Page last updated: 2024-09-04

ag 3-5 and pyrimidinones

ag 3-5 has been researched along with pyrimidinones in 99 studies

Compound Research Comparison

Studies
(ag 3-5)
Trials
(ag 3-5)
Recent Studies (post-2010)
(ag 3-5)
Studies
(pyrimidinones)
Trials
(pyrimidinones)
Recent Studies (post-2010) (pyrimidinones)
1260666,0596042,692

Research

Studies (99)

TimeframeStudies, this research(%)All Research%
pre-19903 (3.03)18.7374
1990's0 (0.00)18.2507
2000's35 (35.35)29.6817
2010's56 (56.57)24.3611
2020's5 (5.05)2.80

Authors

AuthorsStudies
Seid, DA; Wei, ET1
Wei, ET1
Cowan, A1
Andersson, DA; Bevan, S; Chase, HW1
Chuang, HH; Julius, D; Neuhausser, WM1
Babes, A; Reid, G; Zorzon, D1
Nagao, M; Shimada, S; Ueda, T; Ugawa, S; Yamamura, H1
Colburn, RW; Flores, CM; Liu, Y; Lubin, ML; Qin, N; Reitz, TL; Wang, Y1
Bandell, M; Dubin, AE; Hwang, SW; Mathur, J; Orth, A; Patapoutian, A; Petrus, MJ1
Fu, Y; Kochukov, MY; McNearney, TA; Westlund, KN1
Cowan, A; Rawls, SM; Werkheiser, JL3
Anderson, H; Cottrell, DF; Fleetwood-Walker, SM; Garry, EM; Mitchell, R; Proudfoot, CJ; Robertson, DC; Rosie, R1
Barrit, G; Bavencoffe, A; Beck, B; Bidaux, G; Lemonnier, L; Prevarskaya, N; Shuba, Y; Skryma, R; Thebault, S1
Doerner, JF; Gisselmann, G; Hatt, H; Wetzel, CH1
Giesecke, Y; Grötzinger, C; Hosokawa, H; Kaiser, S; Kobayashi, S; Langrehr, J; Mergler, S; Neuhaus, P; Neumann, M; Plath, T; Plöckinger, U; Strowski, MZ; Wiedenmann, B1
De Petrocellis, L; Di Marzo, V; Moriello, AS; Orlando, P; Starowicz, K; Vivese, M1
Dhaka, A; Earley, TJ; Mathur, J; Murray, AN; Patapoutian, A; Petrus, MJ1
Brandt, MR; Colburn, RW; D'Andrea, MR; Flores, CM; Lawrence, D; Liu, Y; Lubin, ML; Qin, N; Stone, DJ; Wang, Y1
Bödding, M; Flockerzi, V; Wissenbach, U1
Cahusac, PM; Noyce, R1
Ding, Z; Gomez, T; Raffa, RB; Rawls, SM1
Horie, S; Matsumoto, K; Nakamura, T; Penuelas, A; Tashima, K; Tsuchiya, S; Yano, S1
Endo, T; Hayashi, S; Kubo, Y; Nakamura, E; Takeuchi, K1
Carlton, SM; Ji, G; Kochukov, MY; Westlund, KN; Zhou, S1
Cowan, A; Ding, Z; Gomez, T; Rawls, SM; Werkheiser, JL1
Brignell, JL; Chapman, V; Kendall, DA1
Hasegawa, Y; Ito, S; Kamiya, K; Kondo, M; Kume, H; Makino, Y; Shiraki, A1
Ak, VE; G, G; H, H; Jf, D; Ma, S1
Kühn, C; Kühn, FJ; Lückhoff, A1
Bettinelli, I; Marconi, C; Pedretti, A; Vistoli, G1
Baron, DA; Chau, S; Cowan, A; Gomez, T; Henry, C; Parekh, S; Rawls, SM; Werkheiser, J1
Atoyan, R; Botchkareva, NV; Shander, D1
Jeong, HJ; Vaughan, CW; Wrigley, PJ2
Caudle, RM; Neubert, JK; Rossi, HL; Vierck, CJ; Yezierski, RP1
Ma, S1
Cahusac, PM1
Andersson, DA; Bevan, S; Gentry, C; Stoakley, N1
Chodon, D; Dhennin-Duthille, I; Gautier, M; Guilbert, A; Ouadid-Ahidouch, H; Sevestre, H; Telliez, MS1
Biel, M; Leinders-Zufall, T; Pyrski, M; Schmid, A; Zufall, F1
Kühn, C; Kühn, FJP; Lückhoff, A; Witschas, K1
Dayanithi, G; Kayano, T; Kitamura, N; Moriya, T; Ozaki, Y; Shibuya, I; Tsutsumi, A1
Belmonte, C; Morenilla-Palao, C; Valero, M; Viana, F1
Baylie, RL; Cheng, H; James, AF; Langton, PD1
Anand, P; Anand, U; Otto, WR1
Jeon, JH; Kim, J; Kim, SH; Kim, SJ; Kim, SY; Park, EJ; Park, HH; So, I1
Cowan, A; Hirsch, DD; Kim, J; Lisek, R; Rawls, SM; Raymondi, N; Rosenthal, A1
Beltrán, C; Darszon, A; De Blas, G; de la Vega-Beltrán, JL; Gibbs, GM; Martínez-López, P; Monroy, E; O'Bryan, MK; Orta, G; Treviño, CL1
Tsai, ML; Wu, PY; Wu, SN1
Blackshaw, AL; Brierley, SM; Castro, J; Harrington, AM; Hughes, PA; Isaacs, NJ; Martin, CM; Yang, J1
Choi, HK; Han, JH; Kim, SJ1
Filippov, IB; Iurkevych, A; Kuliieva, IeM; Prevarskaia, N; Shuba, IaM; Skryma, R; Vladymyrova, IA1
Ikebe, T; Ohkubo, T; Okamoto, Y; Yamazaki, J1
Bartberger, MD; Bo, Y; Chen, J; Correll, TL; Deng, H; Gavva, NR; Gore, V; Klionsky, L; Lehto, SG; Ma, V; Nishimura, N; Norman, MH; Tamayo, NA; Tang, P; Wang, W; Youngblood, B1
Gisselmann, G; Hatt, H; Sherkheli, MA1
Cho, JH; Choi, IS; Jang, IS; Jeong, MY; Lee, HJ1
Bharate, SB; Bharate, SS1
Hilgers, RD; Hoffmann, DC; Kühn, C; Kühn, FJ; Lückhoff, A; Winking, M1
Mello de Queiroz, F; Pardo, LA; Stühmer, W; Valero, ML; Viana, F1
Daimon, T; Imai, Y; Kimura, A; Kurohane, K; Narukawa, M; Sahara, Y; Watanabe, T1
Brandt, MR; Colburn, RW; Dax, SL; Flores, CM; Hutchinson, TL; Lubin, ML; Ludovici, DW; Macielag, MJ; Matthews, JM; Qin, N; Stone, DJ; Tennakoon, M; Xia, M; Xu, X; Youngman, MA; Zhu, B1
McCoy, ES; Pribisko, AL; Street, SE; Taylor-Blake, B; Zheng, J; Zylka, MJ1
Altier, C; Beck, PL; Chapman, K; Ghosh, S; Hirota, CL; Hollenberg, MD; Hyun, E; Lapointe, TK; McKemy, DD; Ramachandran, R; Vergnolle, N; Zhao, L1
Dean, S; Doran, O; Drake, MJ; Parsons, BA; Rhodes, A; Vahabi, B1
Babes, A; Ciobanu, AC; Dobre, C; Reid, G; Selescu, T1
Abdelmessih, S; Böhm, A; Derckx, R; Garreis, F; Khajavi, N; Mergler, S; Polat, OK; Ramesh, N; Reinach, PS; Riechardt, AI; Schmelzer, L; Skosyrski, S1
Chun, JN; Jeon, JH; Kim, SH; Lee, S; So, I1
Bassetto, F; Calcagno, A; De Caro, R; De Stefani, D; Granzotto, M; Macchi, V; Petrelli, L; Porzionato, A; Rizzuto, R; Rossato, M; Silvestrin, V; Vencato, J; Vettor, R1
Kawaguchi, A; Kuroda, H; Nishiyama, A; Sato, M; Shibukawa, Y; Shimada, M; Sobhan, U; Soya, M; Tazaki, M; Tsumura, M1
Horie, S; Takayama, H; Terada, Y; Tominaga, M; Uchida, K; Watanabe, T1
Hagenacker, T; Lampe, M; Schäfers, M1
Bartberger, MD; Bo, Y; Clarine, J; Davis, CD; Gavva, NR; Gore, VK; Horne, DB; Kaller, MR; Lehto, SG; Ma, VV; Monenschein, H; Nguyen, TT; Nishimura, N; Norman, MH; Tamayo, NA; Tang, P; Wang, W; Youngblood, BD; Zhang, M1
Babes, A; Chiritoiu, G; Cucu, D; Dima, SO; Duda, DG; Horii, A; Petrescu, S; Popescu, I; Stanica, L1
Di Silvio, L; Duggal, AK; Egbuniwe, O; Grant, AD; Grover, S; Mavroudis, A; Renton, T; Yazdi, M1
McCoy, ES; Zylka, MJ1
Khajavi, N; Köhrle, J; Lucius, A; Mergler, S; Reinach, PS; Skrzypski, M; Slavi, N; Strauß, O1
Davis, C; Gavva, NR; Kerstein, PC; Lehto, SG; Stucky, CL; Wang, J; Wang, W; Weyer, AD; Wild, KD; Youngblood, BD; Zhang, M1
Alvarez de la Rosa, D; Armas-Capote, N; Buckley, ST; Ehrhardt, C; Fischer, H; Harvey, BJ; Huwer, H; Illek, B; Lehr, CM; Schneider-Daum, N; Schwagerus, E; Sladek, S1
De Petrocellis, L; Ortar, G; Rusterholz, DB; Schiano Moriello, A; Serum, EM1
Ahn, DD; Bischoff, C; Burgos-Vega, CC; Dussor, G; Gavva, N; Horne, D; Wang, J; Wang, W1
Dhandapani, P; Grötzinger, C; Huimann, P; Khajavi, N; Köhrle, J; Ljubojevic, N; Lucius, A; Mergler, S; Reinach, PS1
Benoit, M; Danglot, L; Galli, T; Ghosh, D; Janssens, A; Pinto, S; Segal, A; Van Ranst, N; Vanden Berghe, P; Vandewauw, I; Vennekens, R; Voets, T; Vriens, J1
An, X; He, M; Wang, Q; Zhang, L1
Ohta, T; Saito, S; Takahashi, K; Tominaga, M; Yamamoto, A1
Borysova, L; Burdyga, TV; Johnson, CD; Kustov, MV; Melanaphy, D; Watson, CA; Zholos, AV1
Allan, ERO; Ewanchuk, BW; Ramachandran, R; Warren, AL; Yates, RM1
Jiao, HX; Lin, DC; Lin, MJ; Mu, YP; Sham, JSK; Zheng, SY1
Allen, JR; Bartberger, MD; Biswas, K; Brown, J; Chen, JJ; Clarine, J; Davis, CD; Gavva, NR; Gore, VK; Harried, S; Horne, DB; Horner, M; Kaller, MR; Lehto, SG; Liu, Q; Ma, VV; Monenschein, H; Nguyen, TT; Youngblood, BD; Yuan, CC; Zhang, M; Zhong, W1
Clemmensen, C; Cowley, MA; Feuchtinger, A; Finan, B; Fischer, K; Grandl, G; Gruber, T; Hofmann, SM; Jall, S; Jastroch, M; Karlas, A; Keipert, S; Kleinert, M; Loher, D; Müller, TD; Nascimento, EBM; Ntziachristos, V; Quarta, C; Reber, J; Sachs, S; Sanchez-Quant, E; Schrauwen, P; Simonds, SE; Tschöp, MH1
Borgnia, MJ; Hsu, AL; Le, SC; Lee, SY; Yang, H; Yin, Y1
Clemmensen, C; Collden, G; Dong, X; Finan, B; Fischer, K; Jall, S; Müller, TD; Tschöp, MH1
Minegishi, Y; Ota, N; Sugita, S; Tamura, K; Tokunaga, T1
Thiel, G; Ulrich, M; Wissenbach, U1
Huang, G; Lai, R; Li, B; Liu, X; Luo, A; Nie, Y; Wei, F; Yang, S; Zhou, W1
Fujimori, Y; Hirasawa, H; Ikeda, T; Kamada, N; Kanbe, H; Kobayashi, JI; Nakanishi, O; Yamamoto, A1
Fedinec, AL; Harsono, M; Liu, J; Parfenova, H; Pourcyrous, M; Zhang, R1
Borgnia, MJ; Butay, KJ; Feng, S; Im, W; Lee, SY; Yin, Y; Zhang, F1

Reviews

1 review(s) available for ag 3-5 and pyrimidinones

ArticleYear
Modulation of thermoreceptor TRPM8 by cooling compounds.
    ACS chemical neuroscience, 2012, Apr-18, Volume: 3, Issue:4

    Topics: Animals; Cold Temperature; Humans; Menthol; Pyrimidinones; Thermoreceptors; Thermosensing; TRPM Cation Channels

2012

Other Studies

98 other study(ies) available for ag 3-5 and pyrimidinones

ArticleYear
AG-3-5: a chemical producing sensations of cold.
    The Journal of pharmacy and pharmacology, 1983, Volume: 35, Issue:2

    Topics: Animals; Cold Temperature; Male; Menthol; Mutagens; Pyrimidinones; Rats; Sensation

1983
Pharmacological aspects of shaking behavior produced by TRH, AG-3-5, and morphine withdrawal.
    Federation proceedings, 1981, Volume: 40, Issue:5

    Topics: Animals; Cold Temperature; Escape Reaction; Humans; Morphine Dependence; Naloxone; Pentobarbital; Pyrimidinones; Rats; Receptors, Adrenergic, alpha; Receptors, Muscarinic; Receptors, Opioid; Sensation; Shivering; Structure-Activity Relationship; Substance Withdrawal Syndrome; Thyrotropin-Releasing Hormone

1981
RX 336-M, a new chemical tool in the analysis of the quasi-morphine withdrawal syndrome.
    Federation proceedings, 1981, Volume: 40, Issue:5

    Topics: Animals; Codeine; Drug Tolerance; Humans; Hydroxamic Acids; Male; Morphine Dependence; Pyrimidinones; Rats; Shivering; Structure-Activity Relationship; Substance Withdrawal Syndrome; Thyrotropin-Releasing Hormone; Valproic Acid

1981
TRPM8 activation by menthol, icilin, and cold is differentially modulated by intracellular pH.
    The Journal of neuroscience : the official journal of the Society for Neuroscience, 2004, Jun-09, Volume: 24, Issue:23

    Topics: Animals; CHO Cells; Cold Temperature; Cricetinae; Cricetulus; Electrophysiology; Fluorescent Dyes; Fura-2; Hydrogen-Ion Concentration; Ion Channels; Menthol; Neoplasm Proteins; Pyrimidinones

2004
The super-cooling agent icilin reveals a mechanism of coincidence detection by a temperature-sensitive TRP channel.
    Neuron, 2004, Sep-16, Volume: 43, Issue:6

    Topics: Acetylcholine; Animals; Calcium; Calcium Signaling; Cell Line; Cell Membrane; Chelating Agents; Chickens; Cold Temperature; Cyclohexane Monoterpenes; Cytoplasm; Dose-Response Relationship, Drug; Dose-Response Relationship, Radiation; Drug Interactions; Egtazic Acid; Humans; Ion Channel Gating; Ion Channels; Membrane Potentials; Menthol; Molecular Biology; Molecular Sequence Data; Mutagenesis, Site-Directed; Neoplasm Proteins; Patch-Clamp Techniques; Potassium Channels; Potassium Channels, Calcium-Activated; Pyrimidinones; Small-Conductance Calcium-Activated Potassium Channels; Terpenes; Transfection; TRPM Cation Channels; Xenopus laevis

2004
Two populations of cold-sensitive neurons in rat dorsal root ganglia and their modulation by nerve growth factor.
    The European journal of neuroscience, 2004, Volume: 20, Issue:9

    Topics: Animals; Ankyrins; Calcium; Calcium Channels; Calcium Signaling; Capsaicin; Cells, Cultured; Cold Temperature; Drug Synergism; Ganglia, Spinal; Ion Channels; Menthol; Mustard Plant; Neoplasm Proteins; Nerve Growth Factor; Neurons, Afferent; Plant Extracts; Plant Oils; Pyrimidinones; Rats; Thermosensing; Transient Receptor Potential Channels; TRPA1 Cation Channel; TRPC Cation Channels; TRPM Cation Channels

2004
Icilin activates the delta-subunit of the human epithelial Na+ channel.
    Molecular pharmacology, 2005, Volume: 68, Issue:4

    Topics: Amiloride; Animals; Capsaicin; Epithelial Sodium Channels; Humans; Protons; Pyrimidinones; Sodium Channel Agonists; Sodium Channels; Xenopus laevis

2005
Molecular identification and functional characterization of a temperature-sensitive transient receptor potential channel (TRPM8) from canine.
    European journal of pharmacology, 2006, Jan-13, Volume: 530, Issue:1-2

    Topics: Action Potentials; Amino Acid Sequence; Animals; Calcium; Cell Line; Cloning, Molecular; Cold Temperature; DNA, Complementary; Dogs; Dose-Response Relationship, Drug; Fluorometry; Ganglia, Spinal; Gene Library; Humans; Menthol; Mice; Molecular Sequence Data; Mustard Plant; Oocytes; Patch-Clamp Techniques; Plant Oils; Pyrazines; Pyridines; Pyrimidinones; Rats; Reverse Transcriptase Polymerase Chain Reaction; Sequence Alignment; Sequence Analysis, DNA; Sequence Homology, Amino Acid; Transfection; TRPM Cation Channels; Xenopus laevis

2006
High-throughput random mutagenesis screen reveals TRPM8 residues specifically required for activation by menthol.
    Nature neuroscience, 2006, Volume: 9, Issue:4

    Topics: Amino Acid Sequence; Animals; CHO Cells; Cold Temperature; Cricetinae; Gene Library; Menthol; Mice; Molecular Sequence Data; Molecular Structure; Mutagenesis; Patch-Clamp Techniques; Protein Structure, Tertiary; Pyrimidinones; TRPM Cation Channels

2006
Thermosensitive TRP ion channels mediate cytosolic calcium response in human synoviocytes.
    American journal of physiology. Cell physiology, 2006, Volume: 291, Issue:3

    Topics: Arthritis, Rheumatoid; Calcium; Calcium Channels; Calcium Signaling; Capsaicin; Cell Line, Tumor; Cells, Cultured; Chondrocalcinosis; Cytosol; Diterpenes; Hot Temperature; Humans; Inflammation; Nerve Tissue Proteins; Pyrimidinones; RNA, Messenger; Synovial Membrane; Transient Receptor Potential Channels; TRPA1 Cation Channel; TRPM Cation Channels; TRPV Cation Channels

2006
Icilin evokes a dose- and time-dependent increase in glutamate within the dorsal striatum of rats.
    Amino acids, 2006, Volume: 30, Issue:3

    Topics: Animals; Ankyrins; Behavior, Animal; Calcium Channels; Corpus Striatum; Dose-Response Relationship, Drug; Ganglia, Spinal; Glutamic Acid; Male; Pyrimidinones; Rats; Rats, Sprague-Dawley; Time Factors; TRPA1 Cation Channel; TRPC Cation Channels; TRPM Cation Channels

2006
Analgesia mediated by the TRPM8 cold receptor in chronic neuropathic pain.
    Current biology : CB, 2006, Aug-22, Volume: 16, Issue:16

    Topics: Acrolein; Amino Acids; Analgesia; Analysis of Variance; Animals; Blotting, Western; Cold Temperature; Dose-Response Relationship, Drug; Electrophysiology; Immunohistochemistry; Male; Menthol; Neuralgia; Oligonucleotides, Antisense; Pyrimidinones; Rats; Rats, Wistar; Receptors, Glutamate; Reflex; TRPM Cation Channels; Xanthenes

2006
Mu and kappa opioid receptor agonists antagonize icilin-induced wet-dog shaking in rats.
    European journal of pharmacology, 2006, Oct-10, Volume: 547, Issue:1-3

    Topics: 3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer; Animals; Behavior, Animal; Benzamides; Buprenorphine; Dose-Response Relationship, Drug; Injections, Intraperitoneal; Injections, Subcutaneous; Morphinans; Morphine; Piperazines; Pyrimidinones; Pyrrolidines; Rats; Rats, Sprague-Dawley; Receptors, Opioid, delta; Receptors, Opioid, kappa; Receptors, Opioid, mu; Spiro Compounds

2006
Prospects for prostate cancer imaging and therapy using high-affinity TRPM8 activators.
    Cell calcium, 2007, Volume: 41, Issue:3

    Topics: Animals; Antineoplastic Agents; Antipruritics; Biomarkers, Tumor; Cell Line, Tumor; Diagnostic Imaging; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; Humans; Ligands; Male; Menthol; Prostatic Neoplasms; Pyrimidinones; TRPM Cation Channels

2007
Nalfurafine, the kappa opioid agonist, inhibits icilin-induced wet-dog shakes in rats and antagonizes glutamate release in the dorsal striatum.
    Neuropharmacology, 2007, Volume: 52, Issue:3

    Topics: Analysis of Variance; Animals; Area Under Curve; Behavior, Animal; Corpus Striatum; Drug Interactions; Electrochemistry; Glutamic Acid; Male; Morphinans; Pyrimidinones; Rats; Rats, Sprague-Dawley; Receptors, Opioid, kappa; Shivering; Spiro Compounds

2007
Transient receptor potential channel A1 is directly gated by calcium ions.
    The Journal of biological chemistry, 2007, May-04, Volume: 282, Issue:18

    Topics: Calcium; Calcium Channels; Humans; Inflammation; Ion Channel Gating; Irritants; Mutagenesis, Site-Directed; Nerve Tissue Proteins; Protein Structure, Tertiary; Pyrimidinones; Transient Receptor Potential Channels; TRPA1 Cation Channel

2007
Transient receptor potential channel TRPM8 agonists stimulate calcium influx and neurotensin secretion in neuroendocrine tumor cells.
    Neuroendocrinology, 2007, Volume: 85, Issue:2

    Topics: Calcium; Humans; Membrane Potentials; Menthol; Models, Biological; Neuroendocrine Tumors; Neurotensin; Pancreatic Neoplasms; Pyrimidinones; TRPM Cation Channels; Tumor Cells, Cultured

2007
Regulation of transient receptor potential channels of melastatin type 8 (TRPM8): effect of cAMP, cannabinoid CB(1) receptors and endovanilloids.
    Experimental cell research, 2007, May-15, Volume: 313, Issue:9

    Topics: 8-Bromo Cyclic Adenosine Monophosphate; Arachidonic Acids; Benzaldehydes; Cannabinoid Receptor Modulators; Cell Line; Cell Membrane; Colforsin; Cyclic AMP; Cyclic AMP-Dependent Protein Kinases; Dopamine; Dose-Response Relationship, Drug; Drug Interactions; Endocannabinoids; Enzyme Inhibitors; Humans; Ion Channel Gating; Menthol; Polyunsaturated Alkamides; Pyrimidinones; Receptor, Cannabinoid, CB1; Signal Transduction; Transfection; TRPM Cation Channels

2007
TRPM8 is required for cold sensation in mice.
    Neuron, 2007, May-03, Volume: 54, Issue:3

    Topics: Animals; Behavior, Animal; Calcium; Choice Behavior; Cold Temperature; Formaldehyde; Mice; Mice, Knockout; Pain Measurement; Pyrimidinones; Reaction Time; Sensory Thresholds; Thermosensing; Time Factors; TRPM Cation Channels

2007
Attenuated cold sensitivity in TRPM8 null mice.
    Neuron, 2007, May-03, Volume: 54, Issue:3

    Topics: Analysis of Variance; Animals; Behavior, Animal; Calcium; Capsaicin; Cells, Cultured; Cold Temperature; Ganglia, Spinal; Inflammation; Methanol; Mice; Mice, Inbred C57BL; Mice, Knockout; Motor Activity; Neurons, Afferent; Pain Measurement; Pyrimidinones; Reaction Time; Thermosensing; TRPM Cation Channels

2007
Characterisation of TRPM8 as a pharmacophore receptor.
    Cell calcium, 2007, Volume: 42, Issue:6

    Topics: Calcium Signaling; Carboxylic Acids; Cell Line; Cell Line, Tumor; Cytophotometry; Dose-Response Relationship, Drug; Gene Expression; Humans; Membrane Potentials; Menthol; Molecular Structure; Oxides; Patch-Clamp Techniques; Phosphines; Pyrimidinones; Receptors, Cytoplasmic and Nuclear; Transfection; TRPM Cation Channels

2007
A pharmacological study of slowly adapting mechanoreceptors responsive to cold thermal stimulation.
    Neuroscience, 2007, Aug-24, Volume: 148, Issue:2

    Topics: Action Potentials; Adaptation, Physiological; Animals; Behavior, Animal; Cold Temperature; Dose-Response Relationship, Drug; Hot Temperature; Mechanoreceptors; Pyrimidinones; Rats; Rats, Wistar; Reaction Time; Temperature; Thermosensing

2007
Differential behavioral effect of the TRPM8/TRPA1 channel agonist icilin (AG-3-5).
    European journal of pharmacology, 2007, Dec-01, Volume: 575, Issue:1-3

    Topics: Animals; Behavior, Animal; Calcium Channels; Capsaicin; Dose-Response Relationship, Drug; Planarians; Pyrimidinones; Sensory System Agents; Time Factors; TRPM Cation Channels

2007
Contractile effect of TRPA1 receptor agonists in the isolated mouse intestine.
    European journal of pharmacology, 2007, Dec-08, Volume: 576, Issue:1-3

    Topics: Animals; Capsaicin; Disulfides; Gastrointestinal Motility; In Vitro Techniques; Intestines; Isothiocyanates; Male; Menthol; Mice; Pyrimidinones; RNA, Messenger; Sulfinic Acids; Transient Receptor Potential Channels; TRPA1 Cation Channel; TRPM Cation Channels; TRPV Cation Channels

2007
Impairment by activation of TRPA1 of gastric epithelial restitution in a wound model using RGM1 cell monolayer.
    Inflammopharmacology, 2007, Volume: 15, Issue:5

    Topics: Animals; Ankyrins; Calcium Channel Agonists; Calcium Channels; Capsaicin; Cell Line; Epithelial Cells; Gastric Mucosa; Isothiocyanates; Menthol; Pyrimidinones; Rats; Temperature; Time Factors; TRPA1 Cation Channel; TRPC Cation Channels; TRPM Cation Channels; TRPV Cation Channels; Wound Healing

2007
Plasticity in intact A delta- and C-fibers contributes to cold hypersensitivity in neuropathic rats.
    Neuroscience, 2007, Nov-30, Volume: 150, Issue:1

    Topics: Action Potentials; Analysis of Variance; Animals; Calcium; Cold Temperature; Disease Models, Animal; Dose-Response Relationship, Drug; Ganglia, Spinal; Hyperalgesia; Male; Nerve Fibers; Neural Conduction; Neuronal Plasticity; Neurons, Afferent; Pain Threshold; Peripheral Nervous System Diseases; Physical Stimulation; Pyrimidinones; Rats; Rats, Sprague-Dawley; Reaction Time; Statistics, Nonparametric

2007
Icilin induces a hyperthermia in rats that is dependent on nitric oxide production and NMDA receptor activation.
    European journal of pharmacology, 2008, Jan-14, Volume: 578, Issue:2-3

    Topics: Animals; Behavior, Animal; Body Temperature; Dose-Response Relationship, Drug; Enzyme Inhibitors; Excitatory Amino Acid Antagonists; Fever; Injections, Intramuscular; Injections, Intraperitoneal; Injections, Intraventricular; Isoquinolines; Male; NG-Nitroarginine Methyl Ester; Nitric Oxide; Nitric Oxide Synthase; Pyrimidinones; Rats; Rats, Sprague-Dawley; Receptors, N-Methyl-D-Aspartate; Time Factors; Tremor

2008
Comparison of icilin- and cold-evoked responses of spinal neurones, and their modulation of mechanical activity, in a model of neuropathic pain.
    Brain research, 2008, Jun-18, Volume: 1215

    Topics: Analysis of Variance; Animals; Ankyrins; Calcium; Calcium Channel Blockers; Calcium Channels; Cells, Cultured; Cold Temperature; Disease Models, Animal; Dose-Response Relationship, Drug; Evoked Potentials; Ganglia, Spinal; Hyperesthesia; Ligation; Male; Mechanoreceptors; Neuralgia; Neurons; Pain Threshold; Pyrimidinones; Rats; Rats, Sprague-Dawley; Spinal Cord; Spinal Nerves; TRPA1 Cation Channel; TRPC Cation Channels; TRPM Cation Channels

2008
Inhibition by the cold receptor agonists menthol and icilin of airway smooth muscle contraction.
    Pulmonary pharmacology & therapeutics, 2008, Volume: 21, Issue:5

    Topics: Animals; Calcium; Cold Temperature; Dose-Response Relationship, Drug; Guinea Pigs; In Vitro Techniques; Intracellular Fluid; Male; Menthol; Methacholine Chloride; Muscle Contraction; Muscle, Smooth; Potassium Chloride; Pyrimidinones; Spectrometry, Fluorescence; Thermoreceptors; Trachea

2008
Menthol derivative WS-12 selectively activates transient receptor potential melastatin-8 (TRPM8) ion channels.
    Pakistan journal of pharmaceutical sciences, 2008, Volume: 21, Issue:4

    Topics: Analgesics; Anilides; Animals; Calcium; Calcium Channels; Dose-Response Relationship, Drug; Gene Transfer Techniques; Humans; Hydrogen-Ion Concentration; Membrane Potentials; Menthol; Mice; Nerve Tissue Proteins; Pyrimidinones; Rats; Tachyphylaxis; Transient Receptor Potential Channels; TRPA1 Cation Channel; TRPM Cation Channels; TRPV Cation Channels; Xenopus laevis

2008
Inhibition of TRPM8 by icilin distinct from desensitization induced by menthol and menthol derivatives.
    The Journal of biological chemistry, 2009, Feb-13, Volume: 284, Issue:7

    Topics: Antipruritics; Calcium; Calcium Channels; Cell Line; Cold Temperature; Humans; Menthol; Mutation; Nerve Tissue Proteins; Phosphatidylinositol 4,5-Diphosphate; Pyrimidinones; Transient Receptor Potential Channels; TRPA1 Cation Channel; TRPM Cation Channels

2009
Comparative modeling of the quaternary structure for the human TRPM8 channel and analysis of its binding features.
    Biochimica et biophysica acta, 2009, Volume: 1788, Issue:5

    Topics: Binding Sites; Biophysical Phenomena; Humans; Ion Channel Gating; Ligands; Menthol; Models, Molecular; Protein Structure, Quaternary; Protein Structure, Tertiary; Pyrimidinones; Static Electricity; TRPM Cation Channels

2009
Icilin-induced wet-dog shakes in rats are dependent on NMDA receptor activation and nitric oxide production.
    Pharmacology, biochemistry, and behavior, 2009, Volume: 92, Issue:3

    Topics: Animals; Dose-Response Relationship, Drug; Enzyme Inhibitors; Male; NG-Nitroarginine Methyl Ester; Nitric Oxide; Nitric Oxide Synthase; Pyrimidinones; Rats; Rats, Sprague-Dawley; Receptors, N-Methyl-D-Aspartate; Tremor

2009
Non-neuronal expression of transient receptor potential type A1 (TRPA1) in human skin.
    The Journal of investigative dermatology, 2009, Volume: 129, Issue:9

    Topics: Calcium Channels; Fluorescent Antibody Technique; Gene Expression Profiling; Heat-Shock Proteins; HSP27 Heat-Shock Proteins; HSP90 Heat-Shock Proteins; Humans; Molecular Chaperones; Nerve Tissue Proteins; Pyrimidinones; Skin; Transient Receptor Potential Channels; TRPA1 Cation Channel

2009
Primary afferents with TRPM8 and TRPA1 profiles target distinct subpopulations of rat superficial dorsal horn neurones.
    British journal of pharmacology, 2009, Volume: 157, Issue:3

    Topics: Afferent Pathways; Animals; Ankyrins; Calcium Channels; Cold Temperature; Excitatory Postsynaptic Potentials; Glutamic Acid; In Vitro Techniques; Male; Menthol; Patch-Clamp Techniques; Posterior Horn Cells; Pyrimidinones; Rats; Rats, Sprague-Dawley; Synaptic Transmission; TRPA1 Cation Channel; TRPC Cation Channels; TRPM Cation Channels

2009
Dose-dependent effects of icilin on thermal preference in the hindpaw and face of rats.
    The journal of pain, 2009, Volume: 10, Issue:6

    Topics: Analysis of Variance; Animals; Behavior, Animal; Cold Temperature; Dose-Response Relationship, Drug; Face; Foot; Hindlimb; Hot Temperature; Male; Motor Activity; Pyrimidinones; Rats; Rats, Hairless; Rats, Long-Evans; Rats, Sprague-Dawley; Sensory System Agents; Temperature

2009
Letter to the editor: "Is menthol- or icilin-induced vasodilation mediated by the activation of TRPM8?".
    American journal of physiology. Heart and circulatory physiology, 2009, Volume: 297, Issue:2

    Topics: Animals; Humans; Menthol; Pyrimidinones; TRPM Cation Channels; Vasodilation

2009
Effects of transient receptor potential (TRP) channel agonists and antagonists on slowly adapting type II mechanoreceptors in the rat sinus hair follicle.
    Journal of the peripheral nervous system : JPNS, 2009, Volume: 14, Issue:4

    Topics: Acrolein; Action Potentials; Animals; Ankyrins; Calcium Channels; Camphor; Capsaicin; Evoked Potentials; Hair Follicle; In Vitro Techniques; Isothiocyanates; Male; Mechanoreceptors; Menthol; Physical Stimulation; Pyrimidinones; Rats; Rats, Wistar; Ruthenium Red; Time Factors; Transient Receptor Potential Channels; TRPA1 Cation Channel; TRPC Cation Channels; TRPV Cation Channels

2009
The roles of iPLA2, TRPM8 and TRPA1 in chemically induced cold hypersensitivity.
    Molecular pain, 2010, Jan-21, Volume: 6

    Topics: Animals; Antipruritics; Cold Temperature; Dose-Response Relationship, Drug; Foot; Group VI Phospholipases A2; Hyperalgesia; Male; Menthol; Mice; Mice, Knockout; Naphthalenes; Nociceptors; Pain Measurement; Pain Threshold; Pyrimidinones; Pyrones; Rats; Rats, Wistar; Sensory Receptor Cells; Thermosensing; Transient Receptor Potential Channels; TRPA1 Cation Channel; TRPM Cation Channels

2010
Estrogen regulation of TRPM8 expression in breast cancer cells.
    BMC cancer, 2010, May-19, Volume: 10

    Topics: Adenocarcinoma; Blotting, Western; Breast Neoplasms; Calcium; Cell Line, Tumor; Estradiol; Estrogen Receptor alpha; Female; Gene Expression Regulation, Neoplastic; Humans; Immunohistochemistry; Membrane Potentials; Patch-Clamp Techniques; Pyrimidinones; Reverse Transcriptase Polymerase Chain Reaction; RNA Interference; RNA, Messenger; Time Factors; TRPM Cation Channels

2010
Grueneberg ganglion neurons are finely tuned cold sensors.
    The Journal of neuroscience : the official journal of the Society for Neuroscience, 2010, Jun-02, Volume: 30, Issue:22

    Topics: 1-Methyl-3-isobutylxanthine; Animals; Animals, Newborn; Calcium; Calcium Signaling; Cold Temperature; Colforsin; Cyclic GMP; Cyclic Nucleotide-Gated Cation Channels; Ganglia, Sensory; Green Fluorescent Proteins; In Vitro Techniques; Isothiocyanates; Mice; Mice, Transgenic; Microscopy, Confocal; Nasal Cavity; Olfactory Bulb; Olfactory Marker Protein; Olfactory Pathways; Phosphodiesterase Inhibitors; Pyrimidinones; Sensory Receptor Cells; Sodium Channel Blockers; Tetrodotoxin; Thermosensing; Time Factors; Transient Receptor Potential Channels; TRPA1 Cation Channel

2010
Contribution of the S5-pore-S6 domain to the gating characteristics of the cation channels TRPM2 and TRPM8.
    The Journal of biological chemistry, 2010, Aug-27, Volume: 285, Issue:35

    Topics: Adenosine Diphosphate Ribose; Antipruritics; Calcium; Cell Line; Cold Temperature; Humans; Hydrogen Peroxide; Ion Channel Gating; Membrane Potentials; Menthol; Oxidants; Protein Structure, Tertiary; Pyrimidinones; Recombinant Fusion Proteins; TRPM Cation Channels

2010
Chronic treatment with NGF induces spontaneous fluctuations of intracellular Ca(2+) in icilin-sensitive dorsal root ganglion neurons of the rat.
    The Journal of veterinary medical science, 2010, Volume: 72, Issue:12

    Topics: Animals; Calcium; Capsaicin; Cells, Cultured; Drug Administration Schedule; Ganglia, Spinal; Male; Nerve Growth Factor; Neurons; Pyrimidinones; Rats; Rats, Sprague-Dawley

2010
Dissociation of μ- and δ-opioid inhibition of glutamatergic synaptic transmission in superficial dorsal horn.
    Molecular pain, 2010, Oct-26, Volume: 6

    Topics: Animals; Calcium; Calcium Channels; Excitatory Postsynaptic Potentials; Glutamates; In Vitro Techniques; Male; Menthol; Posterior Horn Cells; Presynaptic Terminals; Pyrimidinones; Rats; Rats, Sprague-Dawley; Receptors, Opioid, delta; Receptors, Opioid, mu; Synaptic Transmission

2010
Pharmacological and functional properties of TRPM8 channels in prostate tumor cells.
    Pflugers Archiv : European journal of physiology, 2011, Volume: 461, Issue:1

    Topics: Arginine; Calcium; Cell Line; Cell Line, Tumor; Cell Membrane; Clotrimazole; Cold Temperature; Endoplasmic Reticulum; Glycine; Humans; Male; Menthol; Prostate; Prostatic Neoplasms; Pyrazines; Pyridines; Pyrimidinones; TRPM Cation Channels

2011
Inhibition of the cardiac L-type calcium channel current by the TRPM8 agonist, (-)-menthol.
    Journal of physiology and pharmacology : an official journal of the Polish Physiological Society, 2010, Volume: 61, Issue:5

    Topics: Animals; Calcium Channel Blockers; Calcium Channels, L-Type; Cell Line; Cold Temperature; Heart Ventricles; Male; Membrane Potentials; Menthol; Myocytes, Cardiac; Nimodipine; Patch-Clamp Techniques; Pyrimidinones; Rabbits; TRPM Cation Channels

2010
Sensitization of capsaicin and icilin responses in oxaliplatin treated adult rat DRG neurons.
    Molecular pain, 2010, Nov-24, Volume: 6

    Topics: Animals; Antineoplastic Agents; Capsaicin; Cells, Cultured; Cyclic AMP; Drug Interactions; Neurons; Neurotoxicity Syndromes; Organoplatinum Compounds; Oxaliplatin; Pyrimidinones; Rats; Sensory System Agents; TRPM Cation Channels

2010
Icilin induces G1 arrest through activating JNK and p38 kinase in a TRPM8-independent manner.
    Biochemical and biophysical research communications, 2011, Mar-04, Volume: 406, Issue:1

    Topics: Cell Line, Tumor; Enzyme Activation; G1 Phase; Humans; Male; MAP Kinase Kinase 4; p38 Mitogen-Activated Protein Kinases; Prostatic Neoplasms; Pyrimidinones; TRPM Cation Channels

2011
Icilin-evoked behavioral stimulation is attenuated by alpha₂-adrenoceptor activation.
    Brain research, 2011, Apr-12, Volume: 1384

    Topics: Adrenergic alpha-2 Receptor Agonists; Adrenergic alpha-2 Receptor Antagonists; Agmatine; Analysis of Variance; Animals; Behavior, Animal; Clonidine; Disease Models, Animal; Dose-Response Relationship, Drug; Head Movements; Male; Movement Disorders; Pyrimidinones; Rats; Rats, Sprague-Dawley; Receptors, Adrenergic, alpha-2; Time Factors; Yohimbine

2011
TRPM8 in mouse sperm detects temperature changes and may influence the acrosome reaction.
    Journal of cellular physiology, 2011, Volume: 226, Issue:6

    Topics: Acrosome Reaction; Animals; Capsaicin; Humans; Ion Channel Gating; Male; Menthol; Mice; Mice, Knockout; Pyrazines; Pyridines; Pyrimidinones; Spermatozoa; Temperature; Testis; TRPM Cation Channels

2011
Characterization of TRPM8-like channels activated by the cooling agent icilin in the macrophage cell line RAW 264.7.
    The Journal of membrane biology, 2011, Volume: 241, Issue:1

    Topics: Animals; Cell Line; Electrophysiology; Macrophages; Membrane Potentials; Mice; Pyrimidinones; TRPM Cation Channels

2011
A novel role for TRPM8 in visceral afferent function.
    Pain, 2011, Volume: 152, Issue:7

    Topics: Action Potentials; Animals; Calcitonin Gene-Related Peptide; Cells, Cultured; Cholera Toxin; Colon; Fluorescent Dyes; Ganglia, Spinal; Gene Expression; Hyperalgesia; Male; Mice; Mice, Inbred C57BL; Mice, Knockout; Microdissection; Pyrimidinones; Sensory Receptor Cells; TRPM Cation Channels; TRPV Cation Channels; Visceral Afferents

2011
Topical TRPM8 agonist (icilin) relieved vulva pruritus originating from lichen sclerosus et atrophicus.
    Acta dermato-venereologica, 2012, Volume: 92, Issue:5

    Topics: Administration, Cutaneous; Antipruritics; Female; Humans; Lichen Sclerosus et Atrophicus; Middle Aged; Pruritus; Pyrimidinones; Treatment Outcome; TRPM Cation Channels; Vulvar Lichen Sclerosus

2012
[Comparative effects of menthol and icilin on the induced contraction of the smooth muscles of the vas deferens of normal and castrated rats].
    Fiziolohichnyi zhurnal (Kiev, Ukraine : 1994), 2011, Volume: 57, Issue:4

    Topics: Adrenergic alpha-Agonists; Animals; Epididymis; Male; Menthol; Muscarinic Agonists; Muscle Contraction; Muscle, Smooth; Orchiectomy; Potassium Chloride; Prostate; Pyrimidinones; Rats; TRPM Cation Channels; Vas Deferens

2011
Blockade of TRPM8 activity reduces the invasion potential of oral squamous carcinoma cell lines.
    International journal of oncology, 2012, Volume: 40, Issue:5

    Topics: Anilides; Antineoplastic Agents; Calcium Signaling; Carcinoma, Squamous Cell; Cell Line, Tumor; Cell Movement; Cell Proliferation; Humans; Immunohistochemistry; Matrix Metalloproteinase 9; Membrane Potentials; Menthol; Neoplasm Invasiveness; Patch-Clamp Techniques; Pyrimidinones; Real-Time Polymerase Chain Reaction; Reverse Transcriptase Polymerase Chain Reaction; RNA, Messenger; Tongue Neoplasms; TRPM Cation Channels

2012
Fused piperidines as a novel class of potent and orally available transient receptor potential melastatin type 8 (TRPM8) antagonists.
    Journal of medicinal chemistry, 2012, Feb-23, Volume: 55, Issue:4

    Topics: Administration, Oral; Analgesics; Animals; Calcium; CHO Cells; Cricetinae; Cricetulus; In Vitro Techniques; Male; Microsomes, Liver; Piperidines; Pyrimidinones; Rats; Rats, Sprague-Dawley; Stereoisomerism; Structure-Activity Relationship; TRPM Cation Channels

2012
Supercooling agent icilin blocks a warmth-sensing ion channel TRPV3.
    TheScientificWorldJournal, 2012, Volume: 2012

    Topics: Animals; Cells, Cultured; Hot Temperature; Humans; Pyrimidinones; TRPV Cation Channels; Xenopus laevis

2012
TRPA1-like channels enhance glycinergic transmission in medullary dorsal horn neurons.
    Journal of neurochemistry, 2012, Volume: 122, Issue:4

    Topics: Acetanilides; Action Potentials; Animals; Cadmium; Calcium Channel Blockers; Calcium Signaling; Data Interpretation, Statistical; Dose-Response Relationship, Drug; Excitatory Postsynaptic Potentials; Female; Glycine; Male; Medulla Oblongata; Patch-Clamp Techniques; Posterior Horn Cells; Purines; Pyrimidinones; Rats; Rats, Sprague-Dawley; Real-Time Polymerase Chain Reaction; Synaptic Transmission; TRPA1 Cation Channel; TRPC Cation Channels

2012
Importance of a conserved sequence motif in transmembrane segment S3 for the gating of human TRPM8 and TRPM2.
    PloS one, 2012, Volume: 7, Issue:11

    Topics: Conserved Sequence; HEK293 Cells; Humans; Mutation; Nucleotide Motifs; Patch-Clamp Techniques; Protein Structure, Tertiary; Protein Transport; Pyrimidinones; Static Electricity; Surface Properties; TRPM Cation Channels

2012
TRPM8 ion channels differentially modulate proliferation and cell cycle distribution of normal and cancer prostate cells.
    PloS one, 2012, Volume: 7, Issue:12

    Topics: Benzamides; Cell Cycle; Cell Line; Cell Line, Tumor; Cell Proliferation; Humans; Ion Channels; Male; Menthol; Prostate; Prostatic Neoplasms; Pyrimidinones; Thiophenes; Transfection; TRPM Cation Channels; Wound Healing

2012
Lack of transient receptor potential melastatin 8 activation by phthalate esters that enhance contact hypersensitivity in mice.
    Toxicology letters, 2013, Mar-13, Volume: 217, Issue:3

    Topics: Acetanilides; Animals; Calcium; CHO Cells; Cricetinae; Dermatitis, Contact; Dose-Response Relationship, Drug; Menthol; Mice; Phthalic Acids; Plasticizers; Purines; Pyrimidinones; TRPM Cation Channels; TRPV Cation Channels

2013
Arylglycine derivatives as potent transient receptor potential melastatin 8 (TRPM8) antagonists.
    Bioorganic & medicinal chemistry letters, 2013, Apr-01, Volume: 23, Issue:7

    Topics: Animals; Behavior, Animal; Dose-Response Relationship, Drug; Glycine; HEK293 Cells; Humans; Molecular Structure; Pyrimidinones; Rats; Stereoisomerism; Structure-Activity Relationship; TRPM Cation Channels

2013
Peptidergic CGRPα primary sensory neurons encode heat and itch and tonically suppress sensitivity to cold.
    Neuron, 2013, Apr-10, Volume: 78, Issue:1

    Topics: Animals; Calcitonin Gene-Related Peptide; Capsaicin; Cold Temperature; Diphtheria Toxin; Excitatory Postsynaptic Potentials; Female; Ganglia, Spinal; Gene Expression Regulation; Green Fluorescent Proteins; Histamine; Hot Temperature; In Vitro Techniques; Lectins; Male; Mice; Mice, Transgenic; Neurofilament Proteins; Pruritus; Pyrimidinones; Reaction Time; Receptors, Calcitonin Gene-Related Peptide; Sensory Receptor Cells; Sensory Thresholds; Skin; Sural Nerve; Time Factors; TRPM Cation Channels; TRPV Cation Channels; Ubiquitin Thiolesterase

2013
TRPM8 activation attenuates inflammatory responses in mouse models of colitis.
    Proceedings of the National Academy of Sciences of the United States of America, 2013, Apr-30, Volume: 110, Issue:18

    Topics: Animals; Calcitonin Gene-Related Peptide; Calcium Signaling; Chemokines; Colitis; Colon; Dextran Sulfate; Disease Models, Animal; Humans; Inflammation; Inflammation Mediators; Ion Channel Gating; Mice; Mice, Knockout; Pyrimidinones; Trinitrobenzenesulfonic Acid; TRPM Cation Channels; TRPV Cation Channels

2013
TRPM8 agonists modulate contraction of the pig urinary bladder.
    Canadian journal of physiology and pharmacology, 2013, Volume: 91, Issue:7

    Topics: Animals; Female; Menthol; Muscle Contraction; Pyrimidinones; Swine; TRPM Cation Channels; Urinary Bladder; Urothelium

2013
Camphor activates and sensitizes transient receptor potential melastatin 8 (TRPM8) to cooling and icilin.
    Chemical senses, 2013, Volume: 38, Issue:7

    Topics: Animals; Base Sequence; Boron Compounds; Calcium; Camphor; Cells, Cultured; Chickens; Cold Temperature; Dose-Response Relationship, Drug; Electrophysiology; Ganglia, Spinal; HEK293 Cells; Humans; Male; Menthol; Molecular Sequence Data; Pyrimidinones; Rats; Rats, Wistar; Ruthenium Red; TRPM Cation Channels

2013
Calcium regulation by temperature-sensitive transient receptor potential channels in human uveal melanoma cells.
    Cellular signalling, 2014, Volume: 26, Issue:1

    Topics: Benzoxazines; Calcium; Capsaicin; Cell Line, Tumor; Gene Expression Regulation, Neoplastic; Humans; Immunohistochemistry; Ion Channel Gating; Melanoma; Models, Biological; Morpholines; Naphthalenes; Pyrimidinones; Receptor, Cannabinoid, CB1; RNA, Messenger; Temperature; Transient Receptor Potential Channels; Uveal Neoplasms

2014
Icilin inhibits E2F1-mediated cell cycle regulatory programs in prostate cancer.
    Biochemical and biophysical research communications, 2013, Nov-29, Volume: 441, Issue:4

    Topics: Cell Cycle; Cell Line, Tumor; DNA, Superhelical; E2F1 Transcription Factor; Humans; Male; Prostatic Neoplasms; Pyrimidinones

2013
Human white adipocytes express the cold receptor TRPM8 which activation induces UCP1 expression, mitochondrial activation and heat production.
    Molecular and cellular endocrinology, 2014, Mar-05, Volume: 383, Issue:1-2

    Topics: Adipocytes, White; Body Temperature Regulation; Cold Temperature; Gene Expression Regulation; Glucose; Humans; Intra-Abdominal Fat; Ion Channels; Membrane Potential, Mitochondrial; Menthol; Mitochondria; Mitochondrial Proteins; Primary Cell Culture; Pyrimidinones; Signal Transduction; Subcutaneous Fat; TRPM Cation Channels; Uncoupling Protein 1

2014
Functional expression of TRPM8 and TRPA1 channels in rat odontoblasts.
    PloS one, 2013, Volume: 8, Issue:12

    Topics: Animals; Calcium; Calcium Signaling; Dentin; Male; Menthol; Odontoblasts; Pyrimidinones; Rats; Rats, Wistar; TRPA1 Cation Channel; TRPC Cation Channels; TRPM Cation Channels

2013
Activation and inhibition of thermosensitive TRP channels by voacangine, an alkaloid present in Voacanga africana, an African tree.
    Journal of natural products, 2014, Feb-28, Volume: 77, Issue:2

    Topics: Africa; Alkaloids; Calcium; Capsaicin; Humans; Ibogaine; Menthol; Molecular Structure; Plant Bark; Pyrimidinones; Transient Receptor Potential Channels; Trees; TRPV Cation Channels; Voacanga

2014
Icilin reduces voltage-gated calcium channel currents in naïve and injured DRG neurons in the rat spinal nerve ligation model.
    Brain research, 2014, Apr-04, Volume: 1557

    Topics: Animals; Calcium Channel Blockers; Calcium Channels, L-Type; Calcium Channels, N-Type; Cells, Cultured; Cold Temperature; Disease Models, Animal; Dose-Response Relationship, Drug; Ganglia, Spinal; Hyperalgesia; Ligation; Male; Membrane Potentials; Neuralgia; Neurons; Patch-Clamp Techniques; Peripheral Nerve Injuries; Pyrimidinones; Rats; Rats, Wistar; Spinal Nerves; TRPM Cation Channels

2014
Optimization of potency and pharmacokinetic properties of tetrahydroisoquinoline transient receptor potential melastatin 8 (TRPM8) antagonists.
    Journal of medicinal chemistry, 2014, Apr-10, Volume: 57, Issue:7

    Topics: Animals; Behavior, Animal; Circular Dichroism; Cold Temperature; Dogs; Humans; Male; Microsomes, Liver; Motor Activity; Pyrimidinones; Rats; Rats, Sprague-Dawley; Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization; Stereoisomerism; Tetrahydroisoquinolines; Tissue Distribution; TRPM Cation Channels

2014
Characterization of functional transient receptor potential melastatin 8 channels in human pancreatic ductal adenocarcinoma cells.
    Pancreas, 2014, Volume: 43, Issue:5

    Topics: Adenocarcinoma; Benzamides; Blotting, Western; Carcinoma, Pancreatic Ductal; Cell Line; Cell Line, Tumor; Cell Membrane; Cell Movement; HEK293 Cells; Humans; Immunohistochemistry; Membrane Potentials; Membrane Proteins; Menthol; Pancreatic Neoplasms; Patch-Clamp Techniques; Pyrimidinones; RNA Interference; Thiophenes; TRPM Cation Channels

2014
TRPA1 and TRPV4 activation in human odontoblasts stimulates ATP release.
    Journal of dental research, 2014, Volume: 93, Issue:9

    Topics: Acetanilides; Acrolein; Adenosine Triphosphate; Calcium Channels; Calcium Signaling; Capsaicin; Cell Culture Techniques; Cell Line; Culture Media, Conditioned; Dental Pulp; Humans; Isothiocyanates; Leucine; Nerve Tissue Proteins; Nociceptors; Odontoblasts; Purines; Pyrimidinones; Sensory System Agents; Sulfonamides; Transient Receptor Potential Channels; TRPA1 Cation Channel; TRPM Cation Channels; TRPV Cation Channels

2014
Enhanced behavioral responses to cold stimuli following CGRPα sensory neuron ablation are dependent on TRPM8.
    Molecular pain, 2014, Nov-19, Volume: 10

    Topics: Animals; Body Temperature Regulation; Body Weight; Calcitonin Gene-Related Peptide; Cell Count; Cold Temperature; Diphtheria Toxin; Ganglia, Spinal; Heparin-binding EGF-like Growth Factor; Hot Temperature; Humans; Hyperalgesia; Male; Mice; Mice, Transgenic; Neurofilament Proteins; Phosphopyruvate Hydratase; Pyrimidinones; Sensory Receptor Cells; Sensory Thresholds; TRPM Cation Channels

2014
Thyronamine induces TRPM8 channel activation in human conjunctival epithelial cells.
    Cellular signalling, 2015, Volume: 27, Issue:2

    Topics: Calcium; Capsaicin; Cell Line; Conjunctiva; Epithelial Cells; Humans; Interleukin-6; Membrane Potentials; Patch-Clamp Techniques; Pyrimidinones; RNA, Messenger; Thyronines; TRPM Cation Channels; TRPV Cation Channels

2015
AMG2850, a potent and selective TRPM8 antagonist, is not effective in rat models of inflammatory mechanical hypersensitivity and neuropathic tactile allodynia.
    Naunyn-Schmiedeberg's archives of pharmacology, 2015, Volume: 388, Issue:4

    Topics: Action Potentials; Animals; Behavior, Animal; Blood Pressure; Brain; Calcium; CHO Cells; Cold Temperature; Cricetinae; Cricetulus; Freund's Adjuvant; Humans; Hyperalgesia; Male; Menthol; Mice, Inbred C57BL; Naphthyridines; Pain; Pyrimidinones; Rats; Rats, Sprague-Dawley; Sciatic Nerve; TRPM Cation Channels

2015
Expression and function of the epithelial sodium channel δ-subunit in human respiratory epithelial cells in vitro.
    Pflugers Archiv : European journal of physiology, 2015, Volume: 467, Issue:11

    Topics: Capsaicin; Diuretics; Epithelial Cells; Epithelial Sodium Channels; Evans Blue; Gene Knockdown Techniques; Humans; Primary Cell Culture; Pulmonary Alveoli; Pyrimidinones; Respiratory Mucosa; Sodium

2015
Structure-activity relationships of the prototypical TRPM8 agonist icilin.
    Bioorganic & medicinal chemistry letters, 2015, Jun-01, Volume: 25, Issue:11

    Topics: HEK293 Cells; Humans; Molecular Structure; Pyrimidinones; Structure-Activity Relationship; TRPM Cation Channels

2015
Meningeal transient receptor potential channel M8 activation causes cutaneous facial and hindpaw allodynia in a preclinical rodent model of headache.
    Cephalalgia : an international journal of headache, 2016, Volume: 36, Issue:2

    Topics: Animals; Disease Models, Animal; Hyperalgesia; Male; Migraine Disorders; Pyrimidinones; Rats; Rats, Sprague-Dawley; TRPM Cation Channels

2016
3-Iodothyronamine increases transient receptor potential melastatin channel 8 (TRPM8) activity in immortalized human corneal epithelial cells.
    Cellular signalling, 2016, Volume: 28, Issue:3

    Topics: Calcium; Capsaicin; Cell Line; Epithelial Cells; Humans; Interleukin-6; Membrane Potentials; Patch-Clamp Techniques; Pyrazines; Pyridines; Pyrimidinones; Thyronines; TRPM Cation Channels; TRPV Cation Channels

2016
VAMP7 regulates constitutive membrane incorporation of the cold-activated channel TRPM8.
    Nature communications, 2016, Feb-04, Volume: 7

    Topics: Animals; Calcium; Cell Membrane; Cold Temperature; Female; Ganglia, Spinal; HEK293 Cells; Humans; Hyperesthesia; Lysosomal Membrane Proteins; Mice; Mice, Inbred C57BL; Mice, Knockout; Microscopy, Fluorescence; Patch-Clamp Techniques; Pyrimidinones; R-SNARE Proteins; Reverse Transcriptase Polymerase Chain Reaction; Sensory Receptor Cells; Transport Vesicles; Trigeminal Ganglion; TRPM Cation Channels

2016
Activation of Cold-Sensitive Channels TRPM8 and TRPA1 Inhibits the Proliferative Airway Smooth Muscle Cell Phenotype.
    Lung, 2016, Volume: 194, Issue:4

    Topics: Actins; Airway Remodeling; Animals; Asthma; Bronchi; Calcium Channel Agonists; Cell Movement; Cell Proliferation; Cold Temperature; Disease Models, Animal; Female; Matrix Metalloproteinase 2; Menthol; Microfilament Proteins; Muscle Contraction; Muscle Proteins; Myocytes, Smooth Muscle; p21-Activated Kinases; p38 Mitogen-Activated Protein Kinases; Phenotype; Platelet-Derived Growth Factor; Pyrimidinones; Rats; Rats, Sprague-Dawley; Signal Transduction; Trachea; TRPA1 Cation Channel; TRPM Cation Channels

2016
Two different avian cold-sensitive sensory neurons: Transient receptor potential melastatin 8 (TRPM8)-dependent and -independent activation mechanisms.
    Neuropharmacology, 2016, Volume: 111

    Topics: Anilides; Animals; Avian Proteins; Calcium Signaling; Chickens; Cold Temperature; Ganglia, Spinal; HEK293 Cells; Humans; Menthol; Pyrimidinones; Thermoreceptors; Thermosensing; Transient Receptor Potential Channels; TRPM Cation Channels

2016
Ion channel mechanisms of rat tail artery contraction-relaxation by menthol involving, respectively, TRPM8 activation and L-type Ca2+ channel inhibition.
    American journal of physiology. Heart and circulatory physiology, 2016, 12-01, Volume: 311, Issue:6

    Topics: Anilides; Animals; Antipruritics; Arteries; Calcium Channels, L-Type; Calcium Signaling; Immunohistochemistry; Menthol; Muscle Contraction; Muscle Relaxation; Muscle, Smooth, Vascular; Myocytes, Smooth Muscle; Pyrimidinones; Rats; Tail; TRPM Cation Channels; Vasoconstriction; Vasodilation

2016
The cooling compound icilin attenuates autoimmune neuroinflammation through modulation of the T-cell response.
    FASEB journal : official publication of the Federation of American Societies for Experimental Biology, 2018, Volume: 32, Issue:3

    Topics: Animals; Calcium; Calcium Channel Agonists; Cells, Cultured; Encephalomyelitis, Autoimmune, Experimental; Female; Inflammation; Inflammation Mediators; Mice; Mice, Inbred C57BL; Mice, Knockout; Pyrimidinones; T-Lymphocytes; TRPA1 Cation Channel; TRPM Cation Channels

2018
Transient Receptor Potential Melastatin-8 Activation Induces Relaxation of Pulmonary Artery by Inhibition of Store-Operated Calcium Entry in Normoxic and Chronic Hypoxic Pulmonary Hypertensive Rats.
    The Journal of pharmacology and experimental therapeutics, 2018, Volume: 365, Issue:3

    Topics: Animals; Biological Transport; Calcium; Cell Hypoxia; Endothelin-1; Gene Expression Regulation; Hypertension, Pulmonary; Male; Myocytes, Smooth Muscle; Pulmonary Artery; Pyrimidinones; Rats; Rats, Sprague-Dawley; TRPC Cation Channels; TRPM Cation Channels; Vasoconstriction; Vasodilation

2018
Discovery of TRPM8 Antagonist ( S)-6-(((3-Fluoro-4-(trifluoromethoxy)phenyl)(3-fluoropyridin-2-yl)methyl)carbamoyl)nicotinic Acid (AMG 333), a Clinical Candidate for the Treatment of Migraine.
    Journal of medicinal chemistry, 2018, 09-27, Volume: 61, Issue:18

    Topics: Animals; Anticonvulsants; Calcium Channel Agonists; Drug Discovery; Humans; Male; Microsomes, Liver; Migraine Disorders; Models, Molecular; Molecular Structure; Niacin; Pyrimidinones; Rats; Rats, Sprague-Dawley; Seizures; TRPM Cation Channels

2018
Coordinated targeting of cold and nicotinic receptors synergistically improves obesity and type 2 diabetes.
    Nature communications, 2018, 10-23, Volume: 9, Issue:1

    Topics: Adipose Tissue, Brown; Animals; Body Weight; Cold Temperature; Diabetes Mellitus, Type 2; Diet; Dimethylphenylpiperazinium Iodide; Energy Metabolism; Fatty Liver; Glucose Intolerance; Insulin Resistance; Male; Melanocortins; Mice, Inbred C57BL; Mice, Obese; Obesity; Pyrimidinones; Receptor, Melanocortin, Type 4; Receptors, Nicotinic; Thermogenesis; TRPM Cation Channels

2018
Structural basis of cooling agent and lipid sensing by the cold-activated TRPM8 channel.
    Science (New York, N.Y.), 2019, 03-01, Volume: 363, Issue:6430

    Topics: Animals; Binding Sites; Calcium; Cold Temperature; Cryoelectron Microscopy; Membrane Lipids; Menthol; Models, Molecular; Phosphatidylinositol 4,5-Diphosphate; Protein Structure, Tertiary; Pyrimidinones; Songbirds; TRPM Cation Channels

2019
Pirt deficiency has subtle female-specific effects on energy and glucose metabolism in mice.
    Molecular metabolism, 2019, Volume: 23

    Topics: Adipose Tissue, Brown; Animals; Calcium Channel Agonists; Carrier Proteins; Diet, Fat-Restricted; Diet, High-Fat; Energy Metabolism; Female; Gene Knockout Techniques; Glucose; Glucose Intolerance; Glucose Tolerance Test; Male; Membrane Proteins; Mice; Mice, Inbred C57BL; Mice, Knockout; Obesity; Pyrimidinones; Sex Factors; Thermogenesis; Transcriptome; TRPM Cation Channels

2019
TRPM8-mediated cutaneous stimulation modulates motor neuron activity during treadmill stepping in mice.
    The journal of physiological sciences : JPS, 2019, Volume: 69, Issue:6

    Topics: Animals; Exercise Test; Gene Expression Regulation; Male; Mice; Mice, Inbred C57BL; Motor Neurons; Physical Conditioning, Animal; Proto-Oncogene Proteins c-fos; Pyrimidinones; Skin; TRPM Cation Channels

2019
The super-cooling compound icilin stimulates c-Fos and Egr-1 expression and activity involving TRPM8 channel activation, Ca
    Biochemical pharmacology, 2020, Volume: 177

    Topics: Calcium; Calcium Channels; Early Growth Response Protein 1; ets-Domain Protein Elk-1; Gene Expression Regulation; Gene Transfer Techniques; Genes, fos; HEK293 Cells; Humans; Ions; Promoter Regions, Genetic; Proto-Oncogene Proteins c-fos; Pyrimidinones; Signal Transduction; Transcription, Genetic; Transcriptional Activation; TRPM Cation Channels

2020
Why wild giant pandas frequently roll in horse manure.
    Proceedings of the National Academy of Sciences of the United States of America, 2020, 12-22, Volume: 117, Issue:51

    Topics: Animals; Behavior, Animal; Female; HEK293 Cells; Horses; Humans; Male; Manure; Mice, Inbred C57BL; Phylogeny; Polycyclic Sesquiterpenes; Pyrimidinones; Rats, Wistar; Temperature; TRPM Cation Channels; Ursidae

2020
Identification of N-acyl-N-indanyl-α-phenylglycinamides as selective TRPM8 antagonists designed to mitigate the risk of adverse effects.
    Bioorganic & medicinal chemistry, 2021, 01-15, Volume: 30

    Topics: Administration, Oral; Animals; Behavior, Animal; Dogs; Dose-Response Relationship, Drug; Female; Humans; Molecular Structure; Pyrimidinones; Rats; Rats, Sprague-Dawley; Risk Factors; Structure-Activity Relationship; TRPM Cation Channels

2021
The cold receptor TRPM8 activation leads to attenuation of endothelium-dependent cerebral vascular functions during head cooling.
    Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism, 2021, Volume: 41, Issue:11

    Topics: Animals; Animals, Newborn; Arterioles; Body Temperature; Bradykinin; Brain; Cerebrovascular Circulation; Endothelium; Female; Glutamic Acid; Head; Hypercapnia; Hypothermia, Induced; Male; Nitroprusside; Pyrimidinones; Rewarming; Sodium Channel Agonists; Swine; TRPM Cation Channels; Vasodilation; Vasodilator Agents

2021
Activation mechanism of the mouse cold-sensing TRPM8 channel by cooling agonist and PIP
    Science (New York, N.Y.), 2022, 10-14, Volume: 378, Issue:6616

    Topics: Animals; Cold Temperature; Cryoelectron Microscopy; Ion Channel Gating; Ligands; Menthol; Mice; Phosphatidylinositol 4,5-Diphosphate; Protein Conformation; Pyrimidinones; Thermosensing; TRPM Cation Channels

2022