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

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Showing 11 - 20 of 157 results

Status:
Investigational
Source:
INN:morphine glucuronide [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Morphine-6-glucuronide is a pharmacologically active metabolite of morphine that is being developed by CeNeS Pharmaceuticals as an alternative to morphine for the management of postoperative pain. Compared to morphine, Morphine-6-glucuronide has been reported to have6 and 86 times lower affinity for the human mu and kappa opioid receptors, respectively, and similar affinity for the delta opioid receptor. Morphine-6-glucuronide is was studied in phase III clinical trials for postoperative pain management. Unfortunately, Morphine-6-glucuronide failed to demonstrate superior safety compared to Morphine and further development was discontinued. Morphine-6-glucuronide accumulates after administration of morphine to patients with renal insufficiency, and analgesia can be obtained with lower doses of morphine compared to patients with normal renal function. More importantly, the dose should be reduced to avoid serious side-effects, although the simulations in this review did not account for side-effects.
Status:
Investigational
Source:
INN:methyldesorphine
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Methyldesorphine is a synthetic narcotic analgesic derived from morphine. It has no medicinal value in the US. This compound is listed as a Schedule I Narcotic controlled substance under the Controlled Substances Act 1970.
Status:
Investigational
Source:
INN:diprenorphine
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

As a narcotic antagonist similar in action to naloxone, DIPRENORPHINE is used to remobilize animals after analgesia by super-potent opioid analgesics such as etorphine and carfentanil. It is not used in humans. Diprenorphine binds approximately equally to the three subtypes of opioid receptors (mu, delta, and kappa) and antagonizes them. This compound belongs to the class of organic compounds known as phenanthrenes and derivatives. These are polycyclic compounds containing a phenanthrene moiety, which is a tricyclic aromatic compound with three non-linearly fused benzene. The therapeutic efficacy of many other compounds can be decreased when used in combination with Diprenorphine (54 compounds mentioned on www.drugbank.ca).
Status:
Investigational
Source:
INN:codoxime [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Codoxime is a synthetic derivative of an opiate dihydrocodeinone. It differs from dihydrocodeinone by the substitution of a carboxymethyl oxime for the ketonic oxygen at carbon 6 of the dihydrocodeinone molecule. Codoxime has been proposed as an antitussive with prolonged duration of action. In a clinical trial conducted on prisoner volunteers in 1966, it was found that codoxime has a capacity to produce physical dependence of the morphine type.
Status:
Investigational
Source:
INN:desmetramadol [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

O-Desmethyl tramadol (O-Desmethyltramadol, O-DSMT) is a metabolite of tramadol. O-Desmethyltramadol is an opioid analgesic and the main active metabolite of tramadol. (+)-O-Desmethyltramadol is the most important metabolite of tramadol produced in the liver after tramadol is consumed. This metabolite is considerably more potent as a μ-opioid agonist than the parent compound. O-desmethyl tramadol, inhibits 5-hydroxytryptamine type 2C receptors expressed in xenopus oocytes. O-desmethyl tramadol inhibits functions of M(1) receptors but has little effect on those of M(3) receptors. O-desmethyl tramadol has been widely used clinically and has analgesic activity.
Status:
Investigational
Source:
NCT01161069: Phase 1 Interventional Completed Healthy
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Status:
Investigational
Source:
NCT01740609: Phase 1 Interventional Completed Healthy
(2012)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Parafluorofentanyl is a selective mu-opioid agonist, an analog of fentanyl, developed by Janssen. The drug was not developed for human use but is produced and abused illegally.
Status:
Investigational
Source:
INN:bremazocine
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Bremazocine, a kappa-opioid agonist has limited potential as a clinical analgesic, however, possesses a possible utility for the therapy of alcohol and drug addiction. It was shown that bremazocine-like drugs could lower intraocular pressure and to minimize ischemic damage, that could be used in the therapy of glaucoma and cardiovascular disease.
Status:
Investigational
Source:
INN:methyldihydromorphine
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Methyldihydromorphine is a synthetic narcotic analgesic related to the morphine. This compound has no pharmaceutical value in the US.
Status:
Investigational
Source:
INN:norcodeine [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Norcodeine is the N-demethylated derivative of codeine. It has relatively little opioid activity in its own right, but is formed as a metabolite of codeine following ingestion. Codeine and its other major metabolites codeine-6-glucuronide and norcodeine have weak affinity to opioid μ-receptors.

Showing 11 - 20 of 157 results