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 제품안내  신경약학   Pharmacology

Neuroscience Chemical Tools

Caged compound, DREADDS등 신경과학 연구에 이용되는 chemical tool을 소개합니다.

TOCRIS
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특징
  • Caged compound는 photolysis를 통해 분해되면서 ligand를 방출하고, 이 ligand는 인근 receptor에 결합하면서 시그널링을 유도합니다.
  • Glutamate, GABA, Dopamine등 다양한 GPCR에 ligand를 전달하기 위한 caged compound를 제공합니다. 
  Caged Glutamate Compounds
  Cat. No. Product Name / Activity
  6553 JF-NP-26 
    Caged Raseglurant (Cat. No. 4416)
  2224 MNI-caged-NMDA
    Caged NMDA
  1490 MNI-caged-L-glutamate
    Stable photoreleaser of L-glutamate
  2277 MNI-caged-D-aspartate
    Caged D-aspartate; ; NMDA agonist
  3331 NPEC-caged-(1S,3R)-ACPD
    Caged (1S,3R)-ACPD
  3840 NPEC-caged-(S)-AMPA
    Caged (S)-AMPA
  4230 NPEC-caged-D-AP5
    Caged D-AP5 (Cat.No. 0106)
  3574 RuBi-Glutamate
    Caged glutamate; excited by visible wavelengths
     
  Caged Amino Acid Compounds
  Cat. No. Product Name / Activity
  6315 DMNB-caged-Serine
    Caged serine; excited by visible blue light
  6121 NB-caged Tyrosine hydrochloride
    ortho-nitrobenzyl caged L- tyrosine
     
  Caged Nicotinic Compounds
  Cat. No. Product Name / Activity
  6706 DPNB-ABT 594
    Caged ABT 594 (Cat. No. 6576); suitable for one- or two-photon photolysis
  6700 PA Nic
    Caged nicotine; photoactivated by one-photon and two-photon excitation
  3855 RuBi-Nicotine
    Caged nicotine; rapidly excitable by visible light
     
  Caged Dopamine Compounds
  Cat. No. Product Name / Activity
  6354 CNV Dopamine
    Caged dopamine; photolysed by UV light
  3992 NPEC-caged-dopamine
    Caged dopamine
     
  Caged Second Messenger Compounds
  Cat. No. Product Name / Activity
  6210 ci-IP3/PM
    Caged inositol triphosphate
  5948 DMNPE-4 AM-caged-calcium
    Caged calcium; cell permeable
  5157 DMNPE-caged ATP diammonium salt
    Caged ATP
     
  Caged GABA Compounds
  Cat. No. Product Name / Activity
  3400 RuBi-GABA
    Caged GABA; excitable at visible wavelengths
  4709 RuBi GABA trimethylphosphine
    Caged GABA; inhibits neural activity
     
  Other Caged Compounds
  Cat. No. Product Name / Activity
  2919 NPE-caged-HPTS
    Caged fluorescent pH indicator
  3512 NPE-caged-proton
    Caged proton



특징
  • Photoswitchable ligand는 빛의 다른 파장에 반응하여 신경 이온 채널과 수용체의 반응을 조절하는 photo-sensitive 화합물입니다.
  • 신경신호에 대한 높은 수준의 공간 및 시간적인 제어를 가능하게 합니다.

  Cat. No. Product Name / Activity
  5462 AAQ chloride
    Photoswitchable Kv channel blocker
  5464 AC 4
    Photoswitchable TRPV1 channel blocker
  7013 OptoBI-1
    Photoswitchable TRPC3/6/7 agonist
  4901 Optovin
    Reversible photoactive TRPA1 activator
  5470 QAQ dichloride
    Photoswitchable Nav, Kv and Cav channel blocker



특징
  • Chemogenetics (화학유전학)은 세포내 신호 전달 경로를 제어하고 조사하는데 있어 강력하고 구체적인 툴입니다.  특히 신경과학에서 신경세포나 신경교세포의 활성을 제어하기 위해 가장 널리 사용됩니다.
  • 광섬유를 이식해야 하는 Optogenetics (광유전학)에 비해, 타겟 receptor에 대한 ligand를 intracerebral infusion, intraperitoneal injection, drinking water등의 방법으로 uptake시킬 수 있어 실험이 수월합니다.
  • 유전적으로 변형된 GPCR에 대한 DREADD ligand 및 키메라 이온 채널(PSAM)을 선택적으로 타겟팅하는 PSAM ligand를 제공합니다.





  DREADD Ligands
  Cat. No. Product Name / Activity
  4936 Clozapine N-oxide
    Activator of hM3Dq and hM4Di DREADDs
  6329 Clozapine N-oxide dihydrochloride
    Activator of hM3Dq and hM4Di DREADDs; water soluble version of Clozapine N-oxide (Cat. No. 4936)
  7193 Deschloroclozapine 
    High affinity and highly potent activator of hM3Dq and hM4Di DREADDs; rapidly blood brain barrier penetrant
  5548 DREADD agonist 21
    Potent hM3Dq and hM4Di DREADD agonist; blood brain barrier penetrant
  6422 DREADD agonist 21 dihydrochloride
    Potent hM3Dq and hM4Di DREADD agonist; water soluble version of DREADD agonist 21 (Cat. No. 5548)
  7197 JHU 37152 
    High affinity and highly potent hM3Dq and hM4Di DREADD agonist; blood brain barrier penetrant
  7198 JHU 37160 
    High affinity and highly potent hM3Dq and hM4Di DREADD agonist; blood brain barrier penetrant
  4349 Olanzapine
    Highly potent hM4Di activator; also 5-HT2A and D2 antagonist
  5549 Perlapine
    Potent hM3Dq and hM4Di DREADD agonist in vitro
  5611 Salvinorin B
    Activator of κ-opioid DREADD (KORD)
  7119 Sorbic acid
    Activator of hFFA2-DREADDs
     
  PSEMs  
  Cat. No. Product Name / Activity
  6425 PSEM 308 hydrochloride
    PSAML141F-GlyR and PSAML141F,Y115F-5-HT3 chimeric ion channel agonist
  6426 PSEM 89S
    PSAML141F-GlyR and PSAML141F,Y115F-5-HT3 chimeric ion channel agonist
  6865 uPSEM 792 hydrochloride
    Highly potent PSAM4-GlyR and PSAM4-5-HT3 chimeric ion channel agonist; brain-penetrant
  6866 uPSEM 817 tartrate
    Highly potent and selective PSAM4-GlyR and PSAM4-5-HT3 chimeric ion channel agonist; brain-penetrant
  2459 Tropisetron hydrochloride
    Activates α7Q79G-GlyR; also potent 5-HT3 antagonist and α7 nAChR partial agonist
  3754 Varenicline tartrate
    Potent activator of PSAM4-5-HT3 and PSAM4-GlyR; also selective α4β2 nAChR partial agonist

  Featured Publications Using Tocris DREADD Ligands & PSEMs
  Badimon et al (2020) Negative feedback control of neuronal activity by microglia. Nature 586, 417. PMID: 32999463
  Francois et al (2017) A Brainstem-Spinal Cord Inhibitory Circuit for Mechanical Pain Modulation by GABA and Enkephalins. Neuron 93, 822. PMID: 28162807
  Leroy et al (2018) A circuit from hippocampal CA2 to lateral septum disinhibits social aggression. Nature 564, 213. PMID: 30518859
  Nam et al (2019) Activation of Astrocytic μ-Opioid Receptor Causes Conditioned Place Preference. Cell Rep 28, 1154. PMID: 31365861
  Pina et al (2020) The kappa opioid receptor modulates GABA neuron excitability and synaptic transmission in midbrain-projections from the insular cortex. Neuropharmacology 165, 107831. PMID: 31870854
 
References
  Campbell & Marchant (2018) The use of chemogenetics in behavioural neuroscience: receptor variants, targeting approaches and caveats. Br J Pharmacol 175, 994. PMID: 29338070
  Coward et al (1998) Controlling signaling with a specifically designed Gi-coupled receptor. Proc Natl Acad Sci USA 95, 352. PMID: 9419379
  Magnus et al (2011) Chemical and genetic engineering of selective ligand-ion channel interactions. Science 333, 1292. PMID: 21885782
  Roth (2016) DREADDs for Neuroscientists. Neuron 89, 683. PMID: 26889809
  Sternson & Roth (2014) Chemogenetic tools to interrogate brain functions. Annu Rev Neurol 37, 387. PMID: 25002280



주문정보(Ordering Information)
CATNUM PRODUCT SIZE
4936 Clozapine N-oxide 10 mg
4936 Clozapine N-oxide 50 mg
5157 DMNPE-caged ATP diammonium salt 10 mg
5462AAQ chloride10 mg
5462AAQ chloride50 mg
5464AC 450 mg
5464AC 410 mg
6210ci-IP3/PM10 ug
6329Clozapine N-oxide dihydrochloride10mg
6329Clozapine N-oxide dihydrochloride50mg
6354CNV Dopamine5 mg
7193Deschloroclozapine10 mg
7193Deschloroclozapine50 mg
6315DMNB-caged-Serine100 mg
5948DMNPE-4 AM-caged-calcium5 mg
6706DPNB-ABT 5945 mg
5548DREADD agonist 2110mg
5548DREADD agonist 2150mg
6422DREADD agonist 21 dihydrochloride50 mg
6422DREADD agonist 21 dihydrochloride10 mg
6553JF-NP-265 mg
7197JHU 3715210 mg
7197JHU 3715250 mg
7198JHU 3716010 mg
7198JHU 3716050 mg
2277MNI-caged-D-aspartate50 mg
2277MNI-caged-D-aspartate10 mg
1490MNI-caged-L-glutamate 10mg
2224MNI-caged-NMDA 10mg
6121NB-caged Tyrosine hydrochloride100 mg
2919NPE-caged-HPTS5mg
3512NPE-caged-proton10mg
3331NPEC-caged-(1S,3R)-ACPD50mg
3331NPEC-caged-(1S,3R)-ACPD10mg
3840NPEC-caged-(S)-AMPA10 mg
4230NPEC-caged-D-AP550mg
4230NPEC-caged-D-AP510mg
3992NPEC-caged-dopamine10mg
3992NPEC-caged-dopamine50mg
4349Olanzapine10mg
4349Olanzapine50mg
7013OptoBI-110 mg
7013OptoBI-150 mg
4901Optovin50 mg
4901Optovin10 mg
6700PA Nic500U
5549Perlapine50 mg
5549Perlapine10 mg
6425PSEM 308 hydrochloride5 mg
6425PSEM 308 hydrochloride25 mg
6426PSEM 89S5 mg
6426PSEM 89S25 mg
5470QAQ dichloride10 mg
5470QAQ dichloride50 mg
4709RuBi GABA trimethylphosphine10 mg
3400RuBi-GABA10mg
3574RuBi-Glutamate10mg
3855RuBi-Nicotine10mg
5611Salvinorin B1 mg
7119Sorbic acid100 mg
2459Tropisetron hydrochloride 10mg
2459Tropisetron hydrochloride 50mg
6865uPSEM 792 hydrochloride25 mg
6865uPSEM 792 hydrochloride5 mg
6866uPSEM 817 tartrate5 mg
6866uPSEM 817 tartrate25 mg
3754Varenicline tartrate10mg
3754Varenicline tartrate50mg