Isoguvacine Hydrochloride
Isoguvacine Hydrochloride structure
|
Common Name | Isoguvacine Hydrochloride | ||
|---|---|---|---|---|
| CAS Number | 68547-97-7 | Molecular Weight | 163.60200 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C6H10ClNO2 | Melting Point | N/A | |
| MSDS | USA | Flash Point | N/A | |
| Symbol |
GHS07 |
Signal Word | Warning | |
Use of Isoguvacine HydrochlorideIsoguvacine hydrochloride is a GABA receptor agonist. |
| Name | 1,2,3,6-Tetrahydro-4-pyridinecarboxylic Acid Hydrochloride |
|---|---|
| Synonym | More Synonyms |
| Description | Isoguvacine hydrochloride is a GABA receptor agonist. |
|---|---|
| Related Catalog | |
| Target |
GABA[1] |
| In Vitro | Isoguvacine binds to a mouse forebrain synaptic membrane preparation. The specific binding is displaceable by GABA, muscimol and bicuculline but not by picrotoxin or diaminobutyric acid. Kinetic data suggest two binding affinities. Highest levels of binding are observed in the cerebellum, cortex and hippocampus[1]. Isoguvacine binds to membrane preparations of rat forebrain with pharmacological characteristics similar to the postsynaptic GABA recognition site: that it is transported into synaptosomal preparations by an uptake system similar to the high-affinity GABA uptake system; and that recently accumulated isoguvacine is released in a Ca2+-dependent manner and by heteroexchange with external GABA[2]. Isoguvacine at a concentration of 50 μM blocks the seizure like events in 2 out of 6 organotypic hippocampal slice cultures. Isoguvacine inhibits the low magnesium induced seizure like events dose dependently[3]. |
| Kinase Assay | The assay for 3H-Isoguvacine binding is carried out as follows: membranes suspended in Tris-citrate buffer pH 7.1 are incubated at 4°C for 10 min with 8 nM 3H-Isoguvacine. Identical samples are incubated in the presence of cold 0.5 mM GABA or 10 μM cold isoguvacine. The assay is terminated by centrifugation for 10 min at 4°C in a micro-centrifuge. The supernatants are rapidly aspirated and the surface of the pellets washed (2x) with ice-cold buffer. The pellet is resuspended in I00 μL of 0.1% Triton and placed in a scintillation vial. The assay tube is washed with I00 μL of distilled water and the wash added to the vial along with 10 ml of PCS: xylene (2:1). Counting efficiency is determined to be 40-45% in a Beckman liquid scintillation counter. Specific binding is defined as those radioactive cpm of bound 3H-Isoguvacine that are displaced by excess cold isoguvacine or GABA[1]. |
| References |
| Molecular Formula | C6H10ClNO2 |
|---|---|
| Molecular Weight | 163.60200 |
| Exact Mass | 163.04000 |
| PSA | 49.33000 |
| LogP | 1.12150 |
| Symbol |
GHS07 |
|---|---|
| Signal Word | Warning |
| Hazard Statements | H315-H319-H335 |
| Precautionary Statements | P261-P305 + P351 + P338 |
| Personal Protective Equipment | dust mask type N95 (US);Eyeshields;Gloves |
| Hazard Codes | Xi |
| RIDADR | NONH for all modes of transport |
|
~%
Isoguvacine Hyd... CAS#:68547-97-7 |
| Literature: Heterocycles, , vol. 57, # 12 p. 2321 - 2334 |
|
~%
Isoguvacine Hyd... CAS#:68547-97-7 |
| Literature: Heterocycles, , vol. 57, # 12 p. 2321 - 2334 |
|
~%
Isoguvacine Hyd... CAS#:68547-97-7 |
| Literature: Heterocycles, , vol. 57, # 12 p. 2321 - 2334 |
|
~%
Isoguvacine Hyd... CAS#:68547-97-7 |
| Literature: Journal of Medicinal Chemistry, , vol. 24, # 3 p. 285 - 289 |
|
~98%
Isoguvacine Hyd... CAS#:68547-97-7 |
| Literature: Reeves, Diana C.; Rodriguez, Sonia; Lee, Heewon; Haddad, Nizar; Krishnamurthy, Dhileepkumar; Senanayake, Chris H. Organic Letters, 2011 , vol. 13, # 9 p. 2495 - 2497 |
|
~51%
Isoguvacine Hyd... CAS#:68547-97-7 |
| Literature: Chang, Meng-Yang; Chen, Shui-Tein; Chang, Nein-Chen Heterocycles, 2002 , vol. 57, # 12 p. 2321 - 2334 |
CAS#:70684-84-3
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A molecular characterization of the agonist binding site of a nematode cys-loop GABA receptor.
Br. J. Pharmacol. 172 , 3737-47, (2015) Cys-loop GABA receptors represent important targets for human chemotherapeutics and insecticides and are potential targets for novel anthelmintics (nematicides). However, compared with insect and mamm... |
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The Kölliker-Fuse nucleus gates the postinspiratory phase of the respiratory cycle to control inspiratory off-switch and upper airway resistance in rat.
Eur. J. Neurosci. 24(4) , 1071-84, (2006) Lesion or pharmacological manipulation of the dorsolateral pons can transform the breathing pattern to apneusis (pathological prolonged inspiration). Apneusis reflects a disturbed inspiratory off-swit... |
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Subthalamic stimulation evokes complex EPSCs in the rat substantia nigra pars reticulata in vitro.
J. Physiol. 573(Pt 3) , 697-709, (2006) The subthalamic nucleus (STN) plays an important role in movement control by exerting its excitatory influence on the substantia nigra pars reticulata (SNR), a major output structure of the basal gang... |
| 1,2,3,6-tetrahydropyridine-4-carboxylic acid,hydrochloride |
| Isoguvacine (hydrochloride) |
| Isoguvacine Hydrochloride |
- Dayang Chem (Hangzhou) Co., Ltd.
- China
- Product Name: 1,2,3,6-tetrahydro-4-pyridinecarboxylic acid hydrochloride
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- Zhejiang Hangyu API Co., Ltd
- China
- Product Name: 1,2,3,6-tetrahydro-4-pyridinecarboxylic acid hydrochloride
- Price: ￥Inquiry/1kg
- Purity: 99.5%
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