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Talk:Brorphine: Difference between revisions
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==History and culture== | ==History and culture== | ||
{{historyStub}} | {{historyStub}} | ||
Brorphine was first described in the scientific literature as a μ-opioid receptor agonist in 2018.<ref name="DEA2020"/> It was | Brorphine was first described in the scientific literature as a μ-opioid receptor agonist in 2018.<ref name="DEA2020"/> It was reported to the UNODC Early Warning Advisory on NPS in 2019.<ref name="UNODC2020"/> In mid-2019 brorphine | ||
emerged in the United States’ drug market.<ref name="DEA2020"/> After the temporarily scheduling of isotonitazene in June 2020 by the Drug Enforcement Administration, detections of brorphine in the U.S. began to increase, appearing as similar gray drug powders and an apparent | |||
replacement for isotonitazene.<ref name="CFSRE2020">{{cite web|title=The Rise of Brorphine — A Potent New Synthetic Opioid Identified in the Midwestern United States|date=July 2020|first1=A. J.|last1=Krotulski|first2=D. M.|last2=Papsun|first3=C.|last3=Noble|first4=S. L.|last4=Kacinko|first5=L.|last5=Nelson|first6=B. K.|last6=Logan|publisher=Center for Forensic Science Research and Education (CFSRE)|url=https://www.npsdiscovery.org/wp-content/uploads/2020/07/Public-Alert_Brorphine_NPS-Discovery_072720.pdf}}</ref> | replacement for isotonitazene.<ref name="CFSRE2020">{{cite web|title=The Rise of Brorphine — A Potent New Synthetic Opioid Identified in the Midwestern United States|date=July 2020|first1=A. J.|last1=Krotulski|first2=D. M.|last2=Papsun|first3=C.|last3=Noble|first4=S. L.|last4=Kacinko|first5=L.|last5=Nelson|first6=B. K.|last6=Logan|publisher=Center for Forensic Science Research and Education (CFSRE)|url=https://www.npsdiscovery.org/wp-content/uploads/2020/07/Public-Alert_Brorphine_NPS-Discovery_072720.pdf}}</ref> | ||
==Chemistry== | ==Chemistry== | ||
{{chemistry}} | {{chemistry}} | ||
Brorphine is an atypical opioid of the piperidine and benzimidazolone class which has some structural similarities with fentanyl.<ref name="UNODC2020"/><ref name="CFSRE2020"/> It is comprised of three main units: A 4-bromophenethyl group, a piperidine ring, and a 1,3-dihydro-2H-benzoimidzole-2-one group. Brorphine is being trafficked as its hydrochloride salt which would be water-soluble.<ref name="DEA2020">{{cite web|date=August 2020|title=Brorphine|url=https://www.deadiversion.usdoj.gov/drug_chem_info/brorphine.pdf|publisher=Drug Enforcement Administration (DEA)}}</ref> | Brorphine is an atypical opioid of the [[piperidine]] and benzimidazolone class which has some structural similarities with [[fentanyl]].<ref name="UNODC2020"/><ref name="CFSRE2020"/> It is comprised of three main units: A 4-bromophenethyl group, a piperidine ring, and a 1,3-dihydro-2H-benzoimidzole-2-one group. Brorphine is being trafficked as its hydrochloride salt which would be water-soluble.<ref name="DEA2020">{{cite web|date=August 2020|title=Brorphine|url=https://www.deadiversion.usdoj.gov/drug_chem_info/brorphine.pdf|publisher=Drug Enforcement Administration (DEA)}}</ref> | ||
==Pharmacology== | ==Pharmacology== | ||
{{pharmacology}} | {{pharmacology}} | ||
Opioids exert their effects by binding to and activating the [[Opioid#Mu_.28.CE.BC.29|μ-opioid]] [[receptor]]. This occurs because opioids structurally mimic endorphins which are naturally found in the body and also work with the μ-opioid receptor set. The way in which opioids structurally mimic these natural endorphins results in their [[physical euphoria|euphoria]], [[pain relief]] and [[anxiolytic]] effects. This is because endorphins are responsible for reducing pain, causing sleepiness, and feelings of pleasure. They can be released in response to pain, strenuous exercise, orgasm, or general excitement. | [[Opioids]] exert their effects by binding to and activating the [[Opioid#Mu_.28.CE.BC.29|μ-opioid]] [[receptor]]. This occurs because opioids structurally mimic endorphins which are naturally found in the body and also work with the μ-opioid receptor set. The way in which opioids structurally mimic these natural endorphins results in their [[physical euphoria|euphoria]], [[pain relief]] and [[anxiolytic]] effects. This is because endorphins are responsible for reducing pain, causing sleepiness, and feelings of pleasure. They can be released in response to pain, strenuous exercise, orgasm, or general excitement. | ||
''In vitro'' pharmacological data show brorphine exhibits potency similar to fentanyl | ''In vitro'' pharmacological data show brorphine exhibits potency similar to [[fentanyl]]<ref name="CFSRE2020"/> and activation of mu-opioid receptors involves recruitment of beta-arrestin-2, a regulatory protein<ref name="DEA2020"/> | ||
==Subjective effects== | ==Subjective effects== | ||
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*'''[[Effect::Pain relief]]''' | *'''[[Effect::Pain relief]]'''<ref name="DEA2020"/> | ||
*'''[[Effect::Physical euphoria]]''' | *'''[[Effect::Physical euphoria]]'''<ref name="DEA2020"/> | ||
*'''[[Effect::Itchiness]]''' - This compound, like most opioids, tends to cause strong histamine reactions which cause the skin to feel itchy. | *'''[[Effect::Itchiness]]''' - This compound, like most opioids, tends to cause strong histamine reactions which cause the skin to feel itchy. | ||
*'''[[Effect::Respiratory depression]]''' | *'''[[Effect::Respiratory depression]]'''<ref name="DEA2020"/> | ||
*'''[[Effect::Sedation]]''' | *'''[[Effect::Sedation]]''' | ||
*'''[[Effect::Constipation]]''' | *'''[[Effect::Constipation]]''' | ||
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|{{effects/cognitive| | |{{effects/cognitive| | ||
*'''[[Effect::Cognitive euphoria]]''' | *'''[[Effect::Cognitive euphoria]]'''<ref name="DEA2020"/> | ||
*'''[[Effect::Anxiety suppression]]''' | *'''[[Effect::Anxiety suppression]]''' | ||
*'''[[Effect::Compulsive redosing]]''' | *'''[[Effect::Compulsive redosing]]''' | ||
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Recent detections in drug related deaths leads to the conclusion that brorphine has the potential to cause widespread harm.<ref name="CFSRE2020"/> There are no published studies on safety for human use as of August 2020.<ref name="DEA2020"/> | Recent detections in drug related deaths leads to the conclusion that brorphine has the potential to cause widespread harm.<ref name="CFSRE2020"/> There are no published studies on safety for human use as of August 2020.<ref name="DEA2020"/> | ||
It is strongly recommended that one use [[responsible drug use|harm reduction practices]], and take extreme caution when using this substance. | It is strongly recommended that one use [[responsible drug use|harm reduction practices]], and take extreme caution when using this substance. | ||
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Brorphine is not under international control.<ref name="UNODC2020"/> | Brorphine is not under international control.<ref name="UNODC2020"/> | ||
*'''Turkey:''' Metonitazene is a classed as drug and is illegal to possess, produce, supply, or import.<ref>https://resmigazete.gov.tr/eskiler/2020/10/20201007-8.pdf</ref> | |||
*'''United States''': As of August 2020, brorphine is not controlled under the Controlled Substances Act.<ref name="DEA2020"/> | *'''United States''': As of August 2020, brorphine is not controlled under the Controlled Substances Act.<ref name="DEA2020"/> | ||