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Bremazocine: a potent, long-acting opiate kappa-agonist.
It is suggested that morphine and bremazocine interact with different subpopulations of opiate receptors, and the actions of the antagonists naloxone and Mr 2266 suggest a preference for opiate kappa-receptors. Expand
Opiate antagonistic properties of an octapeptide somatostatin analog.
Electrophysiological data from hippocampal cultures and results from animal studies demonstrate the opiate antagonistic properties of SMS 201-995. Expand
A synthetic enkephalin analogue with prolonged parenteral and oral analgesic activity
The pharmacological properties of five synthetic pentapeptides structurally related to met-enkephalin are reported, two of which exhibit significant analgesic activity after oral administration and which are more potent analgesics administered parenterally than β-endorphin. Expand
Synthesis, Opiate Receptor Binding and Analgesic Activity of Enkephalin Analogues
The synthesis and biological testing of analogues of Met-enkephalin, a recently discovered opioid peptide from mammalian brain, are described. Testing involved determination of affinity constants forExpand
Unexpected opioid activity in a known class of drug.
Tifluadom is characterised as an opiate kappa-receptor agonist in vitro and in vivo with potent analgesic activity in animals and no dependence potential. Expand
Correlation between substance P content of primary sensory neurones and pain sensitivity in rats exposed to antibodies to nerve growth factor.
Results suggest that substance P-containing primary sensory neurones are involved in certain types of nociception. Expand
Lormetazepam (Lorámet®): A Multicentre Assessment of its Efficacy and Acceptability as a Hypnotic in Out-Patients with Sleep Disturbances
In an open, multicentre study, the short-acting benzodiazepine hypnotic lormetazepam (Loramet®) was administered nightly (1–2 mg p.o.) for a period of 7 nights to 665 out-patients with various typesExpand
Analgesic properties of the GABA-mimetic THIP.
The analgesic effects of THIP, baclofen and muscimol were not reversed by naloxone or bicuculline, and THIP was active orally and parenterally and resembled muscicimol qualitatively in its actions. Expand
Evidence for analgesic activity of enkephalin in the mouse
It is indicated that the two natural compounds induce analgesia in mice, whereas the two analogues are devoid of such activity. Expand