| Bioactivity | 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[1]. |
| In Vivo | 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[1].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[1]. |
| Name | Tryptamine guanosine carbamate |
| CAS | 1414808-96-0 |
| Formula | C21H23N7O6 |
| Molar Mass | 469.45 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Garzón J, et al. HINT1 protein: a new therapeutic target to enhance opioid antinociception and block mechanical allodynia. Neuropharmacology. 2015;89:412-423. |