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  1. Article ; Online: WIN55212-2 Modulates Intracellular Calcium via CB

    Pulgar, Victor M / Howlett, Allyn C / Eldeeb, Khalil

    Cells

    2022  Volume 11, Issue 19

    Abstract: ... The ... ...

    Abstract The CB
    MeSH term(s) Benzoxazines ; Calcium/metabolism ; Calcium Channels/metabolism ; Fura-2 ; Humans ; Morpholines ; Naphthalenes ; Neuroblastoma ; Receptor, Cannabinoid, CB1/metabolism ; Receptors, Calcium-Sensing/metabolism ; Receptors, Cannabinoid/metabolism ; Rimonabant
    Chemical Substances Benzoxazines ; Calcium Channels ; Morpholines ; N-(2-hydroxy-3-(2-cyano-3-chlorophenoxy)propyl)-1,1-dimethyl-2-(2-nephthyl)ethylamine ; Naphthalenes ; Receptor, Cannabinoid, CB1 ; Receptors, Calcium-Sensing ; Receptors, Cannabinoid ; (3R)-((2,3-dihydro-5-methyl-3-((4-morpholinyl)methyl)pyrrolo-(1,2,3-de)-1,4-benzoxazin-6-yl)(1-naphthalenyl))methanone (5H31GI9502) ; Rimonabant (RML78EN3XE) ; Calcium (SY7Q814VUP) ; Fura-2 (TSN3DL106G)
    Language English
    Publishing date 2022-09-21
    Publishing country Switzerland
    Document type Journal Article ; Research Support, Non-U.S. Gov't ; Research Support, N.I.H., Extramural
    ZDB-ID 2661518-6
    ISSN 2073-4409 ; 2073-4409
    ISSN (online) 2073-4409
    ISSN 2073-4409
    DOI 10.3390/cells11192947
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article: Endocannabinoid System in Pregnancy Maintenance and Labor: A Mini-Review.

    Kozakiewicz, Melissa L / Grotegut, Chad A / Howlett, Allyn C

    Frontiers in endocrinology

    2021  Volume 12, Page(s) 699951

    Abstract: The endocannabinoid system (ECS) is a cell-signaling system present in multiple organ systems and is an integral part of sustaining the microenvironment necessary for early pregnancy success and maintenance. It plays a significant role in embryo ... ...

    Abstract The endocannabinoid system (ECS) is a cell-signaling system present in multiple organ systems and is an integral part of sustaining the microenvironment necessary for early pregnancy success and maintenance. It plays a significant role in embryo development, transport and implantation as well as placentation. The current theory behind the initiation of term labor is that it is a complex, multifactorial process involving sex steroid hormones, prostaglandin production and interplay at the maternal-fetal interface resulting in increased expression of receptors and gap junctions that promote uterine activation. There is increasing evidence that, in addition to early pregnancy events, the ECS plays a regulatory role in pregnancy maintenance and the timing of labor. This review presents an overview of the ECS in pregnancy that focuses on late gestation and parturition.
    MeSH term(s) Animals ; Embryo Implantation ; Embryonic Development ; Endocannabinoids/pharmacology ; Female ; Humans ; Pregnancy ; Pregnancy Maintenance ; Uterus/drug effects
    Chemical Substances Endocannabinoids
    Language English
    Publishing date 2021-06-16
    Publishing country Switzerland
    Document type Journal Article ; Research Support, N.I.H., Extramural ; Review
    ZDB-ID 2592084-4
    ISSN 1664-2392
    ISSN 1664-2392
    DOI 10.3389/fendo.2021.699951
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  3. Article ; Online: The Spicy Story of Cannabimimetic Indoles.

    Howlett, Allyn C / Thomas, Brian F / Huffman, John W

    Molecules (Basel, Switzerland)

    2021  Volume 26, Issue 20

    Abstract: The Sterling Research Group identified pravadoline as an aminoalkylindole (AAI) non-steroidal anti-inflammatory pain reliever. As drug design progressed, the ability of AAI analogs to block prostaglandin synthesis diminished, and antinociceptive activity ...

    Abstract The Sterling Research Group identified pravadoline as an aminoalkylindole (AAI) non-steroidal anti-inflammatory pain reliever. As drug design progressed, the ability of AAI analogs to block prostaglandin synthesis diminished, and antinociceptive activity was found to result from action at the CB
    MeSH term(s) Analgesics/chemistry ; Analgesics/pharmacology ; Animals ; Benzoxazines/pharmacology ; Binding Sites ; Biomimetic Materials/chemistry ; Biomimetic Materials/pharmacology ; Cannabinoids/chemistry ; Cannabinoids/pharmacology ; Designer Drugs/chemistry ; Designer Drugs/pharmacology ; Drug Design ; Humans ; Indoles/chemistry ; Indoles/pharmacology ; Ligands ; Morpholines/pharmacology ; Naphthalenes/pharmacology ; Receptor, Cannabinoid, CB1/agonists ; Receptor, Cannabinoid, CB1/chemistry ; Receptor, Cannabinoid, CB2/agonists ; Receptor, Cannabinoid, CB2/chemistry ; Static Electricity ; Structure-Activity Relationship
    Chemical Substances Analgesics ; Benzoxazines ; Cannabinoids ; Designer Drugs ; Indoles ; Ligands ; Morpholines ; Naphthalenes ; Receptor, Cannabinoid, CB1 ; Receptor, Cannabinoid, CB2 ; (3R)-((2,3-dihydro-5-methyl-3-((4-morpholinyl)methyl)pyrrolo-(1,2,3-de)-1,4-benzoxazin-6-yl)(1-naphthalenyl))methanone (5H31GI9502) ; pravadoline (P3JW662TWA)
    Language English
    Publishing date 2021-10-14
    Publishing country Switzerland
    Document type Journal Article ; Review
    ZDB-ID 1413402-0
    ISSN 1420-3049 ; 1431-5165 ; 1420-3049
    ISSN (online) 1420-3049
    ISSN 1431-5165 ; 1420-3049
    DOI 10.3390/molecules26206190
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  4. Article: CB

    Dalton, George D / Carney, Skyla T / Marshburn, Jamie D / Norford, Derek C / Howlett, Allyn C

    Frontiers in cellular neuroscience

    2020  Volume 14, Page(s) 176

    Abstract: ... ...

    Abstract CB
    Language English
    Publishing date 2020-06-23
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2452963-1
    ISSN 1662-5102
    ISSN 1662-5102
    DOI 10.3389/fncel.2020.00176
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  5. Article ; Online: CB

    Howlett, Allyn C / Abood, Mary E

    Advances in pharmacology (San Diego, Calif.)

    2017  Volume 80, Page(s) 169–206

    Abstract: ... The ... ...

    Abstract The CB
    MeSH term(s) Alternative Splicing/genetics ; Animals ; Humans ; Phylogeny ; Polymorphism, Genetic ; Receptor, Cannabinoid, CB1/agonists ; Receptor, Cannabinoid, CB1/genetics ; Receptor, Cannabinoid, CB1/metabolism ; Receptor, Cannabinoid, CB2/agonists ; Receptor, Cannabinoid, CB2/genetics ; Receptor, Cannabinoid, CB2/metabolism ; Signal Transduction/drug effects
    Chemical Substances Receptor, Cannabinoid, CB1 ; Receptor, Cannabinoid, CB2
    Language English
    Publishing date 2017-06-12
    Publishing country United States
    Document type Journal Article ; Review
    ISSN 1557-8925
    ISSN (online) 1557-8925
    DOI 10.1016/bs.apha.2017.03.007
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  6. Article ; Online: Effects of Δ

    Breivogel, Chris S / Brenseke, Bonnie M / Eldeeb, Khalil / Nichols, Katlyn / Jonas, Amreen / Mistry, Artik H / Barbalato, Laura / Luibil, Nicholas / Howlett, Allyn C / Leone-Kabler, Sandra / Hilgers, Rob P H / Pulgar, Victor M

    Cannabis and cannabinoid research

    2023  

    Abstract: Background: ...

    Abstract Background:
    Language English
    Publishing date 2023-04-03
    Publishing country United States
    Document type Journal Article
    ZDB-ID 2867624-5
    ISSN 2378-8763 ; 2578-5125
    ISSN (online) 2378-8763
    ISSN 2578-5125
    DOI 10.1089/can.2022.0325
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  7. Article ; Online: The Spicy Story of Cannabimimetic Indoles

    Allyn C. Howlett / Brian F. Thomas / John W. Huffman

    Molecules, Vol 26, Iss 6190, p

    2021  Volume 6190

    Abstract: The Sterling Research Group identified pravadoline as an aminoalkylindole (AAI) non-steroidal anti-inflammatory pain reliever. As drug design progressed, the ability of AAI analogs to block prostaglandin synthesis diminished, and antinociceptive activity ...

    Abstract The Sterling Research Group identified pravadoline as an aminoalkylindole (AAI) non-steroidal anti-inflammatory pain reliever. As drug design progressed, the ability of AAI analogs to block prostaglandin synthesis diminished, and antinociceptive activity was found to result from action at the CB 1 cannabinoid receptor, a G-protein-coupled receptor (GPCR) abundant in the brain. Several laboratories applied computational chemistry methods to ultimately conclude that AAI and cannabinoid ligands could overlap within a common binding pocket but that WIN55212-2 primarily utilized steric interactions via aromatic stacking, whereas cannabinoid ligands required some electrostatic interactions, particularly involving the CB 1 helix-3 lysine. The Huffman laboratory identified strategies to establish CB 2 receptor selectivity among cannabimimetic indoles to avoid their CB 1 -related adverse effects, thereby stimulating preclinical studies to explore their use as anti-hyperalgesic and anti-allodynic pharmacotherapies. Some AAI analogs activate novel GPCRs referred to as “Alkyl Indole” receptors, and some AAI analogs act at the colchicine-binding site on microtubules. The AAI compounds having the greatest potency to interact with the CB 1 receptor have found their way into the market as “Spice” or “K2”. The sale of these alleged “herbal products” evades FDA consumer protections for proper labeling and safety as a medicine, as well as DEA scheduling as compounds having no currently accepted medical use and a high potential for abuse. The distribution to the public of potent alkyl indole synthetic cannabimimetic chemicals without regard for consumer safety contrasts with the adherence to regulatory requirements for demonstration of safety that are routinely observed by ethical pharmaceutical companies that market medicines.
    Keywords aminoalkylindole ; allodynia ; antinociception ; cannabinoid receptor ; CP55940 ; JWH-018 ; Organic chemistry ; QD241-441
    Subject code 540
    Language English
    Publishing date 2021-10-01T00:00:00Z
    Publisher MDPI AG
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  8. Article ; Online: Reward, Control & Decision-Making in Cannabis Use Disorder: Insights from Functional MRI.

    Fatima, Hudaisa / Howlett, Allyn C / Whitlow, Christopher T

    The British journal of radiology

    2019  Volume 92, Issue 1101, Page(s) 20190165

    Abstract: The recreational consumption of cannabis has increased significantly across the world with an estimated 180 million people currently using. In the United States, 4.1 million are currently diagnosed with cannabis use disorder. Cannabis dependence and ... ...

    Abstract The recreational consumption of cannabis has increased significantly across the world with an estimated 180 million people currently using. In the United States, 4.1 million are currently diagnosed with cannabis use disorder. Cannabis dependence and abuse was combined into a single entity as a behavioral disorder with a problematic pattern of cannabis use and termed cannabis use disorder by the Diagnostic and Statistical Manual of Mental Disorders. Chronic use of cannabis has been linked with region-specific effects across the brain mediating reward processing, cognitive control and decision-making that are central to understanding addictive behaviors. This review presents a snapshot of the current literature assessing the effects of chronic cannabis use on human brain function via functional MRI. Studies employing various paradigms and contrasting cognitive activation amongst cannabis users and non-users were incorporated. The effects of trans-del-ta-9-tetrahydrocannabinol (Δ9-THC) in marijuana and other preparations of cannabis are mediated by the endocannabinoid system, which is also briefly introduced.Much variation exists in the current literature regarding the functional changes associated with chronic cannabis use. One possible explanation for this variation is the heterogeneity in study designs, with little implementation of standardized diagnostic criteria when selecting chronic users, distinct time points of participant assessment, differing cognitive paradigms and imaging protocols. As such, there is an urgent requirement for future investigations that further characterize functional changes associated with chronic cannabis use.
    MeSH term(s) Adolescent ; Adult ; Brain/diagnostic imaging ; Brain/physiopathology ; Decision Making/physiology ; Female ; Humans ; Magnetic Resonance Imaging/methods ; Male ; Marijuana Abuse/physiopathology ; Marijuana Abuse/psychology ; Reward ; Young Adult
    Language English
    Publishing date 2019-08-09
    Publishing country England
    Document type Journal Article ; Review
    ZDB-ID 2982-8
    ISSN 1748-880X ; 0007-1285
    ISSN (online) 1748-880X
    ISSN 0007-1285
    DOI 10.1259/bjr.20190165
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  9. Article ; Online: Molecular Interaction between Distal C-Terminal Domain of the CB

    Singh, Pratishtha / Ganjiwale, Anjali / Howlett, Allyn C / Cowsik, Sudha M

    Journal of chemical information and modeling

    2019  Volume 59, Issue 12, Page(s) 5294–5303

    Abstract: We have investigated the structure of the distal C-terminal domain of the of the CB ...

    Abstract We have investigated the structure of the distal C-terminal domain of the of the CB
    MeSH term(s) Amino Acid Sequence ; Carrier Proteins/chemistry ; Carrier Proteins/metabolism ; Models, Molecular ; Protein Binding ; Protein Domains ; Protein Structure, Secondary ; Receptor, Cannabinoid, CB1/chemistry ; Receptor, Cannabinoid, CB1/metabolism
    Chemical Substances Carrier Proteins ; Receptor, Cannabinoid, CB1
    Language English
    Publishing date 2019-12-10
    Publishing country United States
    Document type Journal Article ; Research Support, N.I.H., Extramural ; Research Support, Non-U.S. Gov't
    ZDB-ID 190019-5
    ISSN 1549-960X ; 0095-2338
    ISSN (online) 1549-960X
    ISSN 0095-2338
    DOI 10.1021/acs.jcim.9b00948
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  10. Article ; Online: Differential Expression of CB

    Kozakiewicz, Melissa L / Zhang, Jie / Leone-Kabler, Sandra / Yamaleyeva, Liliya M / McDonald, Anna G / Brost, Brian C / Howlett, Allyn C

    Cannabis and cannabinoid research

    2021  Volume 7, Issue 3, Page(s) 279–288

    Abstract: Background: ...

    Abstract Background:
    MeSH term(s) Cannabinoids/metabolism ; Carrier Proteins/genetics ; Endocannabinoids/metabolism ; Female ; Humans ; Placenta/metabolism ; Pregnancy ; Receptors, Cannabinoid/metabolism
    Chemical Substances Cannabinoids ; Carrier Proteins ; Endocannabinoids ; Receptors, Cannabinoid
    Language English
    Publishing date 2021-04-16
    Publishing country United States
    Document type Journal Article ; Research Support, N.I.H., Extramural
    ZDB-ID 2867624-5
    ISSN 2378-8763 ; 2578-5125
    ISSN (online) 2378-8763
    ISSN 2578-5125
    DOI 10.1089/can.2020.0107
    Database MEDical Literature Analysis and Retrieval System OnLINE

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