RTI-6037-13
Also called 2-(N-tert-Butylamino)-3''-chloropentanophenone
Overview
RTI-6037-13, also known as 3′-chloro-2-(tert-butylamino)pentanophenone, is an experimental stimulant drug from the cathinone family and a bupropion analogue; this compound is related to pyrrolidinophenone (it is an α-propylphenethylamine) which has been proposed for use as a treatment for smoking cessation and as a potential treatment for cocaine dependence.[1]
Drug class
Norepinephrine–dopamine reuptake inhibitor Stimulant WP
From the Wikipedia article's infobox.
Pharmacology
Pharmacodynamics
RTI-6037-13 is a central nervous system stimulant; it acts as a norepinephrine–dopamine reuptake inhibitor. It is more effective at inhibiting the dopamine transporter than bupropion and cocaine, and more effective at inhibiting the norepinephrine transporter than bupropion, but not as effective as cocaine. The binding affinities (Kᵢ) for the norepinephrine and dopamine transporters were 96 ± 20 nM and 1,171 ± 260 nM, respectively, whilst the IC₅₀ values (for catecholamine reuptake) for RTI-6037-13 were 33 ± 7 nM and 472 ± 93 nM for dopamine and norepinephrine, respectively. It had no affinity for the serotonin transporter. RTI-6037-13 is a nicotinic antagonist. It blocks nicotinic receptors; it blocks the α3β4 receptor with an IC₅₀ value of 0.70 µM (2.5 times more potent than bupropion), and is more effective than bupropion at blocking the α4β2 receptor (7.7 µM versus 12 µM for bupropion). It blocked the α4β4 receptor with an affinity of 2 µM.[1]
RTI-6037-13 has an ED₅₀ (half-maximal effective dose) of 15.5 mg/kg. This means that it is approximately half as potent as cocaine (7.8 mg/kg), and almost three times less potent than bupropion (5.5 mg/kg) — that is, a higher dose is required to achieve 50 per cent of its maximum effect; at the peak of its activity, RTI-6037-13 reaches 108 per cent of the maximum effect of cocaine. This shows that, in terms of its maximum stimulant potency, it is practically equivalent to cocaine (and surpasses bupropion, for which this figure is 87 per cent), RTI-6037-13 has a delayed onset of maximum effect, which occurs only 90–120 minutes after administration; RTI-6037-13 effect lasts from 210 to 480 minutes (up to 8 hours), which significantly exceeds the duration of action of cocaine (40–100 minutes) and bupropion (130–270 minutes).[1]
The results of a drug discrimination test in rats (the subjective effect of the substance on cocaine-induced stimulation) are known; RTI-6037-13 is approximately four times weaker than cocaine in its ability to induce similar subjective sensations, but stronger than bupropion; following administration of a 25 mg/kg dose, the overall frequency of lever presses (the rat’s behavioural activity) increased, RTI-6037-13 acted as a potent stimulant.[1]
Chemistry
Mixing
For best safety practice, don't mix this drug with other stimulants.
Why: vasoconstriction, heart rate and blood pressure. PsychonautWiki says:
- “... may be dangerous to combine with other stimulants ... as they can increase one's heart rate and blood pressure to dangerous levels.” (PsychonautWiki, dangerous interactions table, "Stimulants" row, revision 148925)
- “Vasoconstriction can be described as a narrowing of the veins and blood vessels which results from a contraction of their muscular wall.” (PsychonautWiki, Vasoconstriction, revision 170337)
- “... it can also occur under the influence of traditional stimulants such as methamphetamine, caffeine, and MDMA.” (PsychonautWiki, Vasoconstriction, revision 170337)
- “Increased blood pressure is most commonly induced under the influence of heavy dosages of vasoconstricting compounds, such as traditional stimulants and stimulating psychedelics.” (PsychonautWiki, Increased blood pressure, revision 152273)
Quotes from PsychonautWiki, CC BY-SA 4.0.
Harm reduction information
No harm reduction data is on file for this compound yet. That means no dose, timing or combination data from PsychonautWiki or TripSit. Please don't guess a dose from similar compounds. If you have taken it and feel unwell, contact emergency services or a poison control center.
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Sources
- Journal / agency Carroll FI, Blough BE, Mascarella SW, Navarro HA, Lukas RJ, Damaj MI. Advances in Pharmacology. 2014. doi:10.1016/B978-0-12-420118-7.00005-6
- Journal / agency Carroll FI, Blough BE, Abraham P, Mills AC, Holleman JA, Wolckenhauer SA, Decker AM, Landavazo A, McElroy KT, Navarro HA, Gatch MB, Forster MJ. Synthesis and biological evaluation of bupropion analogues as potential pharmacotherapies for cocaine addiction. Journal of Medicinal Chemistry. November 2009. doi:10.1021/jm901189z · PMID 19821577
- Journal / agency Carroll FI, Blough BE, Mascarella SW, Navarro HA, Eaton JB, Lukas RJ, Damaj MI. Synthesis and biological evaluation of bupropion analogues as potential pharmacotherapies for smoking cessation. Journal of Medicinal Chemistry. March 2010. doi:10.1021/jm9017465 · PMID 20158204 · PMC2841507
Text and values on this page are quoted from Wikipedia (CC BY-SA 4.0), PubChem (public domain). Each value links to the exact revision it came from.