While I appreciate it unlikely that anyone will get to sample it, we found pynazolam to be the most euphoric. The reaon being that it is a 'frustrated α1 ligand i.e. it buns to the α3,α5 & and α5 subunits so it has reasonably potent anxiolytic activity, it's also a serotonin releaser. A potent serotonin releaser.
ALL nitrobenzodiazepines are serotonin releasers although one or two (such as clonazepam), it's serotonin releasing action isn't encounterd at theraputic doses. We noted that nimetazepam is the most favoured benzodiazepine in nations where it is available. People would consume nimetazepam before socializing - not typical for a benzodiazepine.
We asked ourselves the simple question, to whit 'Why were all the early benzodiazepine hypnotiic nitrobenzodiazepines?' and so we decided to design a 'frustrated α1 ligand' i.e. it would LOVE to fit into the α1 subunit but the pendent aromatic being a pyridyl ring, it cannot. So we noted that it had notable seratanogenic activity (hence sociability of nimetazepam) overlaid with the usual action produced by the α3 and α4 subunits i.e. anxiolytic but not hypnotic.
THAT is why nitrobenzodiazepines were noted for their hypnotic activity. Both their α1 affinity AND their SRI activity combine to induce sleep.
None of us had ever tasted methaqualone but a few older memers of the cohort did make direct comparisons with methaqualone. You just want to sit down and enjoy the experience. Higher dises intesify the seratonegenic activity and the anxiolytic activity but we were still minded to remember than nitrobenzodiazepines are more toxic in overdose than other benzodiazepines. Later we discovered that pynazolam is essentially exreted unchanged. Hydroxylayion of the 2 methyl being the only metabolite and that was only found in small quantities. It being the metabolites of nitrobenzodiazepines that are toxic - still, discression is the better part of valour.
So 5mg was nice, 10mg was great but we didn't go any further. We had sufficient to either go higher or to test chronic use i.e. on consecutive evenings. Only after about a week did we note any reduction in the intensity of the effects so knowing tolerance is the 'yellow warning' that dependence would soon follow, we stopped.
Only eight people tasted pyrazolam, pyeyzolam AND pynazolam and what was of most interest to me was when asked which of the three was preferred, without a moment's thought, they all agreed that pynazolam was the best.
Luckily there are now a number of two step reactions that replace an aryl halide (the -Br of pyrazolam) with an aryl nitro moiety. I believe at bench scale pynazolam was synthesized from pyrazoam via the boronic acid route. Nott practical to scale and of course you need a ready supply of pyrazolam to hand. Luckily, that was not an issue for us.
So 5-10mg reliably produced extremely social evenings followed by restful sleep and no hangover.
But that's the thing isn't it? Nobody is going to offer an RC where 10mg is a dose when crazy stuff like flunitrazolam are far more potent and far simpler to produce. In the case of flunitrazolam, norflunitrazepam --> northionitrazepam --> flunitrazolam. Easy.
