Buy U-47700 opioid suppliers

Buy U-47700 opioid suppliers

U-47700, also known as U4, pink heroin, pinky, and pink, is an opioid analgesic drug developed by a team at Upjohn in the 1970s which has around 7.5 times the potency of morphine in animal models.

U-47700 is a structural isomer of the earlier opioid AH-7921^[6] and the result of a great deal of work elucidating the quantitative structure–activity relationship of the scaffold. Upjohn looked for the key moieties which gave the greatest activity^[7] and posted over a dozen patents on related compounds, each optimizing one moiety^{[8][9][10][11][12][13][14][15]} until they discovered that U-47700 was the most active.^[16]

U-47700 became the lead compound of selective kappa-opioid receptor ligands such as U-50488, U-51754 (containing a pyrrolidine rather than a dimethylamine substituent) and U-69,593, which share very similar structures.^[17]^[18] Although not used medically, the selective kappa ligands are used in research.^[19]^[20]

Pharmacology

U-47700 is an agonist of the μ-opioid receptor (K_i 11.1 ± 0.4 nM) and possesses significantly lower affinity for the κ-opioid receptor (K_i 287 ± 24 nM) and δ-opioid receptor (K_i 1220 ± 82 nM). U-47700 is approximately 10-fold more potent than morphine in rats, although the binding of U-47700 is 2-4 times weaker than morphine at all three opioid receptors.^[21]

The metabolism of U-47700 in humans involves mono- and didesmethylation followed by hydroxylation.^[22] The desmethyl metabolites of U-47700 have negligible affinity for the opioid receptors and are not thought to contribute to the activity of U-47700.^[23]^[24]

Side effects

U-47700 has never been studied in humans, but it would be expected to produce effects similar to those of other potent opioid agonists, including strong analgesia, sedation, euphoria, constipation, itching and respiratory depression which could be harmful or fatal.^[25]^[26]^[27]^[28]^[29]^[30]^[31]^[32] Tachycardia was another side effect encountered with U-47700 use.^[32] Tolerance and dependence would be expected to develop.^[33]

Deaths

Combined consumption of U-47700 with fentanyl and flubromazepam caused one fatality each in Belgium and Germany, respectively.^[34]^[35]^[36] One death was reported in Ireland ^[37] and another one in Italy.^[38] 17 opioid overdoses and several deaths in the United States had initially been associated with U-47700 in April 2016.^[39] As of September 2016 at least 15 fatalities were confirmed. By December 2017, at least 46 fatalities had been associated with the use of U-47700.^[40]^[41]^[42]^[43]^[44]^[45]^[46]

U-47700 was found in combination with fentanyl during the autopsy of the American artist Prince in 2016.^[47]

Detection in biological fluids

U-47700 may be measured in serum, plasma, blood or urine to monitor for abuse, confirm a diagnosis of poisoning, or assist in a medicolegal death investigation. Serum or blood U-47700 concentrations are expected to be in a range of 10–250 μg/L in intoxicated patients and 100–1,500 μg/L in deceased victims of acute overdosage. The detection usually involves analysis by liquid chromatography-mass spectrometry.^[48]

Society and culture

Common street names for U-47700 include pinky, pink, and U4.^[49]

Legal status

Following its sale as a designer drug, U-47700 was made illegal in Sweden on January 26, 2016.^[50]

U-47700 was emergency scheduled in Ohio on May 3, 2016, by executive order of Governor John Kasich.^[51]

U-47700 was emergency scheduled in Florida on September 27, 2016, by an emergency rule of Florida Attorney General Pam Bondi.^[52]

Responding to a perceived threat to public health and safety, the U.S. Drug Enforcement Administration has placed U-47700 into Schedule I of the Controlled Substances Act, effective November 14, 2016.^[53] In April 2018, U-47700 was placed into Schedule I indefinitely.^[54]

U-47700 was placed into Schedule 1 of South Dakota’s Controlled Substance Schedule. It was signed by Governor Daugaard on February 9, 2017.^[55]

U-47700 was made a Class A, Schedule 1 drug under the Misuse of Drugs Act in the UK in 2017.^[56]

In popular culture

U-47700 is the title of a 2021 Dutch sci-fi short film by director Erasmo de la Parra.^[57] In the film, the characters are addicted to a new drug containing the substance U-47700.

N-Desmethyl U-47700 is the primary urinary metabolite of U-47700 . It is a certified reference material suitable for use as a starting material in calibrators and controls in N-Desmethyl U-47700 LC/MS or GC/MS testing methods for clinical toxicology, urine drug testing, or forensic analysis applications .

Scientific Research Applications

Safety and Hazards

N-Desmethyl U-47700 is classified as Acute Tox. 4 Dermal, Acute Tox. 4 Inhalation, Acute Tox. 4 Oral, Eye Irrit. 2, and Flam. Liq. 2. It is considered dangerous with the signal word “Danger” and has hazard statements H225, H302 + H312 + H332, and H319.

Mechanism of Action

Target of Action

N-Desmethyl U-47700 is a primary metabolite of U-47700, a synthetic opioid . The primary target of N-Desmethyl U-47700 is the μ-opioid receptor . This receptor plays a crucial role in mediating the effects of opioids, including analgesia and euphoria.

Mode of Action

N-Desmethyl U-47700 acts as an agonist at the μ-opioid receptor . Agonists bind to receptors and activate them to produce a biological response. In this case, N-Desmethyl U-47700 binds to the μ-opioid receptor, triggering a series of intracellular events that lead to the drug’s effects .

Biochemical Pathways

Upon activation of the μ-opioid receptor, N-Desmethyl U-47700 initiates a cascade of biochemical events. These include the inhibition of adenylate cyclase, decreased cAMP production, and the opening of potassium channels. This leads to hyperpolarization of the cell membrane and inhibition of neurotransmitter release . The exact pathways affected by N-Desmethyl U-47700 are still under investigation.

Pharmacokinetics

The pharmacokinetics of N-Desmethyl U-47700 involve its absorption, distribution, metabolism, and excretion (ADME). It is primarily metabolized in the liver, and its metabolites are excreted in urine . The compound’s plasma concentrations are positively correlated with its pharmacodynamic effects .

Result of Action

The activation of the μ-opioid receptor by N-Desmethyl U-47700 results in potent analgesic effects . It also poses a serious risk for overdosing and death due to its strong opioid activity . The loss of one or two methyl groups from U-47700 to form N-Desmethyl U-47700 reduces the MOR activation potential .

Action Environment

The action of N-Desmethyl U-47700 can be influenced by various environmental factors. For instance, the compound’s stability may be affected by temperature and pH Additionally, individual factors such as age, health status, and genetic makeup can influence the compound’s action, efficacy, and stability

properties

CAS RN	67579-73-1	Source

Q & A

Q1: What is the significance of N-Desmethyl U-47700 in forensic toxicology?

A1: N-Desmethyl U-47700 is a primary metabolite of U-47700 and has been detected in higher concentrations than the parent drug in certain tissues, like pig brain. [] This highlights the importance of analyzing for metabolites in addition to the parent compound in forensic toxicology, as metabolite presence can provide crucial information about drug exposure even when parent drug concentrations are low. [, ]

Q2: Are there any analytical challenges in detecting and quantifying N-Desmethyl U-47700?

A2: Identifying and quantifying N-Desmethyl U-47700, especially in the context of forensic investigations, requires specialized analytical techniques. Liquid chromatography coupled with tandem mass spectrometry (LC-MS/MS) is commonly employed for this purpose. [, , ] This method allows for the separation and sensitive detection of the metabolite in complex biological matrices. [, , ]

Q3: How does the tissue distribution of N-Desmethyl U-47700 compare to U-47700?

A3: Research using a pig model showed that N-Desmethyl U-47700 reaches higher concentrations in certain tissues compared to U-47700, notably in the brain. [] While U-47700 was found in higher concentrations in duodenum content, bile fluid, and adipose tissue, N-Desmethyl U-47700 was more prominent in organs involved in metabolism, such as the liver and kidney. [] This difference in distribution patterns underscores the importance of considering both parent and metabolite concentrations when interpreting toxicological findings. []

Q4: What is the postmortem redistribution potential of N-Desmethyl U-47700?

A4: Studies using a controlled pig model suggest that N-Desmethyl U-47700 demonstrates low to moderate postmortem redistribution. [] This finding is crucial for forensic investigations, as it implies that measured concentrations of this metabolite in postmortem samples can provide relatively reliable information about drug exposure prior to death. []

Q5: What are the implications of the metabolic profile of U-47700 for forensic analysis?

A5: U-47700 exhibits metabolic transformations similar to U-49900, resulting in a shared metabolite and isomeric species. [] This overlap in metabolic pathways presents a challenge for forensic analysts, as it necessitates careful interpretation of analytical data to differentiate between exposure to these two substances. []

Disclaimer and Information on In-Vitro Research Products

Please be aware that all articles and product information presented on BenchChem are intended solely for informational purposes. The products available for purchase on BenchChem are specifically designed for in-vitro studies, which are conducted outside of living organisms. In-vitro studies, derived from the Latin term “in glass,” involve experiments performed in controlled laboratory settings using cells or tissues. It is important to note that these products are not categorized as medicines or drugs, and they have not received approval from the FDA for the prevention, treatment, or cure of any medical condition, ailment, or disease. We must emphasize that any form of bodily introduction of these products into humans or animals is strictly prohibited by law. It is essential to adhere to these guidelines to ensure compliance with legal and ethical standards in research and experimentation.

N-Desmethyl-U-47700 is a primary metabolite of the synthetic opioid U-47700. [, , , ] It is formed through metabolic processes within the body, specifically identified as a product of human liver microsomes. [] This compound serves as a crucial target for analysis in various scientific investigations, particularly in forensic toxicology, due to its presence in biological samples after U-47700 administration. [, , , ]

Synthesis Analysis

The synthesis of N-Desmethyl-U-47700 is not directly addressed in the provided literature. The studies primarily focus on its identification and analysis as a metabolic product of U-47700. [, , , ]

Molecular Structure Analysis

While the provided literature does not delve into the specific structural analysis of N-Desmethyl-U-47700, it confirms the loss of a methyl group compared to the parent compound, U-47700. [, ] This structural change influences its interaction with μ-opioid receptors. []

Applications

Forensic Toxicology: N-Desmethyl-U-47700 is a crucial marker for detecting U-47700 use in forensic investigations. [, , , ] Its presence in biological samples, even at higher concentrations than the parent compound in certain tissues, aids in confirming U-47700 intake. [, ]
Toxicological Studies: Research utilizes N-Desmethyl-U-47700 to understand the metabolic pathways and distribution patterns of U-47700 in biological systems. [, , ] This information is vital for interpreting toxicological findings and understanding the pharmacokinetics of U-47700.
Receptor Binding Assays: N-Desmethyl-U-47700 serves as a tool in evaluating μ-opioid receptor activation potential and comparing it to U-47700 and other opioids. [] This contributes to a better understanding of structure-activity relationships for opioid compounds.

Related Compounds

U-47700

Compound Description: U-47700 is a synthetic opioid agonist with potent analgesic effects [, , , ]. It is a Schedule I controlled substance in the United States.
Relevance: U-47700 is the parent compound of N-Desmethyl U-47700, meaning N-Desmethyl U-47700 is a direct metabolite of U-47700 [, , , ]. Both compounds act on μ-opioid receptors, but U-47700 exhibits a stronger activation potential compared to its metabolite [].

N,N-Didesmethyl-U-47700

Compound Description: N,N-Didesmethyl-U-47700 is a metabolite of U-47700, formed through further demethylation of N-Desmethyl U-47700 [, ].
Relevance: N,N-Didesmethyl-U-47700 is structurally similar to N-Desmethyl U-47700, differing by the removal of an additional methyl group [, ]. Both are metabolites of U-47700 and can be detected in biological samples after U-47700 use []. N,N-Didesmethyl-U-47700 shows significantly weaker μ-opioid receptor activation compared to both U-47700 and N-Desmethyl U-47700 [].

O-Desmethyltramadol (ODT)

Compound Description: O-Desmethyltramadol (ODT) is the primary active metabolite of tramadol, another synthetic opioid analgesic [].
Relevance: Although structurally different from N-Desmethyl U-47700, ODT serves as a point of comparison in research studying the tissue distribution and metabolic pathways of novel synthetic opioids like U-47700 []. Both ODT and N-Desmethyl U-47700 are primary metabolites of their respective parent compounds and exhibit significant presence in organs involved in metabolism [].

Tramadol

Compound Description: Tramadol is a centrally acting synthetic opioid analgesic used to treat moderate to moderately severe pain [, ].
Relevance: Tramadol, similar to U-47700, is a synthetic opioid whose pharmacokinetic properties and metabolic pathways are studied in relation to understanding the behavior of newer synthetic opioids like U-47700 [, ]. Both Tramadol and U-47700 are investigated for their postmortem redistribution patterns, with their primary metabolites, ODT and N-Desmethyl U-47700 respectively, playing a key role in understanding their distribution in the body after death [].
Buy U-47700 opioid suppliers
Buy U-47700 opioid suppliers
Buy U-47700 opioid suppliers
Buy U-47700 opioid suppliers
Buy U-47700 opioid suppliers
Buy U-47700 opioid suppliers
Buy U-47700 opioid suppliers
Buy U-47700 opioid suppliers
Buy U-47700 opioid suppliers

Bromazolam Powder Sales