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

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Showing 61 - 70 of 190 results

Status:
Investigational
Source:
INN:amoxecaine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

AMOXECAINE is an local anaesthetic.
Status:
Investigational
Source:
INN:pincainide
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Pincainide is a new beta-amino anilide with local anesthetic properties. It has been shown to be 3 times more potent than lidocaine as a local anaesthetic on desheathed frog sciatic nerve. It was found to be effective against arrhythmias induced in guinea-pigs by ouabain infusion or by administration of adrenaline and chloroform. Pincainide not only inhibited the influx of Ca 2+ and increased 45Ca efflux, thus reducing the contractile responses induced in rat aorta by noradrenaline and high K +, but it also inhibited other effects related to the noradrenaline-induced release of intracellular Ca 2+ stores. Further studies, however, must be performed in experimental models of arrhythmias before the effectiveness of pincainide as an antiarrhythmic drug can be established.
Status:
Investigational
Source:
NCT02942017: Phase 3 Human clinical trial Completed Depression, Postpartum/psychology
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Eltanolone (pregnanolone) is an endogenous neuro active steroid that is biosynthesized from progesterone. It is a positive allosteric modulator of the GABAA receptor, as well as a negative allosteric modulator of the glycine receptor. There is strong evidence that it is involved in the pathophysiology of premenstrual syndrome, catamenial epilepsy, major depression, and stress-sensitive brain disorders and is known to have sedative, anxiolytic, anesthetic, and anticonvulsant effects. It was investigated for clinical use as a general (intravenous) anesthetic. It produced unwanted side effects such as convulsions on occasion, and for that reason was not marketed. Pregnanolone possesses neuroprotective and neurotrophic properties thus has been through a number of clinical trials including for treatment of traumatic brain injury (TBI), Alzheimer disease, cognitive impairment and fragile X-associated tremor/ataxia syndrome.
Status:
Investigational
Source:
INN:aptocaine
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Aptocaine (Pirothesin, Pharmaceutical Manufacturing Company) is a new local anaesthetic agent, the first of note to be synthesized in Britain. It is related toprilocaine; like prilocaine, it has a low sub-cutaneous toxicity, but preliminary studies suggest that, unlike prilocaine, it does not induce methaemoglobinaemia. It has been found to produce satisfactory analgesia, of longer duration than lignocaine, by several routes, at a concentration of 3% in animals.
Status:
Investigational
Source:
INN:gavestinel [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



GV 150526A (gavestinel) is an investigational drug for a neuroprotective therapy of acute ischemic stroke within 6 hours of symptom onset. It is a potent and selective non-competitive antagonist at the glycine site of the N-methyl-D-aspartate receptor (NMDA) which reduces infarct volume in experimental stroke models. Gavestinel acts at the strychnine-insensitive glycine binding site of the NMDA receptor-channel complex with nanomolar affinity (pKi = 8.5), coupled with high glutamate receptor selectivity. Gavestinel displays higher than 1000-fold selectivity over NMDA, AMPA and kainate binding sites and is orally bioavailable and active in vivo. GV 150526A inhibited convulsions induced by NMDA in mice, when administered by both IV and po routes (ED50 = 0.06 and 6 mg/kg, respectively). The safety and efficacy of GV150526 were studied in two phase III randomized placebo-controlled clinical trials of acute ischemic stroke patients within 6 h from onset [The Glycine Antagonist in Neuroprotection (GAIN) International and GAIN Americas Trials] sponsored by GlaxoSmithKline. The results of these trials suggested that gavestinel was not of substantial benefit or harm to patients with primary intracerebral hemorrhage.
Status:
Investigational
Source:
INN:risocaine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

There is no information in the scientific papers related to the biological properties of risocaine (also known as n-propyl 4-aminobenzoate). However, exists mention, that it is used as a local anesthetic.
Status:
Investigational
Source:
INN:diamocaine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Diamocaine is the local anesthetic.
Status:
Investigational
Source:
INN:etoxadrol [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Etoxadrol is an NMDA receptor antagonist. It exerts phencyclidine-like properties. Etoxadrol has anticonvulsant and anesthetic activity. Intravenous etoxadrol was clinically tested as an anesthetic.
Status:
Other

Class (Stereo):
CHEMICAL (MIXED)

Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)