Pentoxyverine

[BothHands]

I've just recently heard about this chemical, but I can't seem to find any information on it.

I've read a few uncited sources claiming that it's hallucinogenic, and related to DXM. But I've also seen an uncited source claiming that it is purely a sigma agonist, and that it has no recreational value.

What's your take on this chemical? Is it worth looking into?



I was also wondering if anyone had any information on the sigma receptors, other than the basics.

 

[lkpjh]

also known as carbetapentane, it may have utility in mu-agonist wd, and has various merits on its own, "recreational" & otherwise. Sigma receptor affinity is an interesting critter, as so many things are ligands for the receptor, but at what sort of effective dose? It's possible that some of the "spiritual" activity produced by certain drugs is mediated by activity at sigma receptors (DMT, d-methorphan, etc)
I've been looking for it for a while, but it seems like medicines with carpetapentane &/v pentoxyverine in them aren't all that commonly available anymore. There's a few "niche" pharmaceutical houses that produce just a few products, with, say carpetapentane & guaifenesin combinations, though at least one that I found was phasing that product out.

http://en.cnki.com.cn/Article_en/CJFDTOTAL-XYYL199302017.htm
"Comparison of antitussive effects between dextromethorphan and pentoxyverine

WU Jia-Rong (Shanghai Sixth People's Hospital, Shanghai 200233) CHEN Shu-Xia (Ren-ji Hospital, Shanghai Second Medical University, Shanghai 200001) WU Feng-Bao (Children Hospital, Shanghai Medical University, Shanghai 200032) ZHANG Si-Wei (Huashan Hospital, Shanghai Medical University, Shanghai 200040)
A double-blind randomized trial was made on 300 patients with respiratory tract diseases. The daily oral dosage were 90mg for adults (90 in each group) or Img/kg for children (60 in each group) for 7d. The antitussive efficacies for dextromethorphan and pentoxyverine were 95.3% and 82.0%, respectively (P0.01). Few adverse reactions were seen. It is concluded that dextromethorphan is better than pentoxyverine.
【Key Words】： cough/drug therapy dextromethorphan/therapeutic use pentoxyverine/therapeutic use double-blind method randomized-controlled trials
【DOI】： CNKI:SUNYYL.0.1993-02-017"

so, it appears that d-methorphan has a slightly increased efficacy for antitussive effects...however, given that there has been some interest in the greater regulation or even scheduling of d-methorphan, I wonder if it might bring consumer products featuring pentoxyverine / carpetapentane back into vogue...

 

[lkpjh]

this is interesting: http://journals.lww.com/cardiovascu...f_Common_Antitussive_Drugs_on_the_hERG.3.aspx
"Journal of Cardiovascular Pharmacology:
December 2008 - Volume 52 - Issue 6 - pp 494-499
doi: 10.1097/FJC.0b013e31818eec8d
Original Article
Effects of Common Antitussive Drugs on the hERG Potassium Channel Current
Deisemann, Heike; Ahrens, Nadine; Schlobohm, Irene; Kirchhoff, Christian PhD; Netzer, Rainer PhD; Möller, Clemens PhD
Abstract
A common over-the-counter (OTC) non-opioid antitussive drug, clobutinol, was recently withdrawn from the market due to its potential to induce cardiac arrhythmias by a blockade of the potassium channel coded by the human ether-à-go-go-related gene (hERG). In this study, we investigated the effects of a number of antitussive compounds on the hERG ion channel current using patch-clamp electrophysiology, and compared the effects to that of clobutinol. The compounds clobutinol, pentoxyverine, dextromethorphan, and codeine inhibited the outward current in hERG transfected cells with half-maximal inhibition concentrations (IC50) of 1.9 μM, 3.0 μM, 5.1 μM, and 97 μM, respectively. For theobromine, no significant effect on the hERG current at a concentration up to 100 μM was detected. Safety margins between the effects of the drugs on the hERG ion channel current and their calculated maximal free therapeutic plasma concentration were calculated. These results were compared to assess potential risks of the compounds to induce torsade de pointes-type arrhythmias."

 

[lkpjh]

also interesting:
http://md1.csa.com/partners/viewrec...883&q=pentoxyverine&uid=1236796&setcookie=yes
"Carbetapentane Toxicity Presenting as a Pseudo-Parkinsonian Reaction
Banner, W | McGoodwin, PL | Badillo, R
Journal of Toxicology: Clinical Toxicology [J. Toxicol.: Clin. Toxicol.]. Vol. 42, no. 5, p. 728. Aug 2004.

Carbetapentane (pentoxyverine, CBP) is a non-opioid antitussive present in prescription cough medications. It is relatively new and little is known about its toxic side effects. This drug has a high affinity for sigma receptors similar to haloperidol and blocks NMDA effects in the CNS as well as binding to dopamine 3 receptors.

Descriptors: Article Subject Terms Calcium-binding protein | Central nervous system | Cough | Dopamine receptors | Haloperidol | N-Methyl-D-aspartic acid | Side effects | Sigma receptors | Toxicity"

 

[lkpjh]

also interesting:
http://md1.csa.com/partners/viewrec...883&q=pentoxyverine&uid=1236796&setcookie=yes
"Carbetapentane Toxicity Presenting as a Pseudo-Parkinsonian Reaction
Banner, W | McGoodwin, PL | Badillo, R
Journal of Toxicology: Clinical Toxicology [J. Toxicol.: Clin. Toxicol.]. Vol. 42, no. 5, p. 728. Aug 2004.

Carbetapentane (pentoxyverine, CBP) is a non-opioid antitussive present in prescription cough medications. It is relatively new and little is known about its toxic side effects. This drug has a high affinity for sigma receptors similar to haloperidol and blocks NMDA effects in the CNS as well as binding to dopamine 3 receptors.

Descriptors: Article Subject Terms Calcium-binding protein | Central nervous system | Cough | Dopamine receptors | Haloperidol | N-Methyl-D-aspartic acid | Side effects | Sigma receptors | Toxicity"

this is also relevant:
http://www.springerlink.com/content/k756621w18032618/

"PHARMACEUTICAL RESEARCH
Volume 17, Number 5, 565-571, DOI: 10.1023/A:1007516916077
Published in partnership with

The American Association of Pharmaceutical Scientists
Propiverine-Induced Parkinsonism: A Case Report and a Pharmacokinetic/Pharmacodynamic Study in Mice
Hirotami Matsuo, Akiko Matsui, Risa Nasu, Hitomi Takanaga, Naohide Inoue, Fumitada Hattori, Hisakazu Ohtani and Yasufumi Sawada
Abstract
Purpose. We present a case report of propiverine-inducedParkinsonism. We previously reported the induction of catalepsy by amiodarone,aprindine and procaine, which possess a diethylaminomethyl moietyand demonstrated selective blockade of dopamine D2 receptors bythese drugs in mice. We hypothesized that drugs possessing adiethylaminomethyl structure may generally induce Parkinsonism and/orcatalepsy.
Methods. Thus, we performed a study to examine whether oxybutynin,pentoxyverine and etafenone, as well as propiverine, induce catalepsyin mice.
Results. The intensity of drug-induced catalepsy was in the order:haloperidol > etafenone > pentoxyverine > propiverine > oxybutynin.In vivo occupancy of dopamine D1, D2 and mACh receptors in thestriatum was also examined. The in vitro binding affinities to the D1,D2 and mACh receptors in the striatum synaptic membrane were withinthe ranges of 2.4–140 M, 380–4,200 nM, and 1.2–2,800 nM, respectively.
Conclusions. These results support the idea that any drug possessinga diethylaminomethyl moiety may contribute to the induction ofcatalepsy, possibly by occupying dopamine receptors."

 

[BothHands]

Hmm, so it does have NMDA antagonist activity after all? That's interesting. I've never seen this before in the US, but someone on Shroomery who lives in Australia says that pentoxyverine is the most widely available cough suppressant there, and that finding dextromethorphan is quite difficult. This is what sparked my interest in the chemical. If I were to buy it, it would have to be online. And at this point, it doesn't seem like it would be worthwhile. At least not until a lot more is known. Especially since you mention a possibility of developing parkinsons.

I would like to find a safe way to experiment with my sigma receptors though. Apparently they're euphoric for some, and dysphoric for others. I wish there was more literature on this.

 

[sekio]

You might be interested in this thread.

 

[lkpjh]

also relevant:
http://www.ncbi.nlm.nih.gov/pubmed/14653224
"Nihon Shinkei Seishin Yakurigaku Zasshi. 2003 Oct;23(5):187-96.
[Effects of sigma receptor ligands on psychiatric disorders].
[Article in Japanese]
Kamei H, Noda Y, Nabeshima T, Yamada K.
Source

Laboratory of Neuropsychopharmacology, Faculty of Pharmaceutical Sciences, Kanazawa University, 13-1, Takara-machi, Kanazawa, 920-0934, Japan.
Abstract

It has recently been suggested that sigma receptors are involved in psychiatric disorders. Sigma 1 receptor antagonists are effective in animal models of positive symptoms, cognitive deficit and disruption of prepulse inhibition in schizophrenia. They also inhibit the development and expression of the conditioned place preference induced by cocaine. On the other hand, sigma 1 receptor agonists reduce the immobility time in the forced swimming and tail suspension tests. Furthermore, sigma 1 receptor agonists attenuate the conditioned fear stress (CFS) response (which is not attenuated by typical anxiolytics or antidepressants) in rodents. The attenuating effects are mediated through sigma 1 receptors, which are closely related to the mesolimbic dopaminergic systems. Sigma 1 receptor agonists also have anti-amnesic effects in various experimental models. Neurosteroids such as dehydroepiandrosterone sulfate and pregnenolone sulfate attenuate the CFS response and have anti-amnesic effects, the effects being mediated via sigma 1 receptors. These findings suggest that sigma receptors are novel potential targets for the treatment of psychiatric disorders such as schizophrenia, drug abuse, depression and dementia."