Naltalimide
Naltalimide (INN) (code name TRK-130, formerly TAK 363) is a novel, centrally-acting opioid drug which is under development by Takeda and Toray for the treatment of overactive bladder/urinary incontinence. It acts as a potent and selective partial agonist of the μ-opioid receptor (Ki = 0.268 nM, EC50 = 2.39 nM, Emax = 66.1%) over the δ-opioid (Ki = 121 nM, EC50 = 26.1 nM, Emax = 71.0%) and κ-opioid receptors (Ki = 8.97 nM, EC50 = 9.51 nM, Emax = 62.6%). Notably, naltalimide somehow appears to lack certain undesirable side effects such as constipation seen with other μ-opioid receptor agonists such as morphine. It enhances bladder storage via suppression of the afferent limb of the micturition reflex pathway.
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Naltalimide
Naltalimide (INN) (code name TRK-130, formerly TAK 363) is a novel, centrally-acting opioid drug which is under development by Takeda and Toray for the treatment of overactive bladder/urinary incontinence. It acts as a potent and selective partial agonist of the μ-opioid receptor (Ki = 0.268 nM, EC50 = 2.39 nM, Emax = 66.1%) over the δ-opioid (Ki = 121 nM, EC50 = 26.1 nM, Emax = 71.0%) and κ-opioid receptors (Ki = 8.97 nM, EC50 = 9.51 nM, Emax = 62.6%). Notably, naltalimide somehow appears to lack certain undesirable side effects such as constipation seen with other μ-opioid receptor agonists such as morphine. It enhances bladder storage via suppression of the afferent limb of the micturition reflex pathway.
has abstract
Naltalimide (INN) (code name T ...... he micturition reflex pathway.
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ATC prefix
CAS number
160359-68-2
IUPAC name
2-[(5α,6β)-17-(Cyclopropylmeth ...... yl]-1H-isoindole-1,3(2H)-dione
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PubChem
thumbnail
Wikipage page ID
44,928,319
Wikipage revision ID
713,219,456
ChemSpiderID
17,226,389
molecular weight
4.72532e+2
smiles
c1ccc2cCN[C@@H]3CC[C@]4O
StdInChIKey
DHAITNWJDOSRBU-IBHWKQIPSA-N
hypernym
comment
Naltalimide (INN) (code name T ...... he micturition reflex pathway.
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label
Naltalimide
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