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编 号：F744869
分子式：C21H23N7O6
分子量：469.45
分子式：C21H23N7O6
分子量：469.45
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CAS No: 1414808-96-0
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生物活性：
Tryptamine guanosine carbamate (TpGc) is a selective HINT1 (histidine triad nucleotide-binding protein 1) inhibitor (Ki=34 μM, Kd=3.65 μM). Tryptamine guanosine carbamate significantly enhances morphine antinociception while preventing the development of tolerance.
体内研究：
Pretreatment with 20 nmol Tryptamine guanosine carbamate enhances morphine antinociception in 129 HINT1+/+ mice and is devoid of effect in HINT1-/- mice.The administration of 7 and 20 nmol of Tryptamine guanosine carbamate 20min before the morphine priming dose significantly reduces the development of acute antinociceptive tolerance in HINT1+/+ mice but not in HINT1-/- animals.Tryptamine guanosine carbamate reduces the recruitment of NMDAR activity promoted by morphine. In mice suffering from chronic constriction injury concurrent with increased NMDAR activity, a single intracerebroventricular administration of Tryptamine guanosine carbamate (20 nmol) attenuates NMDAR function and alleviated mechanical allodynia for several days.
Tryptamine guanosine carbamate (TpGc) is a selective HINT1 (histidine triad nucleotide-binding protein 1) inhibitor (Ki=34 μM, Kd=3.65 μM). Tryptamine guanosine carbamate significantly enhances morphine antinociception while preventing the development of tolerance.
体内研究：
Pretreatment with 20 nmol Tryptamine guanosine carbamate enhances morphine antinociception in 129 HINT1+/+ mice and is devoid of effect in HINT1-/- mice.The administration of 7 and 20 nmol of Tryptamine guanosine carbamate 20min before the morphine priming dose significantly reduces the development of acute antinociceptive tolerance in HINT1+/+ mice but not in HINT1-/- animals.Tryptamine guanosine carbamate reduces the recruitment of NMDAR activity promoted by morphine. In mice suffering from chronic constriction injury concurrent with increased NMDAR activity, a single intracerebroventricular administration of Tryptamine guanosine carbamate (20 nmol) attenuates NMDAR function and alleviated mechanical allodynia for several days.
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