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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