Trap 101
Trap 101 structure
|
Common Name | Trap 101 | ||
|---|---|---|---|---|
| CAS Number | 1216621-00-9 | Molecular Weight | 434.01500 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C24H36ClN3O2 | Melting Point | N/A | |
| MSDS | Chinese USA | Flash Point | N/A | |
| Symbol |
GHS06 |
Signal Word | Danger | |
Use of Trap 101Trap-101 hydrochloride is a potent, selective and competitive antagonist of NOP receptors over classical opioid receptors. Trap-101 stimulates GTPγ35S binding to CHOhNOP membranes with pKi values of 8.65, 6.60, 6.14 and <5 for NOP, μ-, κ-, and δ-opioid receptors, respectively. Trap-101 attenuates motor deficits in a rat model of parkinson's disease and can be used for the research of nervous system diseases[1]. |
| Name | Trap-101 hydrochloride |
|---|---|
| Synonym | More Synonyms |
| Description | Trap-101 hydrochloride is a potent, selective and competitive antagonist of NOP receptors over classical opioid receptors. Trap-101 stimulates GTPγ35S binding to CHOhNOP membranes with pKi values of 8.65, 6.60, 6.14 and <5 for NOP, μ-, κ-, and δ-opioid receptors, respectively. Trap-101 attenuates motor deficits in a rat model of parkinson's disease and can be used for the research of nervous system diseases[1]. |
|---|---|
| Related Catalog | |
| Target |
pKi: 8.65 (NOP receptor); 6.60 (μ-opioid receptor); 6.14 (κ-opioid receptor); < 5 (δ-opioid receptor)[1] |
| In Vitro | Trap-101 hydrochloride (3, 30, and 300 nM) is inactive per se up to 10 μM, while in the range 3-300 nM, it produces a concentration dependent rightward shift of the concentration-response curve to N/OFQ without modifications of the maximal response to the agonist. Receptor binding affinities of Trap101 (pKi values) at recombinant human NOP, and classical opioid receptors expressed in CHO cell membranes are 8.65, 6.60, 6.14 and < 5 for NOP, μ-, κ-, and δ-opioid receptors respectively[1]. |
| In Vivo | Trap-101 hydrochloride (10-30 mg/kg; detected after 90 min) changes motor activity in naïve rats, it causes a delayed increase in the immobility time in the bar test at 30 mg/kg, Moreover, it increased stepping activity and rotarod performance at 10 mg/kg and reduces them at 30 mg/kg[1]. 6-OHDA lesioning produces motor asymmetry mostly affecting the contralateral paw and overall reduced motor performance. Trap-101 hydrochloride (intraperitoneal injection; 10-30 mg/kg; detected after 90 min) alleviates akinesia/bradykinesia and improves overall gait ability in hemiparkinsonian rats, being effective starting at 1 mg/kg and without worsening motor deficit at 30 mg/kg[1]. Animal Model: 6-OHDA hemilesioned rats[1] Dosage: 10-30 mg/kg Administration: Intraperitoneal injection; 10-30 mg/kg; detected after 90 min Result: Attenuated parkinsonian-like motor deficits in rat. |
| References |
| Molecular Formula | C24H36ClN3O2 |
|---|---|
| Molecular Weight | 434.01500 |
| Exact Mass | 433.25000 |
| PSA | 50.40000 |
| LogP | 4.83240 |
| Symbol |
GHS06 |
|---|---|
| Signal Word | Danger |
| Hazard Statements | H301 |
| Precautionary Statements | P301 + P310 |
| RIDADR | UN 2811 6.1 / PGIII |
|
Combining functional features of whole-grain barley and legumes for dietary reduction of cardiometabolic risk: a randomised cross-over intervention in mature women.
Br. J. Nutr. , 1-9, (2013) The usefulness of dietary strategies against cardiometabolic risk is increasingly being acknowledged. Legumes and whole grains can modulate risk markers associated with cardiometabolic diseases, but t... |
|
|
Effect of insular injury on autonomic functions in patients with ruptured middle cerebral artery aneurysms.
Stroke , (2013) Insular injuries are known to cause autonomic derangements. Patients with ruptured middle cerebral artery aneurysms frequently develop temporal hematomas (THs) in addition to subarachnoid hemorrhages,... |
|
|
Preventive home visits for mortality, morbidity, and institutionalization in older adults: a systematic review and meta-analysis.
PLoS ONE 9(3) , e89257, (2014) Home visits for older adults aim to prevent cognitive and functional impairment, thus reducing institutionalization and mortality. Visitors may provide information, investigate untreated problems, enc... |
| 1-[1-(Cyclooctylmethyl)-5-(hydroxymethyl)-1,2,3,6-tetrahydro-4-py ridinyl]-3-ethyl-1,3-dihydro-2H-benzimidazol-2-one hydrochloride (1:1) |