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Article ; Online: Naltrexone maintenance fails to alter amphetamine effects on intracranial self-stimulation in rats.

Sakloth, Farhana / Negus, S Stevens

Experimental and clinical psychopharmacology

2018 Volume 26, Issue 2, Page(s) 195–204

Abstract: Pharmacotherapy to treat stimulant use disorders continues to be an unmet medical need. Some evidence supports both the role of opioids in mediating abuse-related amphetamine effects and the potential utility of opioid antagonists as therapeutic ... ...

Abstract	Pharmacotherapy to treat stimulant use disorders continues to be an unmet medical need. Some evidence supports both the role of opioids in mediating abuse-related amphetamine effects and the potential utility of opioid antagonists as therapeutic candidates for treating amphetamine abuse. This study used intracranial self-stimulation (ICSS) to evaluate effects of exposure to and termination of naltrexone maintenance on rewarding amphetamine effects in an ICSS procedure in rats. Morphine and cocaine were included as positive and negative controls, respectively. Male Sprague-Dawley rats (N = 40) were trained to lever press for electrical brain stimulation to the medial forebrain bundle via an implanted electrode. Rats were then implanted with osmotic pumps delivering naltrexone (0.001 mg/kg/h, SC, 0.01 mg/kg/h, SC, or 0.1 mg/kg/h, SC) or saline for 14 days. Cumulative dose-effect curves were determined for amphetamine (0.032 mg/kg to 0.32 mg/kg), cocaine (1 mg/kg to 10 mg/kg), and morphine (1 mg/kg to 10 mg/kg) during the 2nd week of naltrexone maintenance. Additionally, dose-effect curves for morphine and amphetamine were determined again 24 hr after pump removal. Our results suggest that (a) exposure to and termination of naltrexone maintenance do not affect baseline ICSS responding, (b) naltrexone doses sufficient to antagonize morphine did not alter amphetamine or cocaine effects, and (c) termination of naltrexone treatment produced weak evidence for increased morphine sensitivity but no change in amphetamine effects. Our results do not support naltrexone as a pharmacotherapy for amphetamine and cocaine abuse and also suggest that termination from chronic naltrexone does not increase sensitivity to abuse-related morphine or amphetamine effects in ICSS. (PsycINFO Database Record
MeSH term(s)	Amphetamine/pharmacology ; Animals ; Central Nervous System Stimulants/pharmacology ; Cocaine/pharmacology ; Deep Brain Stimulation/methods ; Dose-Response Relationship, Drug ; Male ; Medial Forebrain Bundle/drug effects ; Morphine/pharmacology ; Naltrexone/pharmacology ; Narcotic Antagonists/pharmacology ; Narcotics/pharmacology ; Rats ; Rats, Sprague-Dawley ; Self Stimulation/drug effects ; Self Stimulation/physiology ; Substance-Related Disorders/physiopathology ; Substance-Related Disorders/therapy
Chemical Substances	Central Nervous System Stimulants ; Narcotic Antagonists ; Narcotics ; Naltrexone (5S6W795CQM) ; Morphine (76I7G6D29C) ; Amphetamine (CK833KGX7E) ; Cocaine (I5Y540LHVR)
Language	English
Publishing date	2018-03-12
Publishing country	United States
Document type	Journal Article ; Research Support, N.I.H., Extramural
ZDB-ID	1209960-0
ISSN	1936-2293 ; 1064-1297
ISSN (online)	1936-2293
ISSN	1064-1297
DOI	10.1037/pha0000183
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Article ; Online: Regulators of G Protein Signaling in Analgesia and Addiction.

Sakloth, Farhana / Polizu, Claire / Bertherat, Feodora / Zachariou, Venetia

Molecular pharmacology

2020 Volume 98, Issue 6, Page(s) 739–750

Abstract: Regulator of G protein signaling (RGS) proteins are multifunctional proteins expressed in peripheral and neuronal cells, playing critical roles in development, physiologic processes, and pharmacological responses. RGS proteins primarily act as GTPase ... ...

Abstract	Regulator of G protein signaling (RGS) proteins are multifunctional proteins expressed in peripheral and neuronal cells, playing critical roles in development, physiologic processes, and pharmacological responses. RGS proteins primarily act as GTPase accelerators for activated G
MeSH term(s)	Analgesia/methods ; Analgesics, Opioid/administration & dosage ; Analgesics, Opioid/adverse effects ; Animals ; Brain/cytology ; Brain/drug effects ; Brain/physiology ; Disease Models, Animal ; Dopamine/metabolism ; Drug Tolerance/physiology ; GTP-Binding Proteins/metabolism ; Humans ; Neuronal Plasticity/drug effects ; Neuronal Plasticity/physiology ; Neurons/drug effects ; Neurons/metabolism ; Nociception/drug effects ; Nociception/physiology ; Psychotropic Drugs/adverse effects ; RGS Proteins/metabolism ; Signal Transduction/drug effects ; Signal Transduction/physiology ; Substance-Related Disorders/etiology ; Substance-Related Disorders/physiopathology
Chemical Substances	Analgesics, Opioid ; Psychotropic Drugs ; RGS Proteins ; GTP-Binding Proteins (EC 3.6.1.-) ; Dopamine (VTD58H1Z2X)
Language	English
Publishing date	2020-05-30
Publishing country	United States
Document type	Journal Article ; Research Support, N.I.H., Extramural ; Review
ZDB-ID	124034-1
ISSN	1521-0111 ; 0026-895X
ISSN (online)	1521-0111
ISSN	0026-895X
DOI	10.1124/mol.119.119206
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Article ; Online: Tianeptine promotes lasting antiallodynic effects in a mouse model of neuropathic pain.

Serafini, Randal A / Estill, Molly / Pekarskaya, Elizabeth A / Sakloth, Farhana / Shen, Li / Javitch, Jonathan A / Zachariou, Venetia

Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology

2023 Volume 48, Issue 11, Page(s) 1680–1689

Abstract: Tricyclic antidepressants (TCAs), such as desipramine (DMI), are effective at managing neuropathic pain symptoms but often take several weeks to become effective and also lead to considerable side effects. Tianeptine (TIAN) is an atypical antidepressant ... ...

Abstract	Tricyclic antidepressants (TCAs), such as desipramine (DMI), are effective at managing neuropathic pain symptoms but often take several weeks to become effective and also lead to considerable side effects. Tianeptine (TIAN) is an atypical antidepressant that activates the mu-opioid receptor but does not produce analgesic tolerance or withdrawal in mice, nor euphoria in humans, at clinically-relevant doses. Here, we evaluate the efficacy of TIAN at persistently alleviating mechanical allodynia in the spared nerve injury (SNI) model of neuropathic pain, even well after drug clearance. After finding an accelerated onset of antiallodynic action compared to DMI, we used genetically modified mice to gain insight into RGS protein-associated pathways that modulate the efficacy of TIAN relative to DMI in models of neuropathic pain. Because we observed similar behavioral responses to both TIAN and DMI treatment in RGS4, RGSz1, and RGS9 knockout mice, we performed RNA sequencing on the NAc of TIAN- and DMI-treated mice after prolonged SNI to further clarify potential mechanisms underlying TIANs faster therapeutic actions. Our bioinformatic analysis revealed distinct transcriptomic signatures between the two drugs, with TIAN more directly reversing SNI-induced differentially expressed genes, and further predicted several upstream regulators that may be implicated in onset of action. This new understanding of the molecular pathways underlying TIAN action may enable the development of novel and more efficacious pharmacological approaches for the management of neuropathic pain.
MeSH term(s)	Humans ; Mice ; Animals ; Neuralgia/drug therapy ; Antidepressive Agents/therapeutic use ; Hyperalgesia/drug therapy ; Antidepressive Agents, Tricyclic/pharmacology ; Antidepressive Agents, Tricyclic/therapeutic use ; Disease Models, Animal
Chemical Substances	tianeptine (0T493YFU8O) ; Antidepressive Agents ; Antidepressive Agents, Tricyclic
Language	English
Publishing date	2023-07-20
Publishing country	England
Document type	Journal Article ; Research Support, N.I.H., Extramural ; Research Support, Non-U.S. Gov't
ZDB-ID	639471-1
ISSN	1740-634X ; 0893-133X
ISSN (online)	1740-634X
ISSN	0893-133X
DOI	10.1038/s41386-023-01645-w
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Article ; Online: Author Correction: Oxycodone withdrawal induces HDAC1/HDAC2-dependent transcriptional maladaptations in the reward pathway in a mouse model of peripheral nerve injury.

Nature neuroscience

2024 Volume 27, Issue 2, Page(s) 384

Language	English
Publishing date	2024-01-22
Publishing country	United States
Document type	Published Erratum
ZDB-ID	1420596-8
ISSN	1546-1726 ; 1097-6256
ISSN (online)	1546-1726
ISSN	1097-6256
DOI	10.1038/s41593-024-01579-6
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Article ; Online: Effects of acute and repeated treatment with serotonin 5-HT2A receptor agonist hallucinogens on intracranial self-stimulation in rats.

Sakloth, Farhana / Leggett, Elizabeth / Moerke, Megan J / Townsend, E Andrew / Banks, Matthew L / Negus, S Stevens

Experimental and clinical psychopharmacology

2019 Volume 27, Issue 3, Page(s) 215–226

Abstract: The prototype 5-HT2A receptor agonist hallucinogens LSD, mescaline, and psilocybin are classified as Schedule 1 drugs of abuse by the U.S. Drug Enforcement Administration. Accumulating clinical evidence has also suggested that acute or repeated " ... ...

Abstract	The prototype 5-HT2A receptor agonist hallucinogens LSD, mescaline, and psilocybin are classified as Schedule 1 drugs of abuse by the U.S. Drug Enforcement Administration. Accumulating clinical evidence has also suggested that acute or repeated "microdosing" with these drugs may have utility for treatment of some mental health disorders, including drug abuse and depression. The goal of the present study was to evaluate LSD, mescaline, and psilocybin effects on intracranial self-stimulation (ICSS), a procedure that has been used to evaluate abuse-related effects of other classes of abused drugs. Effects of repeated LSD were also examined to evaluate potential changes in its own effects on ICSS or changes in effects produced by the abused psychostimulant methamphetamine or the prodepressant kappa opioid receptor (KOR) agonist U69,593. Male Sprague-Dawley rats were implanted with microelectrodes targeting the medial forebrain bundle and trained to respond under a "frequency-rate" ICSS procedure, in which many drugs of abuse increase (or "facilitate") ICSS. In acute dose-effect and time-course studies, evidence for abuse-related ICSS facilitation was weak and inconsistent; the predominant effect of all 3 drugs was dose- and time-dependent ICSS depression. Repeated LSD treatment failed to alter either its own ICSS depressant effects or the abuse-related effects of methamphetamine; however, repeated LSD did attenuate ICSS depression by U69,593. These results extend those of previous preclinical studies to suggest weak expression of abuse-related effects by 5-HT2A agonist hallucinogens and provide supportive evidence for therapeutic effects of repeated LSD dosing to attenuate KOR-mediated depressant effects but not abuse potential of psychostimulants. (PsycINFO Database Record (c) 2019 APA, all rights reserved).
MeSH term(s)	Analgesics, Opioid/pharmacology ; Animals ; Dose-Response Relationship, Drug ; Hallucinogens/pharmacology ; Male ; Medial Forebrain Bundle/drug effects ; Rats ; Rats, Sprague-Dawley ; Receptor, Serotonin, 5-HT2A/drug effects ; Receptors, Opioid, kappa/agonists ; Self Stimulation/drug effects ; Serotonin 5-HT2 Receptor Agonists/pharmacology
Chemical Substances	Analgesics, Opioid ; Hallucinogens ; Receptor, Serotonin, 5-HT2A ; Receptors, Opioid, kappa ; Serotonin 5-HT2 Receptor Agonists
Language	English
Publishing date	2019-01-10
Publishing country	United States
Document type	Journal Article
ZDB-ID	1209960-0
ISSN	1936-2293 ; 1064-1297
ISSN (online)	1936-2293
ISSN	1064-1297
DOI	10.1037/pha0000253
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Article ; Online: A Regional and Projection-Specific Role of RGSz1 in the Ventrolateral Periaqueductal Grey in the Modulation of Morphine Reward.

Sakloth, Farhana / Sanchez-Reyes, Omar B / Ruiz, Anne / Nicolais, Andrew / Serafini, Randal A / Pryce, Kerri D / Bertherat, Feodora / Torres-Berrío, Angélica / Gomes, Ivone / Devi, Lakshmi A / Wacker, Daniel / Zachariou, Venetia

Molecular pharmacology

2022 Volume 103, Issue 1, Page(s) 1–8

Abstract: Opioid analgesics exert their therapeutic and adverse effects by ... ...

Abstract	Opioid analgesics exert their therapeutic and adverse effects by activating
MeSH term(s)	Mice ; Animals ; Morphine/pharmacology ; Morphine/metabolism ; Analgesics, Opioid/pharmacology ; Analgesics, Opioid/metabolism ; Periaqueductal Gray/metabolism ; Signal Transduction ; GTP-Binding Proteins/metabolism ; Reward ; Receptors, Opioid, mu/metabolism
Chemical Substances	Morphine (76I7G6D29C) ; Analgesics, Opioid ; GTP-Binding Proteins (EC 3.6.1.-) ; Receptors, Opioid, mu
Language	English
Publishing date	2022-10-30
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't ; Research Support, N.I.H., Extramural
ZDB-ID	124034-1
ISSN	1521-0111 ; 0026-895X
ISSN (online)	1521-0111
ISSN	0026-895X
DOI	10.1124/molpharm.122.000528
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Article ; Online: Investigation of the Optical Isomers of Methcathinone, and Two Achiral Analogs, at Monoamine Transporters and in Intracranial Self-Stimulation Studies in Rats.

Davies, Rachel A / Baird, Tyson R / Nguyen, Vy T / Ruiz, Brian / Sakloth, Farhana / Eltit, Jose M / Negus, S Stevens / Glennon, Richard A

ACS chemical neuroscience

2020 Volume 11, Issue 12, Page(s) 1762–1769

Abstract: Methcathinone (MCAT; ...

Abstract	Methcathinone (MCAT;
MeSH term(s)	Animals ; Dopamine Plasma Membrane Transport Proteins ; Norepinephrine Plasma Membrane Transport Proteins ; Propiophenones ; Rats ; Self Stimulation ; Serotonin Plasma Membrane Transport Proteins
Chemical Substances	Dopamine Plasma Membrane Transport Proteins ; Norepinephrine Plasma Membrane Transport Proteins ; Propiophenones ; Serotonin Plasma Membrane Transport Proteins ; monomethylpropion (386QA522QG)
Language	English
Publishing date	2020-05-27
Publishing country	United States
Document type	Journal Article ; Research Support, N.I.H., Extramural
ISSN	1948-7193
ISSN (online)	1948-7193
DOI	10.1021/acschemneuro.9b00617
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Article ; Online: Oxycodone withdrawal induces HDAC1/HDAC2-dependent transcriptional maladaptations in the reward pathway in a mouse model of peripheral nerve injury.

Nature neuroscience

2023 Volume 26, Issue 7, Page(s) 1229–1244

Abstract: The development of physical dependence and addiction disorders due to misuse of opioid analgesics is a major concern with pain therapeutics. We developed a mouse model of oxycodone exposure and subsequent withdrawal in the presence or absence of chronic ... ...

Abstract	The development of physical dependence and addiction disorders due to misuse of opioid analgesics is a major concern with pain therapeutics. We developed a mouse model of oxycodone exposure and subsequent withdrawal in the presence or absence of chronic neuropathic pain. Oxycodone withdrawal alone triggered robust gene expression adaptations in the nucleus accumbens, medial prefrontal cortex and ventral tegmental area, with numerous genes and pathways selectively affected by oxycodone withdrawal in mice with peripheral nerve injury. Pathway analysis predicted that histone deacetylase (HDAC) 1 is a top upstream regulator in opioid withdrawal in nucleus accumbens and medial prefrontal cortex. The novel HDAC1/HDAC2 inhibitor, Regenacy Brain Class I HDAC Inhibitor (RBC1HI), attenuated behavioral manifestations of oxycodone withdrawal, especially in mice with neuropathic pain. These findings suggest that inhibition of HDAC1/HDAC2 may provide an avenue for patients with chronic pain who are dependent on opioids to transition to non-opioid analgesics.
MeSH term(s)	Mice ; Animals ; Oxycodone/pharmacology ; Peripheral Nerve Injuries ; Narcotics ; Histone Deacetylase 1/metabolism ; Neuralgia ; Reward ; Analgesics, Opioid/pharmacology ; Histone Deacetylase 2/metabolism
Chemical Substances	Oxycodone (CD35PMG570) ; Narcotics ; Histone Deacetylase 1 (EC 3.5.1.98) ; Analgesics, Opioid ; Histone Deacetylase 2 (EC 3.5.1.98)
Language	English
Publishing date	2023-06-08
Publishing country	United States
Document type	Journal Article ; Research Support, N.I.H., Extramural
ZDB-ID	1420596-8
ISSN	1546-1726 ; 1097-6256
ISSN (online)	1546-1726
ISSN	1097-6256
DOI	10.1038/s41593-023-01350-3
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Article ; Online: HDAC6-selective inhibitors decrease nerve-injury and inflammation-associated mechanical hypersensitivity in mice.

Sakloth, Farhana / Manouras, Lefteris / Avrampou, Kleopatra / Mitsi, Vasiliki / Serafini, Randal A / Pryce, Kerri D / Cogliani, Valeria / Berton, Olivier / Jarpe, Matthew / Zachariou, Venetia

Psychopharmacology

2020 Volume 237, Issue 7, Page(s) 2139–2149

Abstract: Background: HDAC6 is a class IIB histone deacetylase expressed at many levels of the nociceptive pathway. This study tested the ability of novel and selective HDAC6 inhibitors to alleviate sensory hypersensitivity behaviors in mouse models of peripheral ...

Abstract	Background: HDAC6 is a class IIB histone deacetylase expressed at many levels of the nociceptive pathway. This study tested the ability of novel and selective HDAC6 inhibitors to alleviate sensory hypersensitivity behaviors in mouse models of peripheral nerve injury and peripheral inflammation. Methods: We utilized the murine spared nerve injury (SNI) model for peripheral nerve injury and the Complete Freund's Adjuvant (CFA) model of peripheral inflammation. We applied the Von Frey assay to monitor mechanical allodynia. Results: Using the SNI model, we demonstrate that daily administration of the brain-penetrant HDAC6 inhibitor, ACY-738, abolishes mechanical allodynia in male and in female mice. Importantly, there is no tolerance to the antiallodynic actions of these compounds as they produce a consistent increase in Von Frey thresholds for several weeks. We observed a similar antiallodynic effect when utilizing the HDAC6 inhibitor, ACY-257, which shows limited brain expression when administered systemically. We also demonstrate that ACY-738 and ACY-257 attenuate mechanical allodynia in the CFA model of peripheral inflammation. Conclusions: Overall, our findings suggest that inhibition of HDAC6 provides a promising therapeutic avenue for the alleviation of mechanical allodynia associated with peripheral nerve injury and peripheral inflammation.
MeSH term(s)	Animals ; Histone Deacetylase 6/antagonists & inhibitors ; Histone Deacetylase 6/metabolism ; Histone Deacetylase Inhibitors/pharmacology ; Histone Deacetylase Inhibitors/therapeutic use ; Hydroxamic Acids/pharmacology ; Hydroxamic Acids/therapeutic use ; Hyperalgesia/drug therapy ; Hyperalgesia/metabolism ; Inflammation/drug therapy ; Inflammation/metabolism ; Male ; Mice ; Mice, Inbred C57BL ; Pain Measurement/drug effects ; Pain Measurement/methods ; Pyrimidines/pharmacology ; Pyrimidines/therapeutic use ; Rats ; Rats, Sprague-Dawley
Chemical Substances	Histone Deacetylase Inhibitors ; Hydroxamic Acids ; N-hydroxy-2-(1-phenylcycloproylamino)pyrimidine-5-carboxamide ; Pyrimidines ; HDAC6 protein, human (EC 3.5.1.98) ; Histone Deacetylase 6 (EC 3.5.1.98)
Language	English
Publishing date	2020-05-09
Publishing country	Germany
Document type	Journal Article
ZDB-ID	130601-7
ISSN	1432-2072 ; 0033-3158
ISSN (online)	1432-2072
ISSN	0033-3158
DOI	10.1007/s00213-020-05525-9
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Article ; Online: A promising chemical series of positive allosteric modulators of the μ-opioid receptor that enhance the antinociceptive efficacy of opioids but not their adverse effects.

Pryce, Kerri D / Kang, Hye Jin / Sakloth, Farhana / Liu, Yongfeng / Khan, Susan / Toth, Katalin / Kapoor, Abhijeet / Nicolais, Andrew / Che, Tao / Qin, Lihuai / Bertherat, Feodora / Kaniskan, H Ümit / Jin, Jian / Cameron, Michael D / Roth, Bryan L / Zachariou, Venetia / Filizola, Marta

Neuropharmacology

2021 Volume 195, Page(s) 108673

Abstract: Positive allosteric modulators (PAMs) of the μ-opioid receptor (MOR) have been proposed to exhibit therapeutic potential by maximizing the analgesic properties of clinically used opioid drugs while limiting their adverse effects or risk of overdose as a ... ...

Abstract	Positive allosteric modulators (PAMs) of the μ-opioid receptor (MOR) have been proposed to exhibit therapeutic potential by maximizing the analgesic properties of clinically used opioid drugs while limiting their adverse effects or risk of overdose as a result of using lower drug doses. We herein report in vitro and in vivo characterization of two small molecules from a chemical series of MOR PAMs that exhibit: (i) MOR PAM activity and receptor subtype selectivity in vitro, (ii) a differential potentiation of the antinociceptive effect of oxycodone, morphine, and methadone in mouse models of pain that roughly correlates with in vitro activity, and (iii) a lack of potentiation of adverse effects associated with opioid administration, such as somatic withdrawal, respiratory depression, and analgesic tolerance. This series of MOR PAMs holds promise for the development of adjuncts to opioid therapy to mitigate against overdose and opioid use disorders.
MeSH term(s)	Allosteric Regulation ; Analgesics/pharmacology ; Analgesics/therapeutic use ; Animals ; Female ; Male ; Mice ; Nociception/drug effects ; Pain/drug therapy ; Pain/metabolism ; Pain Measurement ; Pain Threshold/drug effects ; Receptors, Opioid, mu
Chemical Substances	Analgesics ; Receptors, Opioid, mu
Language	English
Publishing date	2021-06-18
Publishing country	England
Document type	Journal Article ; Research Support, N.I.H., Extramural
ZDB-ID	218272-5
ISSN	1873-7064 ; 0028-3908
ISSN (online)	1873-7064
ISSN	0028-3908
DOI	10.1016/j.neuropharm.2021.108673
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