Buy TH-030418 Cas-1374406-56-0
Buy TH-030418 Cas-1374406-56-0
TH-030418 is an extremely potent opioid related to thienorphine. TH-030418 carries about 5,000 times the potency of morphine.[1][2]
See also
- BU72
- Dihydroetorphine
- Etorphine (M99)
- M320
TH-030418: a potent long-acting opioid analgesic with low dependence liability
- PMID: 21594658
- DOI: 10.1007/s00210-011-0652-8
Abstract
Numerous efforts have been made on the chemical modification of opioid compounds, with the ultimate goal of developing new opioid analgesics that is highly potent and low/non-addictive. In a search for such compounds, TH-030418 [7α-[(R)-1-hydroxy-1-methyl-3-(thien-3-yl)-propyl]-6,14-endo-ethanotetrahydrooripavine] was synthesized. Here, we evaluated the pharmacological activities of TH-030418, in comparison with morphine, the prototype opioid analgesic. In radioligand binding assays, TH-030418 bound potently and nonselectively to μ-, δ-, κ-, and ORL1 (opioid receptor-like 1) receptors stably expressed in CHO (Chinese hamster ovary) cells with K (i) values of 0.56, 0.73, 0.60, and 1.55 nM, respectively. When administered subcutaneously, TH-030418 was much more potent than morphine in analgesia, with the ED(50) values of 1.37 μg/kg and 1.70 μg/kg in hot plate and acetic acid writhing tests, respectively. The opioid antagonist naloxone blocked the antinociceptive effect of TH-030418, indicating that the action of TH-030418 was mediated by opioid receptors. The antinociceptive effect of s.c. TH-030418 in hot plate test lasted for more than 12 h, which is much longer than those of morphine (2.5 h) and dihydroetorphine (1.5 h). In addition, naloxone did not precipitate withdrawal syndrome in the mice treated with TH-030418 previously. Most importantly, TH-030418 did not induce conditioned place preference in mice after chronic treatment. These results indicate that TH-030418 is a potent long-acting opioid analgesic with low dependence liability and may be of some value in the development of new analgesics.
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TH-030418: a potent long-acting opioid analgesic with low …
In radioligand binding assays, TH-030418 bound potently and nonselectively to μ-, δ-, κ-, and ORL1 (opioid receptor-like 1) receptors stably expressed in CHO (Chinese hamster ovary) cells with K (i) …
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TH-030418: a potent long-acting opioid analgesic with low dependence …
May 19, 2011 · In radioligand binding assays, TH-030418 bound potently and nonselectively to μ-, δ-, κ-, and ORL1 (opioid receptor-like 1) receptors stably expressed in CHO (Chinese hamster ovary) cells …
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TH-030418: A potent long-acting opioid analgesic with low …
Request PDF | TH-030418: A potent long-acting opioid analgesic with low dependence liability | Numerous efforts have been made on the chemical modification of opioid compounds, with …
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