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  1. Article ; Online: BNC210, a negative allosteric modulator of the alpha 7 nicotinic acetylcholine receptor, demonstrates anxiolytic- and antidepressant-like effects in rodents.

    O'Connor, Susan M / Sleebs, Brad E / Street, Ian P / Flynn, Bernard L / Baell, Jonathan B / Coles, Carolyn / Quazi, Nurul / Paul, Dharam / Poiraud, Etienne / Huyard, Bertrand / Wagner, Stephanie / Andriambeloson, Emile / de Souza, Errol B

    Neuropharmacology

    2024  Volume 246, Page(s) 109836

    Abstract: This work describes the characterization of BNC210 (6-[(2,3-dihydro-1H-inden-2-yl)amino]-1-ethyl-3-(4-morpholinylcarbonyl)-1,8-naphthyridin-4(1H)-one), a selective, small molecule, negative allosteric modulator (NAM) of α7 nicotinic acetylcholine ... ...

    Abstract This work describes the characterization of BNC210 (6-[(2,3-dihydro-1H-inden-2-yl)amino]-1-ethyl-3-(4-morpholinylcarbonyl)-1,8-naphthyridin-4(1H)-one), a selective, small molecule, negative allosteric modulator (NAM) of α7 nicotinic acetylcholine receptors (α7 nAChR). With the aim to discover a non-sedating, anxiolytic compound, BNC210 was identified during phenotypic screening of a focused medicinal chemistry library using the mouse Light Dark (LD) box to evaluate anxiolytic-like activity and the mouse Open Field (OF) (dark) test to detect sedative and/or motor effects. BNC210 exhibited anxiolytic-like activity with no measurable sedative or motor effects. Electrophysiology showed that BNC210 did not induce α7 nAChR currents by itself but inhibited EC
    MeSH term(s) Rats ; Male ; Mice ; Humans ; Animals ; alpha7 Nicotinic Acetylcholine Receptor/metabolism ; Anti-Anxiety Agents/pharmacology ; Rodentia/metabolism ; Receptors, Nicotinic/metabolism ; Antidepressive Agents ; Hypnotics and Sedatives ; Allosteric Regulation
    Chemical Substances alpha7 Nicotinic Acetylcholine Receptor ; Anti-Anxiety Agents ; Receptors, Nicotinic ; Antidepressive Agents ; Hypnotics and Sedatives
    Language English
    Publishing date 2024-01-06
    Publishing country England
    Document type Journal Article
    ZDB-ID 218272-5
    ISSN 1873-7064 ; 0028-3908
    ISSN (online) 1873-7064
    ISSN 0028-3908
    DOI 10.1016/j.neuropharm.2024.109836
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  2. Article: Discovery of BNC375, a Potent, Selective, and Orally Available Type I Positive Allosteric Modulator of α7 nAChRs.

    Harvey, Andrew J / Avery, Thomas D / Schaeffer, Laurent / Joseph, Christophe / Huff, Belinda C / Singh, Rajinder / Morice, Christophe / Giethlen, Bruno / Grishin, Anton A / Coles, Carolyn J / Kolesik, Peter / Wagner, Stéphanie / Andriambeloson, Emile / Huyard, Bertrand / Poiraud, Etienne / Paul, Dharam / O'Connor, Susan M

    ACS medicinal chemistry letters

    2019  Volume 10, Issue 5, Page(s) 754–760

    Abstract: Positive allosteric modulators (PAMs) of α7 nAChRs can have different properties with respect to their effects on channel kinetics. Type I PAMs amplify peak channel response to acetylcholine but do not appear to influence channel desensitization kinetics, ...

    Abstract Positive allosteric modulators (PAMs) of α7 nAChRs can have different properties with respect to their effects on channel kinetics. Type I PAMs amplify peak channel response to acetylcholine but do not appear to influence channel desensitization kinetics, whereas Type II PAMs both increase channel response and delay receptor desensitization. Both Type I and Type II PAMs are reported in literature, but there are limited reports describing their structure-kinetic profile relationships. Here, we report a novel class of compounds with either Type I or Type II behavior that can be tuned by the relative stereochemistry around the central cyclopropyl ring: for example, (
    Language English
    Publishing date 2019-03-25
    Publishing country United States
    Document type Journal Article
    ISSN 1948-5875
    ISSN 1948-5875
    DOI 10.1021/acsmedchemlett.9b00001
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  3. Article ; Online: Pharmacological Characterization of the Novel and Selective

    Wang, Xiaohai / Daley, Christopher / Gakhar, Vanita / Lange, Henry S / Vardigan, Joshua D / Pearson, Michelle / Zhou, Xiaoping / Warren, Lee / Miller, Corin O / Belden, Michelle / Harvey, Andrew J / Grishin, Anton A / Coles, Carolyn J / O'Connor, Susan M / Thomson, Fiona / Duffy, Joseph L / Bell, Ian M / Uslaner, Jason M

    The Journal of pharmacology and experimental therapeutics

    2020  Volume 373, Issue 2, Page(s) 311–324

    Abstract: Treatments for cognitive deficits associated with central nervous system (CNS) disorders such as Alzheimer disease and schizophrenia remain significant unmet medical needs that incur substantial pressure on the health care system. ... ...

    Abstract Treatments for cognitive deficits associated with central nervous system (CNS) disorders such as Alzheimer disease and schizophrenia remain significant unmet medical needs that incur substantial pressure on the health care system. The
    MeSH term(s) Allosteric Regulation ; Animals ; Benzethonium/pharmacology ; Brain/drug effects ; Brain/physiology ; Cell Survival/drug effects ; Cells, Cultured ; Chlorobenzenes/pharmacology ; Cognition/drug effects ; Long-Term Potentiation/drug effects ; Macaca mulatta ; Male ; Neurotransmitter Agents/metabolism ; Rats ; Rats, Sprague-Dawley ; Rats, Wistar ; Scopolamine/pharmacology ; alpha7 Nicotinic Acetylcholine Receptor/agonists
    Chemical Substances BNC375 ; Chlorobenzenes ; Neurotransmitter Agents ; alpha7 Nicotinic Acetylcholine Receptor ; Benzethonium (1VU15B70BP) ; Scopolamine (DL48G20X8X)
    Language English
    Publishing date 2020-02-24
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 3106-9
    ISSN 1521-0103 ; 0022-3565
    ISSN (online) 1521-0103
    ISSN 0022-3565
    DOI 10.1124/jpet.119.263483
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  4. Article ; Online: Structure-activity relationship studies of SEN12333 analogues: determination of the optimal requirements for binding affinities at α7 nAChRs through incorporation of known structural motifs.

    Beinat, Corinne / Reekie, Tristan / Banister, Samuel D / O'Brien-Brown, James / Xie, Teresa / Olson, Thao T / Xiao, Yingxian / Harvey, Andrew / O'Connor, Susan / Coles, Carolyn / Grishin, Anton / Kolesik, Peter / Tsanaktsidis, John / Kassiou, Michael

    European journal of medicinal chemistry

    2015  Volume 95, Page(s) 277–301

    Abstract: Alpha7 nicotinic acetylcholine receptors (nAChRs) have implications in the regulation of cognitive processes such as memory and attention and have been identified as a promising therapeutic target for the treatment of the cognitive deficits associated ... ...

    Abstract Alpha7 nicotinic acetylcholine receptors (nAChRs) have implications in the regulation of cognitive processes such as memory and attention and have been identified as a promising therapeutic target for the treatment of the cognitive deficits associated with schizophrenia and Alzheimer's disease (AD). Structure affinity relationship studies of the previously described α7 agonist SEN12333 (8), have resulted in the identification of compound 45, a potent and selective agonist of the α7 nAChR with enhanced affinity and improved physicochemical properties over the parent compound (SEN12333, 8).
    MeSH term(s) Drug Discovery ; Electrophysiological Phenomena/drug effects ; HEK293 Cells ; Humans ; Models, Molecular ; Morpholines/chemistry ; Morpholines/metabolism ; Morpholines/pharmacology ; Protein Binding ; Protein Conformation ; Pyridines/chemistry ; Pyridines/metabolism ; Pyridines/pharmacology ; Structure-Activity Relationship ; alpha7 Nicotinic Acetylcholine Receptor/chemistry ; alpha7 Nicotinic Acetylcholine Receptor/metabolism
    Chemical Substances 5-morpholin-4-ylpentanoic acid (4-pyridin-3-ylphenyl)amide ; Morpholines ; Pyridines ; alpha7 Nicotinic Acetylcholine Receptor
    Language English
    Publishing date 2015-05-05
    Publishing country France
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 188597-2
    ISSN 1768-3254 ; 0009-4374 ; 0223-5234
    ISSN (online) 1768-3254
    ISSN 0009-4374 ; 0223-5234
    DOI 10.1016/j.ejmech.2015.03.025
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  5. Article ; Online: Investigations of amide bond variation and biaryl modification in analogues of α7 nAChR agonist SEN12333.

    Beinat, Corinne / Reekie, Tristan / Hibbs, David / Xie, Teresa / Olson, Thao T / Xiao, Yingxian / Harvey, Andrew / O'Connor, Susan / Coles, Carolyn / Tsanaktsidis, John / Kassiou, Michael

    European journal of medicinal chemistry

    2014  Volume 84, Page(s) 200–205

    Abstract: Several lines of experimental evidence support the involvement of the α7 nAChR in schizophrenia and Alzheimer's disease. Modulators of the α7 nAChR have been extensively reviewed for the treatment of the cognitive deficits associated with these ... ...

    Abstract Several lines of experimental evidence support the involvement of the α7 nAChR in schizophrenia and Alzheimer's disease. Modulators of the α7 nAChR have been extensively reviewed for the treatment of the cognitive deficits associated with these pathologies. SEN12333 represents a novel α7 nAChR agonist chemotype with potential for reduced side effects but requiring further SAR exploration. The present work investigates the amide bond of SEN12333, specifically its connectivity and replacement with the tetrazole functionality, a known cis amide isostere. The results reveal the original amide bond connectivity of SEN12333 to be favorable for binding affinity and agonist activity at α7 nAChRs. The use of a tetrazole isostere completely abolishes affinity and functional activity and suggests that SEN12333 binds in a linear conformation. Results reported herein also suggest the pyridine nitrogen within the terminal aromatic ring of SEN12333 is not essential for binding affinity or functional activity. Further SAR investigations involving manipulation of other moieties contained within SEN12333 are warranted.
    MeSH term(s) Amides/chemistry ; Dose-Response Relationship, Drug ; Humans ; Models, Molecular ; Molecular Structure ; Morpholines/chemical synthesis ; Morpholines/chemistry ; Morpholines/pharmacology ; Nicotinic Agonists/chemical synthesis ; Nicotinic Agonists/chemistry ; Nicotinic Agonists/pharmacology ; Pyridines/chemical synthesis ; Pyridines/chemistry ; Pyridines/pharmacology ; Structure-Activity Relationship ; alpha7 Nicotinic Acetylcholine Receptor/agonists
    Chemical Substances 5-morpholin-4-ylpentanoic acid (4-pyridin-3-ylphenyl)amide ; Amides ; Morpholines ; Nicotinic Agonists ; Pyridines ; alpha7 Nicotinic Acetylcholine Receptor
    Language English
    Publishing date 2014-09-12
    Publishing country France
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 188597-2
    ISSN 1768-3254 ; 0009-4374 ; 0223-5234
    ISSN (online) 1768-3254
    ISSN 0009-4374 ; 0223-5234
    DOI 10.1016/j.ejmech.2014.07.029
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  6. Article ; Online: Preventability of severe acute maternal morbidity.

    Lawton, Beverley / MacDonald, Evelyn Jane / Brown, Selina Ann / Wilson, Leona / Stanley, James / Tait, John David / Dinsdale, Richard Alan / Coles, Carolyn Lee / Geller, Stacie E

    American journal of obstetrics and gynecology

    2014  Volume 210, Issue 6, Page(s) 557.e1–6

    Abstract: Objective: We sought to assess potential preventability of severe acute maternal morbidity (SAMM) cases admitted to intensive-care units (ICUs) or high-dependency units (HDUs).: Study design: Inclusion criteria were admissions to ICUs or HDUs of ... ...

    Abstract Objective: We sought to assess potential preventability of severe acute maternal morbidity (SAMM) cases admitted to intensive-care units (ICUs) or high-dependency units (HDUs).
    Study design: Inclusion criteria were admissions to ICUs or HDUs of women who were pregnant or within 42 days of delivery in 4 District Health Board areas (accounting for a third of annual births in New Zealand) during a 17-month period. Cases were reviewed by external multidisciplinary panels using a validated model for assessing preventability.
    Results: In all, 98 SAMM cases were assessed; 38 (38.8%) cases were deemed potentially preventable, 36 (36.7%) not preventable but improvement in care was needed, and 24 (24.5%) not preventable. The most frequent preventable factors were clinician related: delay or failure in diagnosis or recognition of high-risk status (51%); and delay or inappropriate treatment (70%). The most common causes of preventable severe morbidity were blood loss and septicemia.
    Conclusion: The majority of SAMM cases were potentially preventable or required improvement in care. Themes around substandard care related to delay in diagnosis and treatment for postpartum hemorrhage and septicemia. These findings can inform clinical educational programs and policies to improve maternal outcomes. This study has now been expanded to a national New Zealand audit of all SAMM cases admitted to an ICU/HDU.
    MeSH term(s) Adult ; Delayed Diagnosis/prevention & control ; Delayed Diagnosis/statistics & numerical data ; Feasibility Studies ; Female ; Hospitalization/statistics & numerical data ; Humans ; Intensive Care Units ; Medical Audit/methods ; New Zealand/epidemiology ; Pregnancy ; Pregnancy Complications/epidemiology ; Pregnancy Complications/etiology ; Pregnancy Complications/prevention & control ; Quality of Health Care/standards ; Quality of Health Care/statistics & numerical data ; Socioeconomic Factors
    Language English
    Publishing date 2014-06
    Publishing country United States
    Document type Journal Article ; Multicenter Study ; Research Support, Non-U.S. Gov't
    ZDB-ID 80016-8
    ISSN 1097-6868 ; 0002-9378
    ISSN (online) 1097-6868
    ISSN 0002-9378
    DOI 10.1016/j.ajog.2013.12.032
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  7. Article ; Online: Audit of severe acute maternal morbidity describing reasons for transfer and potential preventability of admissions to ICU.

    Lawton, Beverley A / Wilson, Leona F / Dinsdale, Richard A / Rose, Sally B / Brown, Selina A / Tait, John / Coles, Carolyn L / McCaw, Amanda

    The Australian & New Zealand journal of obstetrics & gynaecology

    2010  Volume 50, Issue 4, Page(s) 346–351

    Abstract: Background: Maternal mortality is a rare event in the developed world. Assessment of severe acute maternal morbidity (SAMM) is therefore an appropriate measure of the quality of maternity care.: Aims: The aim of the study was to conduct a ... ...

    Abstract Background: Maternal mortality is a rare event in the developed world. Assessment of severe acute maternal morbidity (SAMM) is therefore an appropriate measure of the quality of maternity care.
    Aims: The aim of the study was to conduct a retrospective audit of SAMM cases (pregnant women admitted to a New Zealand Intensive Care Unit) to describe clinical, socio-demographic characteristics, pregnancy outcomes and preventability.
    Methods: Severe acute maternal morbidity cases were reviewed by a multidisciplinary panel to determine reasons for admission to ICU, to classify organ-system dysfunction and to determine whether the SAMM case was preventable or not. Inclusion criteria were: admission to ICU between 2005 and 2007 during pregnancy or within 42 days of delivery.
    Results: Twenty-nine SAMM cases were reviewed, of which 10 (35%) were deemed preventable. The most common reasons for transfer to ICU were: the need for invasive vascular monitoring, hypotension and disseminated intravascular coagulation. The most frequent types of preventable events were: inadequate diagnosis/recognition of high-risk status, inappropriate treatment, communication problems and inadequate documentation. All five SAMM cases of septicaemia were deemed preventable. Of the ten preventable cases, three were Maori (50% of the Maori in total audit), four were Pacific (67% of the Pacific in total audit) and three were women of 'other' ethnicities (17.6%, 3 of 17 in the audit).
    Conclusions: An audit of SAMM cases describing reasons for transfer to ICU and preventability is feasible. We recommend that a prospective national SAMM audit process be introduced in New Zealand as a quality of care measure.
    MeSH term(s) Acute Disease/epidemiology ; Adolescent ; Adult ; Clinical Audit/statistics & numerical data ; Disseminated Intravascular Coagulation/epidemiology ; Disseminated Intravascular Coagulation/prevention & control ; Female ; Hemorrhage/epidemiology ; Hemorrhage/prevention & control ; Humans ; Hypotension/epidemiology ; Hypotension/prevention & control ; Intensive Care Units/statistics & numerical data ; Medical Records ; Middle Aged ; Morbidity ; New Zealand/epidemiology ; Pregnancy ; Pregnancy Complications/epidemiology ; Pregnancy Complications/prevention & control ; Pregnancy Outcome ; Prenatal Care ; Retrospective Studies ; Young Adult
    Language English
    Publishing date 2010-08
    Publishing country Australia
    Document type Journal Article
    ZDB-ID 390815-x
    ISSN 1479-828X ; 0004-8666
    ISSN (online) 1479-828X
    ISSN 0004-8666
    DOI 10.1111/j.1479-828X.2010.01200.x
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