Approval Year
| Substance Class |
Protein
Created
by
admin
on
Edited
Sat Dec 16 14:22:09 GMT 2023
by
admin
on
Sat Dec 16 14:22:09 GMT 2023
|
| Protein Type | RECEPTOR |
| Protein Sub Type | |
| Sequence Origin | HUMAN |
| Sequence Type | COMPLETE |
| Record UNII |
6J2FX2UG0F
|
| Record Status |
Validated (UNII)
|
| Record Version |
|
-
Download
| Name | Type | Language | ||
|---|---|---|---|---|
|
Common Name | English | ||
|
Common Name | English |
| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
|
6J2FX2UG0F
Created by
admin on Sat Dec 16 14:22:09 GMT 2023 , Edited by admin on Sat Dec 16 14:22:09 GMT 2023
|
PRIMARY | |||
|
Q7L0J3
Created by
admin on Sat Dec 16 14:22:09 GMT 2023 , Edited by admin on Sat Dec 16 14:22:09 GMT 2023
|
PRIMARY |
| Glycosylation Link Type | Site |
|---|---|
| N | 1_498 |
| N | 1_548 |
| N | 1_573 |
| Related Record | Type | Details | ||
|---|---|---|---|---|
|
MODULATOR->TARGET |
Positive modulator of SV2A
|
||
|
LIGAND->TARGET |
|
||
|
LIGAND->TARGET | |||
|
RADIOLIGAND->TARGET |
he measured in vivo Kd value of 11C-UCB-J in this study (3.4 +/- 0.2 nM) is in good agreement with the reported in vitro inhibition constant (Ki) value of 6.3 nM for human SV2A (11). Furthermore, the estimated regional density (Bmax) for neuronal SV2A protein in this study is 125350 nM, which also is in close agreement with the reported regional Bmax values in the human brain measured in vitro.
In preparation for the use of 11C-UCB-J in humans, we performed whole-body distribution studies in rhesus monkeys to calculate organ radiation dosimetry. The organs receiving the largest dose were the liver for males (0.0199 mGy/MBq or 0.0735 rad/mCi) and the brain for females (0.0181 mGy/MBq or 0.0671 rad/mCi). The estimated effective dose equivalent (EDE) value of approximately 4.5 .MU.Sv/MBq for 11C-UCB-J EDE is in the lower range of EDE values (3.317.4 .MU.Sv/MBq) reported in a recent review of organ dosimetry for 11C-labeled radiotracer. Therefore, the maximum EDE from a single 740 MBq (20 mCi) administration of 11C-UCB-J is equivalent to 3.4 mSv (0.34 rem). Thus, multiple injections can be performed in healthy subjects per year.
Kd
|
||
|
|
RADIOLIGAND->TARGET | |||
|
LIGAND->TARGET | |||
|
|
INHIBITOR -> TARGET |
IC50
|
||
|
RADIOLIGAND->TARGET |
|
||
|
LIGAND->TARGET | |||
|
RADIOLIGAND->TARGET |
|
| Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
|---|---|---|---|---|---|---|
| MOL_WEIGHT:NUMBER(CALCULATED) | CHEMICAL |
|