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

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Showing 6661 - 6670 of 167129 results

Status:
Investigational
Source:
INN:ceftiolene
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Ceftiolene (42980RP) is a new cephalosporin with a broad antibacterial spectrum similar to cefotaxime or ceftriaxone. The affinities of ceftiolene for penicillin-binding proteins are very comparable with those of ceftriaxone and cefotaxime for Escherichia coli, and generally greater than those of latamoxef (moxalactam) for the higher molecular weight PBPs of E. coli. Enterobacter cloacae. The affinity of ceftiolene for PBP1 of Staphylococcus aureus is greater than those of cefotaxime or latamoxef but comparable with these antibiotics for PBP3. The bacteriolytic activity of ceftiolene at defined concentrations against Gram-negative organisms is similar to that of ceftriaxone and significantly better than that of the other third-generation cephalosporins tested.
Status:
Investigational
Source:
INN:cinepaxadil
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Cinepaxadil is cinnamoyl-piperazine derivative developed by Delalande SA for treatment cardiovascular system disorders. Cinepaxadil decrease dogs cardiac activity after i.v. administration.
Status:
Investigational
Source:
INN:carprazidil
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Carprazidil is oxadiazolopyrimidine derivative patented by pharmaceutical company Hoffmann-La Roche as a direct vasodilator and potent antihypertensive agent. In clinical trials, Carprazidil was evaluated in patients with moderate to severe arterial hypertension. Following the addition of Carprazidil to pre-existing therapy with diuretics and beta-blockers or sympatholytics, blood pressure in most of the patients was normalized within one month. Heart rate was only slightly increased. Orthostatic hypotension was not observed. Weight gain or oedema formation occurred in 14 patients within the first four weeks, but could be controlled satisfactorily by intensified diuretic therapy. After a mean duration of treatment of 2.8 months, plasma volume and plasma and urine sodium were unaltered, and plasma potassium was slightly decreased. Plasma renin activity was doubled, whereas plasma aldosterone concentrations were unaltered. No adverse side effects on hematological parameters, liver or renal function were observed, nor was antinuclear antibody detected.
Status:
Investigational
Source:
INN:carpindolol
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Caprindolol, also known as SDZ 21009, is a beta-adrenoceptor blocker with affinity for serotonin (5-HT1A and 5-HT1B receptors.
Status:
Investigational
Source:
INN:carebastine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Carabestine is the active first-pass metabolite of Ebastine and acts as a histamine H1 receptor antagonist which has been investigated as a potential allergy medication. Ebastine is marketed under a number of brand names.
Status:
Investigational
Source:
INN:carmetizide
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Carmetizide is benzothiadiazine derivative patented by pharmaceutical company Abbott Laboratories as a diuretic. In preclinical studies, Carmetizide demonstrates perfect safety profile. Administration of Carmetizide (10,000 mg/kg, orally or 5000 mg/kg, s.c. or i.p.) to rats had no toxic effect. Carmetizide had no effect on the central nervous system and the cardiovascular system of guinea pigs or on the heart-lung preparation of dogs. These drugs did not affect the body temperature of rats and the blood coagulation of rabbits. Carmetizide had no effect on the spontaneous movement of smooth muscles.
Status:
Investigational
Source:
INN:dicarfen [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Dicarfen hydrochloride is a spasmolytic agent, local anesthetic and antiparkinsonian agent.
Status:
Investigational
Source:
INN:dibemethine [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Dibemethine is an analgesic agent.
Status:
Investigational
Source:
INN:properidine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Properidine is an isopropyl analog of pethidine that acts as opioid analgesic.
Status:
Investigational
Source:
INN:aminoquinol
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Aminoquinol (XIB4035) is a nonpeptidyl small molecule agonist for GFRalpha-1. XIB4035 concentration-dependently inhibited [(125)I]GDNF binding in Neuro-2A cells with an IC(50) of 10.4 uM. GDNF induced autophosphorylation of Ret protein, and promoted neurite outgrowth in Neuro-2A cells. XIB4035, like GDNF, induced Ret autophosphorylation in the Neuro-2A cells. Moreover, XIB4035 promoted neurite outgrowth in a concentration-dependent manner. These results show that XIB4035 may act as an agonist at GFRalpha-1 receptor complex, and mimic neurotrophic effects of GDNF in Neuro-2A cells. It has been shown that topical application of XIB4035 is an effective treatment for small-fiber neuropathy (SFN). Topical application of GFRα/RET receptor signaling modulators may be a unique therapy for SFN, and XIB4035 is a candidate therapeutic agent. Aminoquinol has been also used in the therapy of cutaneous leishmaniasis and lambliasis.

Showing 6661 - 6670 of 167129 results