Approval Year
| Substance Class |
Protein
Created
by
admin
on
Edited
Sat Dec 16 12:08:26 GMT 2023
by
admin
on
Sat Dec 16 12:08:26 GMT 2023
|
| Protein Type | RECEPTOR |
| Protein Sub Type | ACETYLCHOLINE RECEPTOR |
| Sequence Origin | HUMAN |
| Sequence Type | COMPLETE |
| Record UNII |
P4J1I8C6CX
|
| Record Status |
Validated (UNII)
|
| Record Version |
|
-
Download
| Name | Type | Language | ||
|---|---|---|---|---|
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Common Name | English | ||
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Common Name | English | ||
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Common Name | English | ||
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Common Name | English | ||
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Common Name | English | ||
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Common Name | English |
| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
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P4J1I8C6CX
Created by
admin on Sat Dec 16 12:08:29 GMT 2023 , Edited by admin on Sat Dec 16 12:08:29 GMT 2023
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PRIMARY | |||
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P36544
Created by
admin on Sat Dec 16 12:08:29 GMT 2023 , Edited by admin on Sat Dec 16 12:08:29 GMT 2023
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PRIMARY |
| From | To |
|---|---|
| 1_128 | 1_142 |
| 1_190 | 1_191 |
| 2_128 | 2_142 |
| 3_128 | 3_142 |
| 4_128 | 4_142 |
| 5_128 | 5_449 |
| Glycosylation Type | HUMAN |
| Glycosylation Link Type | Site |
|---|---|
| N | 1_24 |
| N | 1_68 |
| N | 1_111 |
| N | 2_24 |
| N | 2_68 |
| N | 2_111 |
| N | 3_24 |
| N | 3_68 |
| N | 3_111 |
| N | 4_24 |
| N | 4_68 |
| N | 4_111 |
| N | 5_24 |
| N | 5_68 |
| N | 5_111 |
| Related Record | Type | Details | ||
|---|---|---|---|---|
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INHIBITOR -> TARGET |
ALZHEIMERS DISEASE DRUG ANTAGONIZING NMDA RECEPTOR, ANTAGONISM OF .ALPHA.7 NACHR IS A SIDE PATHWAY.
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PARTIAL AGONIST->TARGET |
ACTS AS PARTIAL AGONIST; ACTIVATES ERK1/2 AND CREB PHOSPHORYLATION; ENHANCES COGNITIVE PERFORMANCE. ; ALPHA 7 IN VITRO DATA: Ki = 10.8 nM
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AGONIST -> TARGET |
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RADIOLIGAND->TARGET |
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AGONIST -> TARGET |
GTS-21 was able to improve survival rate of BALB/c mice suffered from endotoxemia when applied in dose 4 mg/kg. As proved on a C57BL6 mouse model, the compound is also suitable for prevention of inflammatory injury induced by mechanical ventilation. In addition to the anti-inflammatory pathway, GTS-21 was assessed in a clinical trial and was proved to improve the cognitive functions of schizophrenic patients.
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RADIOLIGAND->TARGET |
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AGONIST -> TARGET |
ALPHA 7 IN VITRO DATA: Ki = 27 +/- 0.9 nM
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AGONIST -> TARGET |
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AGONIST -> TARGET |
PNU-282,987: A SELECTIVE AND POTENT AGONIST, BUT MAY CAUSE LONG QT SYNDROME.
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AGONIST -> TARGET |
ANABASINE IS A PYRIDINE AND PIPERIDINE ALKALOID FOUND IN THE TREE TOBACCO (NICOTIANA GLAUCA) PLANT, A CLOSE RELATIVE OF THE COMMON TOBACCO PLANT (NICOTIANA TABACUM). IT IS A STRUCTURAL ISOMER OF, AND CHEMICALLY SIMILAR TO, NICOTINE. ITS PRINCIPAL (HISTORICAL) INDUSTRIAL USE IS AS AN INSECTICIDE. ANABASINE IS PRESENT IN TRACE AMOUNTS IN TOBACCO SMOKE, AND CAN BE USED AS AN INDICATOR OF A PERSON'S EXPOSURE TO TOBACCO SMOKE.
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AGONIST -> TARGET |
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RADIOLIGAND->TARGET |
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AGONIST -> TARGET |
AGONIST
STRONG
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AGONIST -> TARGET |
Promising compounds acting as a α7 nAChR selective agonists seem to be also AZD0328 and TC-5619, both containing azabicyclooctane group. They are expected to be useful to treating multiple cognitive dysfunctions and schizophrenia .
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AGONIST -> TARGET |
PHA-543,613: A SELECTIVE AND POTENT AGONIST WITH NOOTROPIC PROPERTIES.
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AGONIST -> TARGET |
NICOTINE IS AN ANTIHERBIVORY ALKALOID AND POTENT PARASYMPATHOMIMETIC STIMULANT AND FOUND IN PLANTS, MOSTLY THOSE IN THE NIGHTSHADE FAMILY. NICOTINE ACTS AS A RECEPTOR AGONIST AT MOST NICOTINIC ACETYLCHOLINE RECEPTORS (NACHRS), EXCEPT AT TWO NICOTINIC RECEPTOR SUBUNITS (NACHR.ALPHA.9 AND NACHR.ALPHA.10) WHERE IT ACTS AS A RECEPTOR ANTAGONIST.
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AGONIST -> TARGET |
CNI-1493 was found to be effective for resolving of endotoxic shock in a rat model. In a clinical trial, CNI-1493 was examined as a drug for the treatment of Crohn’s disease, a disease associated with inflammation. The investigators reported no plausible effect for CNI-1493 single and 3 day dosing. However, cumulative dosing brings some positive effects to Crohn’s disease therapy.
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AGONIST -> TARGET |
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AGONIST -> TARGET |
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AGONIST -> TARGET |
AR-R17779 IS A DRUG THAT ACTS AS A POTENT AND SELECTIVE FULL AGONIST FOR THE .ALPHA.7 SUBTYPE OF NEURAL NICOTINIC ACETYLCHOLINE RECEPTORS. IT HAS NOOTROPIC EFFECTS IN ANIMAL STUDIES, BUT ITS EFFECTS DO NOT SUBSTITUTE FOR THOSE OF NICOTINE. IT HAS ALSO RECENTLY BEEN STUDIED AS A POTENTIAL NOVEL TREATMENT FOR ARTHRITIS.
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AGONIST -> TARGET |
(.ALPHA.7 NACHR) IN VITRO DATA KI = 13.5 NM
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AGONIST -> TARGET |
(.ALPHA.7 NACHR) IN VITRO DATA KI = 6 NM (R)
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AGONIST -> TARGET |
WAY-317538 (SEN-12333) IS A DRUG THAT ACTS AS A POTENT AND SELECTIVE FULL AGONIST FOR THE .ALPHA.7 SUBTYPE OF NEURAL NICOTINIC ACETYLCHOLINE RECEPTORS.
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AGONIST -> TARGET |
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NEGATIVE ALLOSTERIC MODULATOR (NAM)->TARGET |
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AGONIST -> TARGET |
TROPISETRON ACTS AS BOTH A SELECTIVE 5-HT3 RECEPTOR ANTAGONIST AND .ALPHA.7-NICOTINIC RECEPTOR AGONIST.
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INHIBITOR -> TARGET |
NEGATIVE ALLOSTERIC MODULATOR
ALLOSTERIC
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RADIOLIGAND->TARGET |
Ki
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AGONIST -> TARGET |
ACETYLCHOLINE (ACH) IS AN ORGANIC CHEMICAL THAT FUNCTIONS IN THE BRAIN AND BODY OF MANY TYPES OF ANIMALS, INCLUDING HUMANS, AS A NEUROTRANSMITTERA CHEMICAL MESSAGE RELEASED BY NERVE CELLS TO SEND SIGNALS TO OTHER CELLS (NEURONS, MUSCLE CELLS, AND GLAND CELLS).
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AGONIST -> TARGET |
(.ALPHA.7 NACHR) IN VITRO DATA KI = 8.8 +/- 1.3 NM
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AGONIST -> TARGET |
ALPHA 7 IN VITRO DATA: INCREASES MAX AGONIST RESPONSE 17 TO 20-FOLD.
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AGONIST -> TARGET |
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PARTIAL AGONIST->TARGET |
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RADIOLIGAND->TARGET |
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AGONIST -> TARGET |
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![Structure of [11C]CHIBA-1001](/img/b46a00fc-9c04-43fc-98b0-625bc8826ac9.svg "Structure of [11C]CHIBA-1001")
| Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
|---|---|---|---|---|---|---|
| MOL_WEIGHT | CHEMICAL |
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| Molecular Formula | CHEMICAL |
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