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Book ; Online ; E-Book: The kappa opioid receptor

Liu-Chen, Lee-Yuan / Inan, Saadet

(Handbook of experimental pharmacology ; 271)

2022

Author's details	Lee-Yuan Liu-Chen, Saadet Inan editors
Series title	Handbook of experimental pharmacology ; 271
Collection
Keywords	Electronic books
Language	English
Size	1 Online-Ressource (xi, 577 Seiten), Illustrationen, Diagramme
Publisher	Springer
Publishing place	Cham
Publishing country	Switzerland
Document type	Book ; Online ; E-Book
Remark	Zugriff für angemeldete ZB MED-Nutzerinnen und -Nutzer
HBZ-ID	HT021202506
ISBN	978-3-030-89074-2 ; 9783030890735 ; 3-030-89074-0 ; 3030890732
DOI	10.1007/978-3-030-89074-2
Database	ZB MED Catalogue: Medicine, Health, Nutrition, Environment, Agriculture

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Article: Kappa Opioid Agonist-Induced Diuresis: Characteristics, Mechanisms, and Beyond.

Inan, Saadet

Handbook of experimental pharmacology

2021 Volume 271, Page(s) 401–417

Abstract: Activation of the kappa opioid receptor (KOR) induces antinociception, anti-pruritic activity, diuresis, sedation, and dysphoria. KOR agonist-induced diuresis is characterized as water diuresis, in which water excretion with urine is increased without ... ...

Abstract	Activation of the kappa opioid receptor (KOR) induces antinociception, anti-pruritic activity, diuresis, sedation, and dysphoria. KOR agonist-induced diuresis is characterized as water diuresis, in which water excretion with urine is increased without altering electrolyte excretion. Both centrally and peripherally acting KOR agonists promote diuresis. KOR antagonists block KOR agonist-evoked diuresis suggesting that the diuretic effect is through activation of the KOR. Studies in different experimental animal species and in humans indicate that KOR agonists decrease antidiuretic hormone (ADH) secretion and release from the hypothalamus and posterior pituitary; decrease response to ADH in kidneys; increase renal sympathetic nerve activity; and increase adrenaline, noradrenaline, and dopamine release from the adrenal medulla. The therapeutic potentials of KOR agonists as water diuretics have been studied in animal models of cerebral edema due to ischemia and intracranial mass, hypertension, and cirrhosis. This chapter reviews characteristics, possible mechanisms, as well as therapeutic potentials of KOR agonist-induced diuresis.
MeSH term(s)	Analgesics, Opioid/pharmacology ; Animals ; Diuresis ; Dopamine ; Humans ; Narcotic Antagonists ; Receptors, Opioid, kappa
Chemical Substances	Analgesics, Opioid ; Narcotic Antagonists ; Receptors, Opioid, kappa ; Dopamine (VTD58H1Z2X)
Language	English
Publishing date	2021-01-21
Publishing country	Germany
Document type	Journal Article
ISSN	0171-2004
ISSN	0171-2004
DOI	10.1007/164_2020_399
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Article: Alan Cowan: Buprenorphine from the bench to the bedside-Personal notes.

Inan, Saadet / Guarnieri, Michael

Journal of opioid management

2021 Volume 17, Issue 7, Page(s) 5–7

MeSH term(s)	Analgesics, Opioid/adverse effects ; Buprenorphine/adverse effects ; Humans
Chemical Substances	Analgesics, Opioid ; Buprenorphine (40D3SCR4GZ)
Language	English
Publishing date	2021-09-14
Publishing country	United States
Document type	Journal Article
ZDB-ID	2397614-7
ISSN	1551-7489
ISSN	1551-7489
DOI	10.5055/jom.2021.0637
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Article ; Online: Clues from planarians about interleukin-17A and stress that result from light avoidance: IL-17A antagonists reduce defensive responding in flatworms.

Milton, Mia / Inan, Saadet / Rawls, Scott M

Cytokine

2023 Volume 170, Page(s) 156345

Abstract: Emerging evidence links interleukin-17A (IL-17A) to anxiety and stress. Circulating levels of IL-17A are elevated in patients with anxiety disorders, and pharmacological blockade of IL-17 signaling or genetic deletion of IL-17 reduces anxiety-like ... ...

Abstract	Emerging evidence links interleukin-17A (IL-17A) to anxiety and stress. Circulating levels of IL-17A are elevated in patients with anxiety disorders, and pharmacological blockade of IL-17 signaling or genetic deletion of IL-17 reduces anxiety-like behaviors in mice. Given that IL-17 is one of the most conserved cytokines among animal phyla, we tested the hypothesis that anti-IL-17 treatments reduce defensive responding in planarians, the simplest animal with bilateral symmetry and a CNS with cephalization. The endpoint selected was light avoidance, which is a common phenotype of planarians and rodents and an index of defensive responding that is reduced by anxiolytic compounds in both species. Planarians were placed at the midline of a Petri dish containing water or test solution that was equally split into light and dark halves. Planarians exposed to a selective IL-17A antibody (0.1, 1, 10 pM) over a 5-min interval spent more time in the light than water-exposed planarians. Cyanidin (0.01, 0.1 1, 10 µM), an anti-inflammatory flavonoid and non-selective IL-17A inhibitor, also increased time spent in the light. Motility was not affected by IL-17A antibody or cyanidin at concentrations that reduced light avoidance, although higher concentrations reduced motility (>10 µM). Our results show that IL-17A antagonists reduce defensive responding in planarians and suggest conservation of IL-17A effects on aspects of anxiety-related behaviors.
MeSH term(s)	Animals ; Mice ; Antibodies ; Anxiety/drug therapy ; Interleukin-17/antagonists & inhibitors ; Planarians ; Water ; Stress, Psychological
Chemical Substances	Antibodies ; Interleukin-17 ; Water (059QF0KO0R)
Language	English
Publishing date	2023-08-23
Publishing country	England
Document type	Journal Article ; Research Support, N.I.H., Extramural
ZDB-ID	1018055-2
ISSN	1096-0023 ; 1043-4666
ISSN (online)	1096-0023
ISSN	1043-4666
DOI	10.1016/j.cyto.2023.156345
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Article ; Online: Oxycodone: A Current Perspective on Its Pharmacology, Abuse, and Pharmacotherapeutic Developments.

Barrett, James E / Shekarabi, Aryan / Inan, Saadet

Pharmacological reviews

2023 Volume 75, Issue 6, Page(s) 1062–1118

Abstract: Oxycodone, a semisynthetic derivative of naturally occurring thebaine, an opioid alkaloid, has been available for more than 100 years. Although thebaine cannot be used therapeutically due to the occurrence of convulsions at higher doses, it has been ... ...

Abstract	Oxycodone, a semisynthetic derivative of naturally occurring thebaine, an opioid alkaloid, has been available for more than 100 years. Although thebaine cannot be used therapeutically due to the occurrence of convulsions at higher doses, it has been converted to a number of other widely used compounds that include naloxone, naltrexone, buprenorphine, and oxycodone. Despite the early identification of oxycodone, it was not until the 1990s that clinical studies began to explore its analgesic efficacy. These studies were followed by the pursuit of several preclinical studies to examine the analgesic effects and abuse liability of oxycodone in laboratory animals and the subjective effects in human volunteers. For a number of years oxycodone was at the forefront of the opioid crisis, playing a significant role in contributing to opioid misuse and abuse, with suggestions that it led to transitioning to other opioids. Several concerns were expressed as early as the 1940s that oxycodone had significant abuse potential similar to heroin and morphine. Both animal and human abuse liability studies have confirmed, and in some cases amplified, these early warnings. Despite sharing a similar structure with morphine and pharmacological actions also mediated by the
MeSH term(s)	Animals ; Humans ; Oxycodone/adverse effects ; Thebaine/therapeutic use ; Analgesics, Opioid/adverse effects ; Opioid-Related Disorders/drug therapy ; Morphine/therapeutic use ; Receptors, Opioid/therapeutic use
Chemical Substances	Oxycodone (CD35PMG570) ; Thebaine (2P9MKG8GX7) ; Analgesics, Opioid ; Morphine (76I7G6D29C) ; Receptors, Opioid
Language	English
Publishing date	2023-06-15
Publishing country	United States
Document type	Journal Article ; Review
ZDB-ID	209898-2
ISSN	1521-0081 ; 0031-6997
ISSN (online)	1521-0081
ISSN	0031-6997
DOI	10.1124/pharmrev.121.000506
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Article: Antipruritic Effects of Kappa Opioid Receptor Agonists: Evidence from Rodents to Humans.

Inan, Saadet / Cowan, Alan

Handbook of experimental pharmacology

2020 Volume 271, Page(s) 275–292

Abstract: Centrally administered bombesin induces scratching and grooming in rats. These behaviors were blocked by early benzomorphan kappa opioid receptor (KOR) agonists as reported by Gmerek and Cowan in 1984. This was the first evidence that KORs may be ... ...

Abstract	Centrally administered bombesin induces scratching and grooming in rats. These behaviors were blocked by early benzomorphan kappa opioid receptor (KOR) agonists as reported by Gmerek and Cowan in 1984. This was the first evidence that KORs may be involved in the sensation of itch-like behaviors. Subsequent development of additional animal models for acute and chronic itch has led to important discoveries since then. For example, it was found that (a) gastrin-releasing peptide (GRP), natriuretic polypeptide b and their cognate receptors are keys for the transmission of itch sensation at the spinal cord level, (b) dynorphins (Dyns), the endogenous KOR agonists, work as inhibitory neuromodulators of itch at the spinal cord level, (c) in a mouse model for acute itch, certain KOR antagonists elicit scratching, (d) in mouse models of acute or chronic itch, KOR agonists (e.g., U50,488, nalfurafine, CR 845, nalbuphine) suppress scratching induced by different pruritogens, and (e) nalfurafine, CR 845, and nalbuphine are in the clinic or in clinical trials for pruritus associated with chronic kidney disease and chronic liver disease, as well as pruritus in chronic skin diseases.
MeSH term(s)	Animals ; Antipruritics/pharmacology ; Humans ; Mice ; Narcotic Antagonists/pharmacology ; Pruritus/drug therapy ; Rats ; Receptors, Opioid, kappa/agonists ; Rodentia
Chemical Substances	Antipruritics ; Narcotic Antagonists ; Receptors, Opioid, kappa
Language	English
Publishing date	2020-12-09
Publishing country	Germany
Document type	Journal Article
ISSN	0171-2004
ISSN	0171-2004
DOI	10.1007/164_2020_420
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Article ; Online: Blocking IL-17A prevents oxycodone-induced depression-like effects and elevation of IL-6 levels in the ventral tegmental area and reduces oxycodone-derived physical dependence in rats.

Inan, Saadet / Meissler, Joseph J / Bessho, Shingo / Wiah, Sonita / Tukel, Cagla / Eisenstein, Toby K / Rawls, Scott M

Brain, behavior, and immunity

2024 Volume 117, Page(s) 100–111

Abstract: Oxycodone is the most prescribed opioid for pain management and has been available in clinics for almost a century, but effects of chronic oxycodone have been studied less than morphine in preclinical and clinical studies. Newly developed depression has ... ...

Abstract	Oxycodone is the most prescribed opioid for pain management and has been available in clinics for almost a century, but effects of chronic oxycodone have been studied less than morphine in preclinical and clinical studies. Newly developed depression has been coupled with chronic oxycodone use in a few clinical studies, but no preclinical studies have investigated the pathogenesis of oxycodone-induced depression. Gut microbiome changes following oxycodone use is an understudied area, and interleukin-17A (IL-17A) is linked to both the development of mood disorders and regulation of gut microbiome. The present study investigated effects of chronic oxycodone exposure on mood-related behaviors (depression and anxiety), pain hypersensitivity, physical dependence, immune markers, and the gut microbiome and tested the hypothesis that blocking IL-17A with a systemically administered monoclonal antibody reduces oxycodone-derived effects. Oxycodone (using an incremental dosing regimen) or saline was injected twice a day for 12 days. IL-17A Ab (200 µg/100 µl) or saline was administered every 3rd day during the 12-day interval. Chronic oxycodone induced a depression-like effect, but not anxiogenic- or anxiolytic-like effects; promoted hyperalgesia; increased IL-17A and IL-6 levels in the ventral tegmental area (VTA); and induced physical dependence. IL-17A Ab co-administration with oxycodone prevented the depression-like effect and hyperalgesia, reduced naloxone-precipitated withdrawal signs, and normalized the increase in cytokine levels. Chronic oxycodone exposure did not affect gut microbiome and integrity. Our results identify a role for IL-17A in oxycodone-related behavioral and neuroimmune effects and show that IL-17A Ab has potential therapeutic value in blocking these effects. Given that humanized IL-17A Ab is approved for treatment of psoriasis and psoriatic arthritis, our findings point toward studying it for use in the treatment of oxycodone use disorder.
MeSH term(s)	Rats ; Animals ; Oxycodone/pharmacology ; Ventral Tegmental Area ; Interleukin-17/metabolism ; Interleukin-6/pharmacology ; Depression/drug therapy ; Hyperalgesia/drug therapy ; Substance-Related Disorders
Chemical Substances	Oxycodone (CD35PMG570) ; Interleukin-17 ; Interleukin-6
Language	English
Publishing date	2024-01-08
Publishing country	Netherlands
Document type	Journal Article ; Research Support, N.I.H., Extramural ; Research Support, Non-U.S. Gov't
ZDB-ID	639219-2
ISSN	1090-2139 ; 0889-1591
ISSN (online)	1090-2139
ISSN	0889-1591
DOI	10.1016/j.bbi.2024.01.001
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Zs.A 2276: Show issues			Location: Je nach Verfügbarkeit (siehe Angabe bei Bestand) bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular Jg. 1995 - 2021: Lesesall (2.OG) ab Jg. 2022: Lesesaal (EG)
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Article ; Online: Epicutaneous Sensitization to the Phytocannabinoid β-Caryophyllene Induces Pruritic Inflammation.

Inan, Saadet / Ward, Sara J / Baltazar, Citlalli T / Peruggia, Gabrielle A / Javed, Elham / Nayak, Ajay P

International journal of molecular sciences

2023 Volume 24, Issue 18

Abstract: In recent years, there has been increased accessibility to cannabis for recreational and medicinal use. Incidentally, there has been an increase in reports describing allergic reactions to cannabis including exacerbation of underlying asthma. Recently, ... ...

Abstract	In recent years, there has been increased accessibility to cannabis for recreational and medicinal use. Incidentally, there has been an increase in reports describing allergic reactions to cannabis including exacerbation of underlying asthma. Recently, multiple protein allergens were discovered in cannabis, yet these fail to explain allergic sensitization in many patients, particularly urticaria and angioedema. Cannabis has a rich chemical profile including cannabinoids and terpenes that possess immunomodulatory potential. We examined whether major cannabinoids of cannabis such as cannabidiol (CBD) and the bicyclic sesquiterpene beta-caryophyllene (β-CP) act as contact sensitizers. The repeated topical application of mice skin with β-CP at 10 mg/mL (50 µL) induced an itch response and dermatitis at 2 weeks in mice, which were sustained for the period of study. Histopathological analysis of skin tissues revealed significant edema and desquamation for β-CP at 10 mg/mL. For CBD and β-CP, we observed a dose-dependent increase in epidermal thickening with profound thickening observed for β-CP at 10 mg/mL. Significant trafficking of CD11b cells was observed in various compartments of the skin in response to treatment with β-CP in a concentration-dependent manner. Mast cell trafficking was restricted to β-CP (10 mg/mL). Mouse proteome profiler cytokine/chemokine array revealed upregulation of complement C5/5a (anaphylatoxin), soluble intracellular adhesion molecule-1 (sICAM-1) and IL-1 receptor antagonist (IL-1RA) in animals dosed with β-CP (10 mg/mL). Moreover, we observed a dose-dependent increase in serum IgE in animals dosed with β-CP. Treatment with β-CP (10 mg/mL) significantly reduced filaggrin expression, an indicator of barrier disruption. In contrast, treatment with CBD at all concentrations failed to evoke scratching and dermatitis in mice and did not result in increased serum IgE. Further, skin tissues were devoid of any remarkable features, although at 10 mg/mL CBD we did observe the accumulation of dermal CD11b cells in skin tissue sections. We also observed increased filaggrin staining in mice repeatedly dosed with CBD (10 mg/mL). Collectively, our studies indicate that repeated exposure to high concentrations of β-CP can induce dermatitis-like pathological outcomes in mice.
MeSH term(s)	Humans ; Animals ; Mice ; Filaggrin Proteins ; Inflammation/chemically induced ; Hallucinogens ; Cannabis ; Angioedema ; Cannabidiol ; Cannabinoid Receptor Agonists ; Pruritus ; Complement C5 ; Complement C5a ; Dermatitis ; Immunoglobulin E
Chemical Substances	caryophyllene (BHW853AU9H) ; Filaggrin Proteins ; Hallucinogens ; Cannabidiol (19GBJ60SN5) ; Cannabinoid Receptor Agonists ; Complement C5 ; Complement C5a (80295-54-1) ; Immunoglobulin E (37341-29-0)
Language	English
Publishing date	2023-09-20
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2019364-6
ISSN	1422-0067 ; 1422-0067 ; 1661-6596
ISSN (online)	1422-0067
ISSN	1422-0067 ; 1661-6596
DOI	10.3390/ijms241814328
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Article ; Online: Antipruritic Effect of Nalbuphine, a Kappa Opioid Receptor Agonist, in Mice: A Pan Antipruritic.

Inan, Saadet / Dun, Nae J / Cowan, Alan

Molecules (Basel, Switzerland)

2021 Volume 26, Issue 18

Abstract: Antipruritic effects of kappa opioid receptor (KOR) agonists have been shown in rodent models of acute and chronic scratching (itchlike behavior). Three KOR agonists, nalfurafine, difelikefalin, and nalbuphine, are in clinical studies for antipruritic ... ...

Abstract	Antipruritic effects of kappa opioid receptor (KOR) agonists have been shown in rodent models of acute and chronic scratching (itchlike behavior). Three KOR agonists, nalfurafine, difelikefalin, and nalbuphine, are in clinical studies for antipruritic effects in chronic itch of systemic and skin diseases. Nalfurafine (in Japan) and difelikefalin (in the USA) were approved to be used in the treatment of chronic itch in hemodialysis patients. The FDA-approved nalbuphine has been used in clinic for over 40 years, and it is the only narcotic agonist that is not scheduled. We aimed to study (a) antiscratch activity of nalbuphine against TAT-HIV-1 protein (controls HIV transcription)-, deoxycholic acid (DCA, bile acid)-, and chloroquine (CQ)-induced scratching in a mouse model of acute itch; and (b) whether the effect of nalbuphine is produced via KORs. First, dose-responses were developed for pruritogens. Mice were pretreated with nalbuphine (0.3-10 mg/kg) and then a submaximal dose of pruritogens were administered and the number of scratching bouts was counted. To study if the antiscratch effect of nalbuphine is produced via KOR, we used KOR knock out mice and pharmacologic inhibition of KORs using nor-binaltorphimine, a KOR antagonist. For this aim, we used CQ as a pruritogen. We found that: (a) TAT-HIV-1 protein elicits scratching in a dose-dependent manner; (b) nalbuphine inhibits scratching induced by TAT-HIV-1, DCA, and CQ dose-dependently; and (c) nalbuphine inhibits scratching induced by CQ through KORs. In conclusion, nalbuphine inhibits scratching elicited by multiple pruritogens.
MeSH term(s)	Animals ; Antipruritics/pharmacology ; Antipruritics/therapeutic use ; Behavior, Animal/drug effects ; Chloroquine/toxicity ; Deoxycholic Acid/toxicity ; Disease Models, Animal ; Dose-Response Relationship, Drug ; Male ; Mice ; Nalbuphine/pharmacology ; Nalbuphine/therapeutic use ; Naltrexone/analogs & derivatives ; Naltrexone/pharmacology ; Naltrexone/therapeutic use ; Narcotic Antagonists/pharmacology ; Narcotic Antagonists/therapeutic use ; Pruritus/chemically induced ; Pruritus/prevention & control ; Receptors, Opioid, kappa/agonists ; Receptors, Opioid, kappa/antagonists & inhibitors ; Receptors, Opioid, kappa/genetics ; Receptors, Opioid, kappa/metabolism ; tat Gene Products, Human Immunodeficiency Virus/toxicity
Chemical Substances	Antipruritics ; Narcotic Antagonists ; Receptors, Opioid, kappa ; tat Gene Products, Human Immunodeficiency Virus ; Deoxycholic Acid (005990WHZZ) ; norbinaltorphimine (36OOQ86QM1) ; Naltrexone (5S6W795CQM) ; Chloroquine (886U3H6UFF) ; Nalbuphine (L2T84IQI2K)
Language	English
Publishing date	2021-09-11
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	1413402-0
ISSN	1420-3049 ; 1431-5165 ; 1420-3049
ISSN (online)	1420-3049
ISSN	1431-5165 ; 1420-3049
DOI	10.3390/molecules26185517
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Article ; Online: Antipruritic Effect of Nalbuphine, a Kappa Opioid Receptor Agonist, in Mice

Saadet Inan / Nae J. Dun / Alan Cowan

Molecules, Vol 26, Iss 5517, p

A Pan Antipruritic

2021 Volume 5517

Abstract	Antipruritic effects of kappa opioid receptor (KOR) agonists have been shown in rodent models of acute and chronic scratching (itchlike behavior). Three KOR agonists, nalfurafine, difelikefalin, and nalbuphine, are in clinical studies for antipruritic effects in chronic itch of systemic and skin diseases. Nalfurafine (in Japan) and difelikefalin (in the USA) were approved to be used in the treatment of chronic itch in hemodialysis patients. The FDA-approved nalbuphine has been used in clinic for over 40 years, and it is the only narcotic agonist that is not scheduled. We aimed to study (a) antiscratch activity of nalbuphine against TAT-HIV-1 protein (controls HIV transcription)-, deoxycholic acid (DCA, bile acid)-, and chloroquine (CQ)-induced scratching in a mouse model of acute itch; and (b) whether the effect of nalbuphine is produced via KORs. First, dose–responses were developed for pruritogens. Mice were pretreated with nalbuphine (0.3–10 mg/kg) and then a submaximal dose of pruritogens were administered and the number of scratching bouts was counted. To study if the antiscratch effect of nalbuphine is produced via KOR, we used KOR knock out mice and pharmacologic inhibition of KORs using nor-binaltorphimine, a KOR antagonist. For this aim, we used CQ as a pruritogen. We found that: (a) TAT-HIV-1 protein elicits scratching in a dose-dependent manner; (b) nalbuphine inhibits scratching induced by TAT-HIV-1, DCA, and CQ dose-dependently; and (c) nalbuphine inhibits scratching induced by CQ through KORs. In conclusion, nalbuphine inhibits scratching elicited by multiple pruritogens.
Keywords	nalbuphine ; kappa opioid receptor agonist ; pruritis ; scratching ; mice ; TAT-HIV ; Organic chemistry ; QD241-441
Subject code	616
Language	English
Publishing date	2021-09-01T00:00:00Z
Publisher	MDPI AG
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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