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  1. Article ; Online: TRP channels and pain.

    Cortright, Daniel N / Szallasi, Arpad

    Current pharmaceutical design

    2009  Volume 15, Issue 15, Page(s) 1736–1749

    Abstract: Preclinical research has identified an array of ion channels in sensory neurons involved in the generation and transduction of pain as potential targets for pharmacological intervention. Paramount among these new targets is the family of thermosensitive ... ...

    Abstract Preclinical research has identified an array of ion channels in sensory neurons involved in the generation and transduction of pain as potential targets for pharmacological intervention. Paramount among these new targets is the family of thermosensitive transient receptor potential channels, referred to as "thermoTRPs". We detect a wide range of noxious stimuli via a limited number (as of today, six) of thermoTRP channels, four of which (TRPV1-TRPV4) respond to heat and two (TRPA1 and TRPM8) are sensitive to cold. Targeting these thermoTRP channels represents a new and logical strategy in pain relief. Unlike traditional analgesic drugs that either suppress inflammation (e.g. NSAIDs and COX-2 inhibitors) or block pain transmission (e.g. opiates), TRP channel inhibitors aim to prevent pain by blocking a receptor where pain is generated. The archetypal thermoTRP is the vanilloid (capsaicin) receptor TRPV1. TRPV1 has a dynamic threshold of activation. Agents in inflammatory soup, including endogenous TRPV1 agonists (so-called "endovanilloids"), act in concert to reduce the heat activation threshold of TRPV1. In patients, the expression of TRPV1 is up-regulated in a number of painful inflammatory disorders. TRPV1 as a pain target has been validated by genetic deletion and pharmacological inhibition experiments. This area of drug development has been moving rapidly. It took less than a decade from the cloning of TRPV1 to clinical trials with potent small molecule TRPV1 antagonists. This review evaluates current evidence that supports particular TRP channels as targets for novel analgesic drugs, along with potential adverse effects that may limit drug development.
    MeSH term(s) Analgesics/pharmacology ; Animals ; Drug Delivery Systems ; Drug Evaluation, Preclinical ; Gene Expression Regulation ; Humans ; Pain/drug therapy ; Pain/physiopathology ; Transient Receptor Potential Channels/antagonists & inhibitors ; Transient Receptor Potential Channels/metabolism
    Chemical Substances Analgesics ; Transient Receptor Potential Channels
    Language English
    Publishing date 2009-02-12
    Publishing country United Arab Emirates
    Document type Journal Article ; Review
    ZDB-ID 1304236-1
    ISSN 1873-4286 ; 1381-6128
    ISSN (online) 1873-4286
    ISSN 1381-6128
    DOI 10.2174/138161209788186308
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  2. Article ; Online: Locomotor activity in a novel environment as a test of inflammatory pain in rats.

    Matson, David J / Broom, Daniel C / Cortright, Daniel N

    Methods in molecular biology (Clifton, N.J.)

    2010  Volume 617, Page(s) 67–78

    Abstract: Creating a robust and unbiased assay for the study of current and novel analgesics has been a daunting task. Traditional rodent models of pain and inflammation typically rely on a negative reaction to various forms of evoked stimuli to elicit a pain ... ...

    Abstract Creating a robust and unbiased assay for the study of current and novel analgesics has been a daunting task. Traditional rodent models of pain and inflammation typically rely on a negative reaction to various forms of evoked stimuli to elicit a pain response and are subject to rater interpretation. Recently, models such as weight bearing and gait analysis have been developed to address these drawbacks while detecting a drug's analgesic properties. We have recently developed the Reduction of Spontaneous Activity by Adjuvant (RSAA) model as a quick, unbiased method for the testing of potential analgesics. Rats, following prior administration of an activity-decreasing inflammatory insult, will positively increase spontaneous locomotor exploration when given single doses of known analgesics. The RSAA model capitalizes on a rat's spontaneous exploratory behavior in a novel environment with the aid of computer tracking software to quantify movement and eliminate rater bias.
    MeSH term(s) Amphetamine/pharmacology ; Amphetamine/therapeutic use ; Analgesics, Opioid/pharmacology ; Analgesics, Opioid/therapeutic use ; Animals ; Arthritis, Experimental/physiopathology ; Behavior, Animal/drug effects ; Behavior, Animal/physiology ; Central Nervous System Stimulants/pharmacology ; Central Nervous System Stimulants/therapeutic use ; Disease Models, Animal ; Environment ; Exploratory Behavior/drug effects ; Exploratory Behavior/physiology ; Inflammation/physiopathology ; Male ; Morphine/pharmacology ; Morphine/therapeutic use ; Motor Activity/drug effects ; Motor Activity/physiology ; Pain/drug therapy ; Pain/physiopathology ; Pain Measurement/instrumentation ; Pain Measurement/methods ; Rats ; Rats, Sprague-Dawley
    Chemical Substances Analgesics, Opioid ; Central Nervous System Stimulants ; Morphine (76I7G6D29C) ; Amphetamine (CK833KGX7E)
    Language English
    Publishing date 2010
    Publishing country United States
    Document type Journal Article
    ISSN 1940-6029
    ISSN (online) 1940-6029
    DOI 10.1007/978-1-60327-323-7_6
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  3. Article: New frontiers in assessing pain and analgesia in laboratory animals.

    Cortright, Daniel N / Matson, David J / Broom, Daniel C

    Expert opinion on drug discovery

    2008  Volume 3, Issue 9, Page(s) 1099–1108

    Abstract: Background: Translating promising analgesic compounds into reliable pain therapeutics in humans is made particularly challenging by the difficulty in measuring the pain quantitatively. This problem is manifest not only in clinical settings in which ... ...

    Abstract Background: Translating promising analgesic compounds into reliable pain therapeutics in humans is made particularly challenging by the difficulty in measuring the pain quantitatively. This problem is manifest not only in clinical settings in which patient pain assessments involve mostly subjective measures but also in preclinical settings wherein laboratory animals, most commonly rodents, are typically evaluated in stimulus-evoked response tests.
    Objective: Given the limitations of traditional pain tests, we sought out new approaches to measure pain, and analgesia, in laboratory animals.
    Methods: We reviewed the peer reviewed literature to identify pain tests that could be utilized in preclinical settings to understand the effects of new and established analgesics.
    Results/conclusions: The tests identified include weight bearing differential, suppression of feeding, reduction in locomotor activity, gait analysis, conditioning models and functional MRI. Although the pharmacology of known and new analgesics has not been broadly established in these models, they hold the promise of better predictive utility for the discovery of pain relievers.
    Language English
    Publishing date 2008-09
    Publishing country England
    Document type Journal Article
    ZDB-ID 2259618-5
    ISSN 1746-0441
    ISSN 1746-0441
    DOI 10.1517/17460441.3.9.1099
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  4. Article: TRP channels and pain.

    Cortright, Daniel N / Krause, James E / Broom, Daniel C

    Biochimica et biophysica acta

    2007  Volume 1772, Issue 8, Page(s) 978–988

    Abstract: Since the molecular identification of the capsaicin receptor, now known as TRPV1, transient receptor potential (TRP) channels have occupied an important place in the understanding of sensory nerve function in the context of pain. Several TRP channels ... ...

    Abstract Since the molecular identification of the capsaicin receptor, now known as TRPV1, transient receptor potential (TRP) channels have occupied an important place in the understanding of sensory nerve function in the context of pain. Several TRP channels exhibit sensitivity to substances previously known to cause pain or pain-like sensations; these include cinnamaldehyde, menthol, gingerol, and icillin. Many TRP channels also exhibit significant sensitivity to increases or decreases in temperature. Some TRP channels are sensitized in vitro by the activation of other receptors such that these channels may be activated by processes, such as inflammation that result in pain. TRP channels are suggested to be involved in processes as diverse as sensory neuron activation events, neurotransmitter release and action in the spinal cord, and release of inflammatory mediators. These functions strongly suggest that specific and selective inhibition of TRP channel activity will be of use in alleviating pain.
    MeSH term(s) Animals ; Body Temperature Regulation/physiology ; Humans ; Inflammation/physiopathology ; Models, Biological ; Nociceptors/physiology ; Pain/etiology ; Pain/physiopathology ; Phospholipids/metabolism ; Spinal Cord/physiology ; Stress, Mechanical ; Transient Receptor Potential Channels/physiology
    Chemical Substances Phospholipids ; Transient Receptor Potential Channels
    Language English
    Publishing date 2007-08
    Publishing country Netherlands
    Document type Journal Article ; Review
    ZDB-ID 60-7
    ISSN 1879-2596 ; 1879-260X ; 1872-8006 ; 1879-2642 ; 1879-2618 ; 1879-2650 ; 0006-3002 ; 0005-2728 ; 0005-2736 ; 0304-4165 ; 0167-4838 ; 1388-1981 ; 0167-4889 ; 0167-4781 ; 0304-419X ; 1570-9639 ; 0925-4439 ; 1874-9399
    ISSN (online) 1879-2596 ; 1879-260X ; 1872-8006 ; 1879-2642 ; 1879-2618 ; 1879-2650
    ISSN 0006-3002 ; 0005-2728 ; 0005-2736 ; 0304-4165 ; 0167-4838 ; 1388-1981 ; 0167-4889 ; 0167-4781 ; 0304-419X ; 1570-9639 ; 0925-4439 ; 1874-9399
    DOI 10.1016/j.bbadis.2007.03.003
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  5. Article: Biochemical pharmacology of the vanilloid receptor TRPV1. An update.

    Cortright, Daniel N / Szallasi, Arpad

    European journal of biochemistry

    2004  Volume 271, Issue 10, Page(s) 1814–1819

    Abstract: There is mounting evidence that the vanilloid (capsaicin) receptor; transient receptor potential channel, vanilloid subfamily member 1 (TRPV1), is subjected to multiple interacting levels of control. The first level is by reversible phosphorylation ... ...

    Abstract There is mounting evidence that the vanilloid (capsaicin) receptor; transient receptor potential channel, vanilloid subfamily member 1 (TRPV1), is subjected to multiple interacting levels of control. The first level is by reversible phosphorylation catalyzed by intrinsic kinases (e.g. protein kinase A and C) and phosphatases (e.g. calcineurin), which plays a pivotal role in receptor sensitization vs. tachyphylaxis. In addition, this mechanism links TRPV1 to intracellular signaling by various important endogenous as well as exogenous substances such as bradykinin, ethanol, nicotin and insulin. It is not clear, however, whether phosphorylation per se is sufficient to liberate TRPV1 under the inhibitory control of phosphatydylinositol-4,5-bisphosphate. The second level of control is by forming TRPV1 heteromers and their association with putative regulatory proteins. The next level of regulation is by subcellular compartmentalization. The membrane form of TRPV1 functions as a nonselective cation channel. On the endoplasmic reticulum, TRPV1 is present in two differentially regulated forms, one of which is inositol triphosphate-dependent whereas the other is not. These three TRPV1 compartments provide a versatile regulation of intracellular Ca(2+) levels. Last, there is a complex and poorly understood regulation of TRPV1 activity via control of gene expression. Factors that downregulate TRPV1 expression include vanilloid treatment and growth factor (notably, nerve growth factor) deprivation. By contrast, TRPV1 appears to be upregulated during inflammatory conditions. Interestingly, following experimental nerve injury and in animal models of diabetic neuropathy TRPV1 is present on neurons that do not normally express TRPV1. Combined, these findings imply an important role for aberrant TRPV1 expression in the development of neuropathic pain and hyperalgesia. In humans, disease-related changes in TRPV1 expression have already been described (e.g. inflammatory bowel disease and irritable bowel syndrome). The mechanisms that regulate TRPV1 gene expression under pathological conditions are unknown but a better understanding of these pathways has obvious implications for rational drug development.
    MeSH term(s) Animals ; Capsaicin/pharmacology ; Humans ; Inflammation/metabolism ; Models, Molecular ; Pain/metabolism ; Receptors, Drug/agonists ; Receptors, Drug/antagonists & inhibitors ; Receptors, Drug/chemistry ; Receptors, Drug/physiology
    Chemical Substances Receptors, Drug ; Capsaicin (S07O44R1ZM)
    Language English
    Publishing date 2004-05
    Publishing country England
    Document type Journal Article ; Review
    ZDB-ID 3032-6
    ISSN 1432-1033 ; 0014-2956
    ISSN (online) 1432-1033
    ISSN 0014-2956
    DOI 10.1111/j.1432-1033.2004.04082.x
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  6. Article: Hunting for ion channel modulators with herpes simplex virus.

    Cortright, Daniel N / Buck, Marianne E / Krause, James E

    Nature methods

    2007  Volume 4, Issue 9, Page(s) 692–693

    MeSH term(s) Cell Line ; Gene Library ; Genetic Vectors ; Herpesvirus 1, Human/genetics ; Herpesvirus 1, Human/physiology ; Ion Channel Gating/genetics ; Ligands ; TRPV Cation Channels/genetics ; Virus Replication
    Chemical Substances Ligands ; TRPV Cation Channels ; TRPV1 receptor
    Language English
    Publishing date 2007-09
    Publishing country United States
    Document type Comment ; News
    ZDB-ID 2169522-2
    ISSN 1548-7105 ; 1548-7091
    ISSN (online) 1548-7105
    ISSN 1548-7091
    DOI 10.1038/nmeth0907-692
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  7. Article: Transient receptor potential ion channels as targets for the discovery of pain therapeutics.

    Krause, James E / Chenard, Bertrand L / Cortright, Daniel N

    Current opinion in investigational drugs (London, England : 2000)

    2005  Volume 6, Issue 1, Page(s) 48–57

    Abstract: A subset of transient receptor potential (TRP) channels exhibits activity that is highly sensitive to temperature changes and is expressed in sensory tissues, such as nociceptors and skin. Some of these thermosensitive TRP channels, such as TRPV1, TRPV4 ... ...

    Abstract A subset of transient receptor potential (TRP) channels exhibits activity that is highly sensitive to temperature changes and is expressed in sensory tissues, such as nociceptors and skin. Some of these thermosensitive TRP channels, such as TRPV1, TRPV4 and TRPA1, are activated or sensitized by molecules generated by inflammation and/or cell damage. TRPV1, also known as the capsaicin receptor, is particularly important in mediating hyperalgesic responses in inflammatory pain states, as demonstrated by research in knockout animals and with small-molecule antagonists. It is anticipated that TRPV1 antagonists, and perhaps antagonists at other thermosensitive TRP channels, will provide new therapeutic options with which to treat clinical pain.
    MeSH term(s) Analgesics/chemistry ; Analgesics/pharmacology ; Analgesics/therapeutic use ; Animals ; Calcium Channels/metabolism ; Drug Design ; Humans ; Molecular Structure ; Nociceptors/metabolism ; Pain/drug therapy ; Pain/metabolism ; TRPC Cation Channels
    Chemical Substances Analgesics ; Calcium Channels ; TRPC Cation Channels
    Language English
    Publishing date 2005-01
    Publishing country England
    Document type Journal Article ; Review
    ZDB-ID 2027913-9
    ISSN 2040-3429 ; 1472-4472 ; 0967-8298
    ISSN (online) 2040-3429
    ISSN 1472-4472 ; 0967-8298
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  8. Article: The vanilloid receptor TRPV1: 10 years from channel cloning to antagonist proof-of-concept.

    Szallasi, Arpad / Cortright, Daniel N / Blum, Charles A / Eid, Samer R

    Nature reviews. Drug discovery

    2007  Volume 6, Issue 5, Page(s) 357–372

    Abstract: The clinical use of TRPV1 (transient receptor potential vanilloid subfamily, member 1; also known as VR1) antagonists is based on the concept that endogenous agonists acting on TRPV1 might provide a major contribution to certain pain conditions. Indeed, ... ...

    Abstract The clinical use of TRPV1 (transient receptor potential vanilloid subfamily, member 1; also known as VR1) antagonists is based on the concept that endogenous agonists acting on TRPV1 might provide a major contribution to certain pain conditions. Indeed, a number of small-molecule TRPV1 antagonists are already undergoing Phase I/II clinical trials for the indications of chronic inflammatory pain and migraine. Moreover, animal models suggest a therapeutic value for TRPV1 antagonists in the treatment of other types of pain, including pain from cancer. We argue that TRPV1 antagonists alone or in conjunction with other analgesics will improve the quality of life of people with migraine, chronic intractable pain secondary to cancer, AIDS or diabetes. Moreover, emerging data indicate that TRPV1 antagonists could also be useful in treating disorders other than pain, such as urinary urge incontinence, chronic cough and irritable bowel syndrome. The lack of effective drugs for treating many of these conditions highlights the need for further investigation into the therapeutic potential of TRPV1 antagonists.
    MeSH term(s) Analgesics/therapeutic use ; Animals ; Cloning, Molecular ; Glucose/metabolism ; Humans ; Migraine Disorders/drug therapy ; Muscular Diseases/drug therapy ; Pain/drug therapy ; Skin Diseases/drug therapy ; TRPV Cation Channels/agonists ; TRPV Cation Channels/antagonists & inhibitors ; TRPV Cation Channels/genetics ; TRPV Cation Channels/physiology ; Urologic Diseases/drug therapy
    Chemical Substances Analgesics ; TRPV Cation Channels ; TRPV1 protein, human ; Glucose (IY9XDZ35W2)
    Language English
    Publishing date 2007-05
    Publishing country England
    Document type Journal Article ; Review
    ZDB-ID 2062954-0
    ISSN 1474-1784 ; 1474-1776
    ISSN (online) 1474-1784
    ISSN 1474-1776
    DOI 10.1038/nrd2280
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  9. Article ; Online: C5a, but not C3a, increases VEGF secretion in ARPE-19 human retinal pigment epithelial cells.

    Cortright, Daniel N / Meade, Robin / Waters, Stephen M / Chenard, Bertrand L / Krause, James E

    Current eye research

    2009  Volume 34, Issue 1, Page(s) 57–61

    Abstract: Purpose: We examined the potential for the pro-inflammatory complement proteins C5a and C3a to increase VEGF expression in ARPE-19 cells.: Materials and methods: Expression of complement receptors in ARPE-19 cells was evaluated by RT-PCR. VEGF ... ...

    Abstract Purpose: We examined the potential for the pro-inflammatory complement proteins C5a and C3a to increase VEGF expression in ARPE-19 cells.
    Materials and methods: Expression of complement receptors in ARPE-19 cells was evaluated by RT-PCR. VEGF secretion from ARPE-19 cells treated with C5a or C3a was determined by ELISA.
    Results: C5a and C3a receptor, but not C5L2, were detected in human eye tissue and ARPE-19 cells. C5a, but not C3a, treatment increased VEGF secretion from ARPE-19 cells, an effect inhibited by the C5aR antagonist, NDT 9513727.
    Conclusions: C5a receptor mediates increased VEGF secretion from ARPE-19 cells, suggesting a role for the C5a receptor in the pathogenesis of macular degeneration.
    MeSH term(s) Cell Line ; Complement C3a/pharmacology ; Complement C5a/pharmacology ; Enzyme-Linked Immunosorbent Assay ; Humans ; Neutrophils/metabolism ; RNA, Messenger/metabolism ; Receptor, Anaphylatoxin C5a/genetics ; Receptors, Complement/genetics ; Retinal Pigment Epithelium/drug effects ; Retinal Pigment Epithelium/metabolism ; Reverse Transcriptase Polymerase Chain Reaction ; Vascular Endothelial Growth Factor A/metabolism
    Chemical Substances RNA, Messenger ; Receptor, Anaphylatoxin C5a ; Receptors, Complement ; VEGFA protein, human ; Vascular Endothelial Growth Factor A ; complement C3a receptor ; Complement C3a (80295-42-7) ; Complement C5a (80295-54-1)
    Language English
    Publishing date 2009-01
    Publishing country England
    Document type Journal Article
    ZDB-ID 82079-9
    ISSN 1460-2202 ; 0271-3683
    ISSN (online) 1460-2202
    ISSN 0271-3683
    DOI 10.1080/02713680802546658
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  10. Article: Inflammation-induced reduction of spontaneous activity by adjuvant: A novel model to study the effect of analgesics in rats.

    Matson, David J / Broom, Daniel C / Carson, Susan R / Baldassari, James / Kehne, John / Cortright, Daniel N

    The Journal of pharmacology and experimental therapeutics

    2007  Volume 320, Issue 1, Page(s) 194–201

    Abstract: The majority of rodent models used to evaluate analgesic drug effects rely on evoked measures of nociceptive thresholds as primary outcomes. These approaches are often time-consuming, requiring extensive habituation sessions and repeated presentations of ...

    Abstract The majority of rodent models used to evaluate analgesic drug effects rely on evoked measures of nociceptive thresholds as primary outcomes. These approaches are often time-consuming, requiring extensive habituation sessions and repeated presentations of eliciting stimuli, and are prone to false-positive outcomes due to sedation or tester subjectivity. Here, we describe the reduction of spontaneous activity by adjuvant (RSAA) model as an objective and quantifiable behavioral model of inflammatory pain that can predict the analgesic activity of a variety of agents following single-dose administration. In the RSAA model, activity was measured in nonhabituated rats using standard, photocell-based monitors. Bilateral inflammation of the knee joints by complete Freund's adjuvant (CFA) reduced the normal level of activity (horizontal locomotion and vertical rearing) by approximately 60% in a novel environment. This reduction in activity was dose-dependently reversed by ibuprofen, rofecoxib, celecoxib, piroxicam, and dexamethasone, whereas gabapentin and amitriptyline were inactive. Morphine significantly reversed the activity-suppressing effects of CFA, at 1 mg/kg s.c., but at higher doses locomotor activity progressively declined, coincident with the induction of sedation. In contrast to morphine and anti-inflammatory therapies, amphetamine did not affect vertical rearing, even though it increased horizontal locomotion. Thus, unlike standard measures of analgesia such as alteration in thermal or mechanical sensitivity, the RSAA model operationally defines analgesia as a drug-induced increase in spontaneous behavior (vertical rearing in a novel environment). We conclude that the RSAA model is valuable as an objective measure of analgesic efficacy that is not dependent on an evoked stimulus response.
    MeSH term(s) Analgesia ; Analgesics/pharmacology ; Animals ; Carrageenan/pharmacology ; Celecoxib ; Dexamethasone/pharmacology ; Dose-Response Relationship, Drug ; Freund's Adjuvant/pharmacology ; Inflammation/psychology ; Kaolin/pharmacology ; Male ; Models, Animal ; Morphine/pharmacology ; Motor Activity/drug effects ; Pyrazoles/pharmacology ; Rats ; Rats, Sprague-Dawley ; Sulfonamides/pharmacology
    Chemical Substances Analgesics ; Pyrazoles ; Sulfonamides ; Kaolin (24H4NWX5CO) ; Morphine (76I7G6D29C) ; Dexamethasone (7S5I7G3JQL) ; Carrageenan (9000-07-1) ; Freund's Adjuvant (9007-81-2) ; Celecoxib (JCX84Q7J1L)
    Language English
    Publishing date 2007-01
    Publishing country United States
    Document type Journal Article
    ZDB-ID 3106-9
    ISSN 1521-0103 ; 0022-3565
    ISSN (online) 1521-0103
    ISSN 0022-3565
    DOI 10.1124/jpet.106.109736
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