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From Blog: Terra Sigillata

David Nichols with chemist blogger Andrea Sella on BBC4 IYC programme

Our beloved C&EN online editor, Rachel Pepling, pointed out to me yesterday an insightful post about David Nichols by University College London chemist, Andrea Sella, at his Solarsaddle’s Blog. You’ll recall that my previous post commented on the Nature commentary by Purdue University distinguished chemist and pharmacologist, David Nichols, as he lamented how some of his synthetic schemes for neuroactive compounds have been adopted by those in the recreational street drug industry.

In his post, “Is David Nichols just a wee bit disingenuous?,” Sella discusses how Nichols did not reveal in the commentary his professional relationship with revered “psychedelic” chemist, Alexander “Sasha” Shulgin. I probably don’t have to tell chemists about Shulgin – and that Shulgin’s 1991 book co-authored with his wife, Ann, entitled, PIKHAL: A Chemical Love Story, is the central holy book of drug users wishing to expand their consciousness and explore their mystic relationship with the world and themselves. (PIKHAL stands for Phenethylamines I Have Known and Loved – the Shulgins also wrote another book on tryptamines, TIKHAL.). PIKHAL is part fictionalized autobiography of the couple and part synthesis and personal bioassay descriptions of about 200 psychoactive compounds.

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From Blog: Terra Sigillata

David Nichols, legal highs, and the social responsibilities of the scientist


David E. Nichols, PhD, Robert C. and Charlotte P. Anderson Distinguished Chair in Pharmacology, Dept. of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, Purdue University.

Since we ended last year with a post on legal highs – and who decides which analogs are illegal – we logically begin this year, the International Year of Chemistry, with further discussion of synthetic, psychoactive intoxicants.

Today, Nature published an excellent commentary from Dr. David E. Nichols, entitled, “Legal highs: the darker side of medicinal chemistry.” Nichols, a distinguished chair in pharmacology at Purdue University’s College of Pharmacy, reflects on how he is haunted by the deaths that could be tracked back to unintended human use of compounds he and his group have synthesized in the course of legitimate biomedical research. Other scientists whose work has been used for nefarious purposes are likely to share these feelings, both in neuropharmacology and other areas of biological and physical sciences.

Even in my area of natural products and dietary supplements, several colleagues and I have had our work co-opted by herbal manufacturers to sell their goods, most often in the form of overinterpreting in vitro data to make false claims for human use. The listing of the full citations of our associated papers – or even investigator photographs – on manufacturer web pages to imply that we academic scientists have supported their product claims.

However, the same use of synthetic chemistry publications by chemists skirting federal drug laws is a far more serious issue that Nichols addresses in the Nature commentary. Back in October, we discussed here the views of Nichols on one’s scholarly work in neuropharmacology being adopted by the legal highs industry following a Wall Street Journal article by Jeanne Whalen. In fact, Nichols cites that WSJ article in his Nature commentary where his work was described by a Dutch legal highs entrepreneur:

He (David Llewellyn) and his chief chemist get ideas for new drugs by scanning scientific literature. They pay particularly close attention to new papers published by scholars known for researching mind-altering, psychoactive substances.

David Nichols, a pharmacologist at Purdue University, has been especially valuable, Mr. Llewellyn says. Through his work studying brain receptors, Dr. Nichols has developed a range of psychoactive substances. His papers give a full description of the drugs he’s using, including their chemical makeup. This provides Llewellyn and others with a roadmap for making the drugs.

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From Blog: Terra Sigillata

Smiles: 2C-I or not 2C-I?

Designer drugs in the news

This is tiring enough for a science writer. I cannot imagine being in law enforcement.

The pace at which psychoactive designer drugs are appearing on the street is about as challenging for me as keeping up with dietary supplement companies that adulterate their products with actual prescription drugs (an area I’ve been covering since 2007 but a practice that goes back decades.)

This week’s designer drug hullabaloo comes to us courtesy of last week’s frightful murder-suicide by Sons of Anarchy actor, the late Johnny Lewis. ABC News is reporting today that Lewis was reportedly taking “Smiles,” a street name for 2C-I, the phenethylamine hallucinogen first synthesized by Alexander Shulgin.

2C-I is more properly known as 2,5-dimethoxy-4-iodophenethylamine. This structural analog of mescaline (3,4,5-trimethoxyphenylethylamine) was among a litany of designer drugs that was criminalized in the US back in July with the Synthetic Drug Abuse Prevention Act of 2012 (Cheryl Hogue had a nice discussion of the Act, including some quotes from yours truly, in the 27 August 2012 issue of C&EN.).
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From Blog: Terra Sigillata

2011: The year in blog numbers

Well, we’re right about at the end of 2011 and it’s time to thank you find readers for checking in with us throughout the year. We’re slowly rebuilding our momentum here at CENtral Science since moving from ScienceBlogs and were just shy of 90,000 visits for the year. Many of our colleagues get that many each month or week, and a few even each day. Still, we’re very happy that you take time to read here – we consider our readers to be top-quality – brilliant, creative, good-looking, and they even smell good, too! I’ll take 90,000 of you folks any day over millions of other less desirable readers.

I can’t resist the temptation to put up our year-end traffic report since I have the data available and I just love data sets. In addition, I find it interesting to see what topics garnered the greatest traffic. Below, I’ve put up the list of posts that received 100 or more views. The homepage is obviously the first because of those who have us saved as a browser bookmark. But, no surprise, our major topic of interest overall was synthetic marijuana and other until-recently-legal high such as “bath salts.” But ranking quite highly were our posts on dietary supplements containing aromatase inhibitors for bodybuilding and the newly-approved natural product analog for multiple sclerosis, fingolimod (Gilenya).

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From Blog: Terra Sigillata

Terra Sig In the News (Hi, Mom!)

For Mom: The author and his best friend, circa 1967

Apologies for the quick note of narcissism but, hey, Mom will be proud of this.

Our continued examination of the legal highs industry brought us attention from the online arms of TIME and Nature Chemistry.

First, science writer and author, Maia Szalavitz, wrote last week at TIME Healthland about the bans by US states being placed on synthetic cannabimimetics and stimulants (think Spice herbal incense and bath salts, respectively). Early in our days here at CENtral Science, Maia interviewed us for her article and photogallery on natural products and the unusual origins of drugs. She’s since revisited with us for the legal highs story.

I had a chance to meet her in person at the recent ScienceOnline meeting in Research Triangle Park and have been really impressed with her science writing on topics ranging from human relationships to substance abuse treatment myths. Before her time at TIME, she was one of the very few writers of high scientific rigor at The Huffington Post. Keep an eye on her at TIME Healthland and Twitter (@maiasz) as the Charlie Sheen trainwreck unfolds. Szalavitz is also the co-author – with Bruce Perry, MD, PhD – of the 2010 book, Born for Love: Why Empathy Is Essential — and Endangered (Amazon link).

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From Blog: Terra Sigillata

“Synthetic marijuana” chemist John W. Huffman interviewed on regional NPR program

Dr. John W. Huffman. Source: Clemson University, Department of Chemistry

John W. Huffman is the retired Clemson University chemist whose non-cannabinoid cannabimimetics synthesized in the 1990s have spawned a legal highs industry in the United States. So-called herbal incense products like K2 Spice are sprayed with some of Huffman’s compounds such as JWH-018 and sold in head shops and convenience stores across the US.

However, many municipalities and 15 states have issued bans on the sales of these products. Nationally, the DEA is currently revising a final order to temporarily place some of Huffman’s compounds on Schedule I of controlled substances. Recreational use of these compounds came on the scene in Germany and across Europe several years ago and are now illegal there. The US military has been particularly aggressive in penalizing soldiers for use of synthetic marijuana products. In fact, Reuters reported yesterday afternoon that seven midshipmen at the US Naval Academy have been expelled for using Spice.

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From Blog: Terra Sigillata

WSJ Feature on “The Other Chemistry”

Jeanne Whalen, a Wall Street Journal reporter based in London, had an article yesterday on the European aspects of a phenomenon we’ve been discussing here at Terra Sig since the beginning of the year: the adoption of academic chemistry to produce legal intoxicants that are just on this side of the law. Whalen spends the first half of her article talking with David Llewellyn, a middle-aged Scotsman in Belgium who works with a chemistry colleague to scour the literature for synthetic schemes and basic pharmacology to manufacture “legal highs.”

I’ve spoken before about Clemson University chemistry professor emeritus, John W. Huffman, and his cannabimimetic naphthoylindoles synthesized in the 1990s that are now creating a buzz, as it were, in the US in the form of herbal incense and synthetic marijuana products.

In Whalen’s article, Llewellyn is quoted as finding the work of Purdue University pharmacologist, Dr. David E. Nichols, as a particularly fruitful information source. Nichols, the Robert C. and Charlotte P. Anderson Distinguished Chair in Pharmacology in the Department of Medicinal Chemistry and Molecular Pharmacology in the College of Pharmacy is not particularly pleased:

“The drugs we make often end up on the black market, and it’s very troubling to me,” he says. Particularly worrying is that the drugs are rarely tested in humans before hitting the street. Random people sometimes write to him to ask for help in making certain chemicals, he says. He doesn’t reply out of caution.

“When people use this stuff chronically, on a weekly basis—suppose it produces liver cancer?” he asks. Also of concern are effects on the kidneys and bone marrow. Most of the designer drugs haven’t been tested in humans at all, let alone in large clinical trials. Dr. Nichols says he himself only ever carried out animal tests of the compounds that others are now copying and selling.

Whalen also speaks with St. George’s University of London toxicologist, Dr. John Ramsey, about his efforts to keep up a database from identification of street drugs as they appear.

It’s a fascinating article on an issue that chemists and law enforcement have been dealing with for decades.

Source: Jeanne Whalen (with Kersten Zhang), In Quest for ‘Legal High,’ Chemists Outfox Law, Wall Street Journal, 30 October 2010.

Hat-tip: Aaron Rowe via Twitter.