis.
Status:
Possibly Marketed Outside US
Source:
CLOFEKTON by Yoshitomi Pharmaceutical Industries
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Clocapramine is a chlorinated derivative of carpipramine. The hydrochloride has been given orally in the treatment of schizophrenia. Clocapramine is an antagonist of the Dopamine D2 and Serotonine (5-HT2) receptors. It has been implicated in at least one strange death, including a suicide. It augments the paroxetine in the panic disorder treatment.
Status:
Possibly Marketed Outside US
Source:
Globacillin by Sjoberg, B.|Undheim, K.
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Azidocillin is a narrow-spectrum, semisynthetic penicillin derivative with antibacterial activity towards Grain-positive and Gram-negative microorganisms, including Haemophilus influenze, against which it is as effective as ampicillin. Azidocillin binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This interrupts bacterial cell wall synthesis and results in the weakening of the bacterial cell wall, eventually causing cell lysis. Azidocillin can be applied in the treatment of inflammation of upper airways, middle ear, sinuses, throat, larynx and palatine tonsils. The substance is excreted with urine in 50-70% in the unchan¬ged form. It binds to the blood plasma proteins in 84%, and its half-life period is 30 min. The side effects are similar as those of benzylpenicillin but occur less frequently.
Bupranolol is a non-selective beta blocker without intrinsic sympathomimetic activity (ISA), but with strong membrane stabilizing activity. Bupranolol competes with sympathomimetic neurotransmitters such as catecholamines for binding at beta(1)-adrenergic receptors in the heart, inhibiting sympathetic stimulation. This results in a reduction in resting heart rate, cardiac output, systolic and diastolic blood pressure, and reflex orthostatic hypotension. Ophthalmic Bupranolol is used for the management of glaucoma and oral Bupranolol is used for the management of cardiovascular disorders. S-Bupranolol has also being shown to have superior preclinical safety profile and great antinociceptive efficacy and should be considered as a unique b-AR compound to advance future clinical pain studies.
Status:
Possibly Marketed Outside US
Source:
Globacillin by Sjoberg, B.|Undheim, K.
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Azidocillin is a narrow-spectrum, semisynthetic penicillin derivative with antibacterial activity towards Grain-positive and Gram-negative microorganisms, including Haemophilus influenze, against which it is as effective as ampicillin. Azidocillin binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This interrupts bacterial cell wall synthesis and results in the weakening of the bacterial cell wall, eventually causing cell lysis. Azidocillin can be applied in the treatment of inflammation of upper airways, middle ear, sinuses, throat, larynx and palatine tonsils. The substance is excreted with urine in 50-70% in the unchan¬ged form. It binds to the blood plasma proteins in 84%, and its half-life period is 30 min. The side effects are similar as those of benzylpenicillin but occur less frequently.
Status:
Possibly Marketed Outside US
Source:
Unknown by Nippon Organon|Pfizer
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Lomerizine (INN) (also known as KB-2796) is a diphenylpiperazine class L-type and T-type calcium channel blocker with relatively selective CNS effects. Voltage dependent L-type Ca2+ channels play an important role Ca2+ influx. L-type calcium currents typically require a strong depolarization for activation and are long-lasting. The common pharmacological profile of L-type channels is determined by the α1 subunit, which forms the Ca2+ selective. Lomerizine was developed as a potential agent for the selective improvement of the ocular or cerebrovascular circulation with minimal adverse cardiovascular effects, and it is used as an anti- migraine drug. Lomerizine selectively relaxes smooth muscle cells by inhibiting L-type Ca2+ influx, thereby reducing tone and increasing blood flow in cerebral vessels. Lomerizine also shows neuroprotective effects against secondary degeneration resulting from injury in retinal ganglion cells. While some calcium-channel blockers, such as flunarizine, act on the dopaminergic system, lomerizine is ineffective in vivo at inhibiting the release of dopamine. However, it has been observed to weakly inhibit the binding of [3H]spiperone to D2 dopamine receptors in vitro. While researchers are unsure of the reason for this difference, one hypothesis is that the doses administered cannot reach a high enough concentration in the brain to affect D2 receptors.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)


Mitoguazone is a guanylhydrazone derivative with potential antineoplastic activity. Mitoguazone inhibits S-adenosyl-L-methionine decarboxylase (SAMD), an enzyme involved in the synthesis of polyamines, resulting in a decreased proliferation of tumor cells, antimitochondrial effects, and p53-independent apoptosis. In the 1960s the drug was investigated in clinical trials. Despite the responses in acute leukemia, chronic myelogenous leukemia, lymphoma, multiple myeloma, head and neck cancer, esophageal cancer and other types of cancer, the development of the drug was discontinued because of marked myelosuppression and mucositis. Using a weekly schedule of administration, mitoguazone had minimal toxicity and showed limited activity in patients with lymphoma, esophageal cancer, prostate cancer, and other types of tumors.
Status:
Possibly Marketed Outside US
Source:
Sulfabrom by English, J.P. et al.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Sulfabromomethazine is a long-acting derivative of sulfamezathine that is used in the poultry, swine and cattle industries for the treatment of coccidiosis and various bacterial infections. Single oral doses of the drug have been used to treat calf diphteria and pneumonia, metritis, foot root and septic mastitis in cattle with repeated dose 48 hors later sometimes required. Use of sulfabromomethazine during the last 3 months of pregnancy should be avoided. The compound is now rarely used.
Status:
Possibly Marketed Outside US
Source:
PANTOGAM by Ammo, T.|Sakai, T.|Aizawa, T.|Fujihira, E.|Naganuma, A.
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Hopantenic acid (homopantothenic acid) is a central nervous system depressant. Formulated as the calcium salt, it is used as a pharmaceutical drug in the Russian Federation under the brand name Pantogam. In Russia it is widely used to treat a variety of neurological, psychological and psychiatric conditions. The drug has been on the pharmaceutical market since 1979 and has been proven to be safe even for children from 3 years old upwards. Hopantenic acid is a natural forming substance, has some of the lowest side effects and considered to be very safe. Use Pantogam to treat a wide variety of cognitive and nervous system disorders with combined sedative and mild stimulant effect. Hopantenic acid is not approved for use in Europe or the United States. GABA receptor agonist.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)


Cloricromen a drug that inhibits platelet aggregation in man and in experimental thrombosis. Experiments on rodents have revealed that cloricromene which reduced tumor necrosis factor production, could be useful in the treatment of periodontitis. In addition, it could be potentially useful in ischemic-retinal diseases where amelioration of blood flow and inflammation is desirable. However, experiments with patients with cerebrovascular occlusive disease didn’t shown any effect of cloricromen on coagulative variables.

Showing 10041 - 10050 of 10251 results