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Opioids Opioids -- Thiambutene Synthetics

Nicomorphinist

Bluelighter
Joined
Apr 18, 2019
Messages
1,401
I wonder what else is known about these:

Also known as thienyl derivatives, these are sometimes considered Open-Chain Opioids and therefore distant relatives of everything from methadone to fentanyl to dextropropoxyphene, but are often given their own family. These were developed mainly at Burroughs-Wellcome in the United Kingdom starting in 1947 I believe it was and the major ones developed were Diethylthiambutene, Dimethylthiambutene, and Ethylmethylthiambutene. The first two are a potent as morphine, the latter 30 per cent stronger.

These three are used particularly in East Asian countries as veterinary opioids and there was something I read about a therapeutic index which was narrower than that of methadone, levorphanol, or the opiates in humans, leading to them being used only for critters. A fourth member of the family, tipepidine, is an over the counter antitussive available in the region which I guess one could say is the codeine of the family in that respect. They all have prominent anticholinergic effects. The Japanese trade names for the veterinary analgesics are Themalon (DETB) and Takaton (DMTB) and Emethibutin (EMTB) amongst others. They are mentioned in the chapter of Morphine & Allied Drugs by Reynolds et al which discusses the structure-activity relationship of opioids then in use (1957)
 
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