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Neurotransmitter Transporter 이미지

Neurotransmitter Transporter

대표적인 신경전달물질인 5-HT, 아세틸콜린, 아드레날린, GABA, 도파민 등의 수용체를 타겟으로 한 small molecule을 소개합니다.

특징  

 

  • 5-HT Transporters :  뇌 전체에 널리 분포되어 있는 solute carrier family 6 (SLC6) 중 sodium- 및 chloride-의존적인 transporter입니다. 5-HT의 재흡수를 담당하며 분자의 이동을 위해 구조적 변화를 거칩니다.
  • Acetylcholine Transporters : vesicular monoamine transporters (VMAT) 1와 VMAT2를 포함하는 ATP 의존 수송체이며, solute carrier family 18 (SLC18) 중 하나 입니다.
  • Adrenergic Transporters : 뇌 전체에 널리 분포되어 있는noradrenergic neuronal plasma membranes 내의 solute carrier family 6 (SLC6) 중 sodium- 및 chloride-의존적인 transporter입니다. 아드레날린과 노르아드레날린의 재흡수를 담당합니다.
  • Cannabinoid Transporters : Anandamide membrane transporters (AMTs) 또는 endocannabinoid membrane transporters (EMTs)라고도 불리며, Endocannabinoids의 세포로의 재흡수를 촉진하는 것으로 알려져 있습니다. 그러나, 신경전달물질 수송체로서의 존재는 논란의 여지가 있으며 막관통 단백질 수송체 또는 수송체를 코딩하는 유전자는 아직 확인되지 않았습니다.
  • Dopamine Transporters : Striatum와 substantia nigra 등 뇌 전역의 도파민 활성과 관련된 영역에 널리 분포된 solute carrier family 6 (SLC6)이며, sodium- 및 chloride에 의존적입니다. 신속하게 도파민을 제거합니다.
  • GABA Transporters : 신속하게 GABA를 제거하도록 매개하며 세포 외 GABA level을 낮게 유지하도록 하는 solute carrier family 6 (SLC6)이며, sodium- 및 chloride에 의존적입니다. 4개의 12-TM 도메인 수송체가 확인되었고 뉴런 및 신경교세포에 국한되었습니다.
  • Glutamate (EAAT) Transporters : 뇌 전역에 분포된 solute carrier family 6 (SLC1)이며, sodium- 및 chloride에 의존적입니다. 5개의 subtype이 존재하며, 각각이 특정 영역에 특이적으로 분포합니다.
  • Glycine Transporters : High affinity Sodium- 및 chloride에 의존적인 neurotransmitter transporter 단백질입니다. GlyT1 및 GlyT2의 두 종류의 subtype이 존재하는데, GlyT1은 caudal brain areas의 glia에 주로 위치합니다.
  • Nucleoside Transporters : Na+-dependent solute carrier family 28 (SLC28) 와 the equilibrative solute carrier family 29 (SLC29)의 두 family 로 존재합니다. SLC28(CNT1,2, 및 3)은 조직에 따라 다른 subtype의 발현 패턴을 보입니다.
  • Vesicular Monoamine Transporters(VMAT) :  도파민과 같은 생체 아민을 모노아민 함유 뉴런 내의 소포로 수송하며, 이는 신경 전달을 돕고 cytoplasmic neurotransmitter concentrations를 유지하는 데 도움이 됩니다.

 

  

주요 제품 

 

5-HT Transporters

 

 Group Cat. No. Product  Activity
5-HT Transporter Inhibitors 4456 Amitriptyline hydrochloride 5-HT and NA reuptake inhibitor (SNRI); also TrkA/B agonist
1427 Citalopram hydrobromide Highly potent and selective 5-HT uptake inhibitor
4358 Dapoxetine hydrochloride Selective serotonin reuptake inhibitor (SSRI)
2695 Dexfenfluramine hydrochloride 5-HT reuptake inhibitor; also stimulates 5-HT release
4798 (S)-Duloxetine hydrochloride Potent 5-HT and NA reuptake inhibitor (SNRI); also blocks dopamine reuptake
4796 Escitalopram oxalate Selective serotonin reuptake inhibitor (SSRI)
0927 Fluoxetine hydrochloride 5-HT reuptake inhibitor
1033 Fluvoxamine maleate 5-HT reuptake inhibitor
1588 Indatraline hydrochloride Potent 5-HT uptake inhibitor; also inhibits dopamine and noradrenalin uptake
2545 Lofepramine 5-HT and NA reuptake inhibitor (SNRI)
3286 Milnacipran hydrochloride 5-HT and NA reuptake inhibitor (SNRI)
2141 Paroxetine maleate Highly potent and selective 5-HT uptake inhibitor
2395 Sertraline hydrochloride 5-HT reuptake inhibitor
2175 Tetrabenazine Potent inhibitor of vesicular monoamine transport; depletes 5-HT stores
2917 Venlafaxine hydrochloride 5-HT and NA reuptake inhibitor (SNRI)
6202 Vilazodone hydrochloride Potent SSRI and 5-HT1A partial agonist; antidepressant
Other 5763 (R)-Citalopram oxalate Enantiomer of escitalopram oxalate (Cat. No. 1427)
3547 Serotonin hydrochloride Endogenous substrate

 

 

Acetylcholine Transporters

 

 Group Cat. No. Product  Activity
Acetylcholine Transporter Inhibitors 0653 (±)-Vesamicol hydrochloride Inhibits ACh transport

  

 

Adrenergic Transporters 

 

 Group Cat. No. Product  Activity
Adrenergic Transporter Inhibitors 4456 Amitriptyline hydrochloride 5-HT and noradrenalin re-uptake inhibitor; also TrkA/B agonist
2831 Bupropion hydrochloride Non-selective inhibitor of dopamine and noradrenalin transporters
3067 Desipramine hydrochloride Selective inhibitor of noradrenalin transporters
4798 (S)-Duloxetine hydrochloride Potent 5-HT and NA reuptake inhibitor; also blocks dopamine reuptake
1588 Indatraline hydrochloride Potent noradrenalin uptake inhibitor; also inhibits 5-HT and dopamine uptake
2545 Lofepramine 5-HT and NA reuptake inhibitor (SNRI)
1812 Threo-methylphenidate hydrochloride Inhibitor of dopamine and noradrenalin transporters. Psychomotor stimulant
3286 Milnacipran hydrochloride 5-HT and NA reuptake inhibitor (SNRI)
1025 Nisoxetine hydrochloride Noradrenalin re-uptake inhibitor
1992 Nomifensine Potent noradrenalin and dopamine uptake inhibitor. Antidepressant
1982 Reboxetine mesylate Potent and selective noradrenalin uptake inhibitor; orally active
2175 Tetrabenazine Potent inhibitor of vesicular monoamine transport; depletes noradrenalin stores
2011 Tomoxetine hydrochloride Potent and selective noradrenalin re-uptake inhibitor
2917 Venlafaxine hydrochloride 5-HT and NA reuptake inhibitor (SNRI)
Substrates 5169 Noradrenaline bitartrate Endogenous adrenergic hormone and neurotransmitter
Other 6717 FFN 270 Fluorescent substrate for NET and VMAT2

 

 

Cannabinoid Transporters 

 

 Group Cat. No. Product  Activity
Cannabinoid Transporter Inhibitors 1116 AM 404 Anandamide transport inhibitor
1570 (-)-Cannabidiol AMT inhibitor; also GPR55 antagonist, weak CB1 antagonist, CB2 inverse agonist; natural cannabinoid

 

 

Dopamine Transporters 

 

 Group Cat. No. Product Activity
Dopamine Transporter Inhibitors 2831 Bupropion hydrochloride Non-selective inhibitor of dopamine and noradrenalin transporters
4798 (S)-Duloxetine hydrochloride Potent 5-HT and NA reuptake inhibitor; also blocks dopamine reuptake
0513 GBR 12783 dihydrochloride Potent and selective DA uptake inhibitor
0421 GBR 12909 dihydrochloride Selective DA uptake inhibitor; also σ ligand
1588 Indatraline hydrochloride Potent dopamine uptake inhibitor; also inhibits 5-HT and noradrenalin uptake
4351 JHW 007 hydrochloride High affinity dopamine uptake inhibitor
1812 Threo-methylphenidate hydrochloride Inhibitor of dopamine and noradrenalin transporters. Psychomotor stimulant
1992 Nomifensine Potent noradrenalin and dopamine uptake inhibitor. Antidepressant
2742 Reserpine Inhibitor of vesicular monoamine transport
1497 Rimcazole dihydrochloride DAT inhibitor. Also σ2 antagonist
2175 Tetrabenazine Potent inhibitor of vesicular monoamine transport; depletes dopamine stores
Other 4946 AIM 100 Promotes endocytosis and oligomerization of DAT; also Ack1 inhibitor
5200 FFN 102 mesylate Selective fluorescent substrate of DAT and VMAT2

 

 

GABA Transporters 

 

 Group Cat. No. Product  Activity
GABA Inhibitors 1296 CI 966 hydrochloride Selective inhibitor of GAT-1
1779 NNC 711 Selective GAT-1 inhibitor
0768 Riluzole hydrochloride GABA uptake inhibitor; also inhibits glutamate release and blocks NaV channels
1081 SKF 89976A hydrochloride Potent GAT-1 inhibitor; brain penetrant
1561 (S)-SNAP 5114 GABA uptake inhibitor
0181 TACA GABA uptake inhibitor; also GABAA agonist and substrate for GABA-T
4256 Tiagabine hydrochloride Selective GAT-1 inhibitor; anticonvulsant

 

 

Glutamate (EAAT) Transporters 

 

 Group Cat. No. Product  Activity
Glutamate Transporter Modulators 6578 GT 949 Potent and selective positive allosteric modulator of EAAT2
Glutamate Transporter Inhibitors 0846 Chicago Sky Blue 6B Potent inhibitor of L-glutamate uptake into synaptic vesicles; also inhibits MIF
3697 7-Chlorokynurenic acid sodium salt Potent competitive inhibitor of L-glutamate uptake. Sodium salt of 7-Chlorokynurenic acid (Cat. No. 0237)
0237 7-Chlorokynurenic acid Potent competitive inhibitor of L-glutamate uptake
0111 Dihydrokainic acid EAAT2 (GLT-1)-selective non-transportable inhibitor of L-glutamate and L-aspartate uptake
0845 Evans Blue tetrasodium salt Potent inhibitor of L-glutamate uptake into synaptic vesicles; also non-NMDA iGluR antagonist; P2X antagonist
0183 L-(-)-threo-3-Hydroxyaspartic acid Transportable EAAT1-4 inhibitor/non-transportable EAAT5 inhibitor
0298 L-trans-2,4-PDC Transportable EAAT1-4 inhibitor/non-transportable EAAT5 inhibitor
1223 DL-TBOA Selective non-transportable inhibitor of EAATs
2532 TFB-TBOA High affinity EAAT1 and EAAT2 blocker
3490 UCPH 101 Selective non-substrate EAAT1 inhibitor
2652 WAY 213613 Potent, non-substrate EAAT2 inhibitor
Other 5082 LDN 212320 Increases EAAT2 expression; neuroprotective

 

 

Glycine Transporters 

 

 Group Cat. No. Product  Activity
Glycine Transporter Inhibitors 1757 ALX 5407 hydrochloride Selective non-transportable GlyT1 inhibitor
5308 ASP 2535 Potent and selective GlyT1 inhibitor
3397 LY 2365109 hydrochloride Potent and selective GlyT1 inhibitor
2789 NFPS Selective non-transportable GlyT1 inhibitor
4447 Org 24598 Potent and selective inhibitor of the glial glycine transporter GlyT1b; active in vivo
4782 Org 25543 hydrochloride Potent and selective GlyT2 inhibitor

 

 

Nucleoside Transporters 

 

 Group Cat. No. Product  Activity
Nucleoside Transporter Inhibitors 4588 8MDP Potent equilibrative nucleoside transporter (ENT) inhibitor
1692 Cilostazol Adenosine uptake inhibitor. Also PDE3A inhibitor
0481 Dilazep dihydrochloride Adenosine uptake inhibitor
0691 Dipyridamole Adenosine transport inhibitor
1745 5-Iodotubercidin Nucleoside transporter inhibitor; also a broad spectrum kinase inhibitor
2924 NBMPR Equilibrative nucleoside transporter 1 (ENT1) inhibitor
6864 Ticagrelor High affinity equilibrative nucleoside transporter (ENT1) inhibitor; also potent P2Y12 antagonist

 

 

 Vesicular Monoamine Transporters 

 

 Group Cat. No. Product  Activity
Vesicular Monoamine Transporter Inhibitors 2742 Reserpine Inhibitor of vesicular monoamine transport
5168 Rose Bengal Potent VGlut and VMAT inhibitor; cell permeable
2175 Tetrabenazine Potent inhibitor of vesicular monoamine transport
Other 5200 FFN 102 mesylate Selective fluorescent substrate of VMAT2 and DAT
5911 FFN 200 dihydrochloride Selective fluorescent VMAT2 substrate
5043 FFN 206 dihydrochloride Fluorescent VMAT2 substrate
6717 FFN 270 Fluorescent substrate for NET and VMAT2
3878 FFN 511 Fluorescent substrate for VMAT2

 

주문정보

주문정보 - Cat No, PRODUCT, SIZE, 수량 등 항목으로 구성되어있습니다.
  Product Cat.No. Size Maker Qty Data Sheet MSDS
8MDP (10 mg) 4588 10 mg TOCRIS
ALX 5407 hydrochloride (10 mg) 1757 10 mg TOCRIS
ASP 2535 (10 mg) 5308 10 mg TOCRIS
CTPI 2 7794/50 50 mg TOCRIS
CTPI 2 7794/10 10 mg TOCRIS
Dilazep dihydrochloride (50 mg) 0481 50 mg TOCRIS
GT 949 (10 MG) 6578 10 mg TOCRIS
LY 2365109 hydrochloride (10 mg) 3397 10 mg TOCRIS
NBMPR (50 mg) 2924 50 mg TOCRIS
NFPS (10 mg) 2789 10 mg TOCRIS
Org 24598 (10 mg) 4447 10 mg TOCRIS
Org 25543 hydrochloride (10 mg) 4782 10 mg TOCRIS
Sakura 6 7897/1 1 mg TOCRIS
전체보기
Maker
TOCRIS
Cat.No.
4588
Product
8MDP (10 mg)
Size
10 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
1757
Product
ALX 5407 hydrochloride (10 mg)
Size
10 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
5308
Product
ASP 2535 (10 mg)
Size
10 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
7794/50
Product
CTPI 2
Size
50 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
7794/10
Product
CTPI 2
Size
10 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
0481
Product
Dilazep dihydrochloride (50 mg)
Size
50 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
6578
Product
GT 949 (10 MG)
Size
10 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
3397
Product
LY 2365109 hydrochloride (10 mg)
Size
10 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
2924
Product
NBMPR (50 mg)
Size
50 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
2789
Product
NFPS (10 mg)
Size
10 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
4447
Product
Org 24598 (10 mg)
Size
10 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
4782
Product
Org 25543 hydrochloride (10 mg)
Size
10 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
7897/1
Product
Sakura 6
Size
1 mg
Qty
Data Sheet
MSDS
전체보기

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