| Identification | Back Directory | [Name]
GR 82334 | [CAS]
129623-01-4 | [Synonyms]
GR 82334
pglu-ala-asp-pro-asn-lys-phe-tyr-pro(spiro-γ-lactam-leu-trp-nh2
[[(S,S)PRO-LEU(SPIRO-GAMMA-LACTAM)]9,10, TRP11]PHYSALAEMIN (1-11)
PGLU-ALA-ASP-PRO-ASN-LYS-PHE-TYR-PRO(SPIRO-GAMMA-LACTAM)-LEU-TRP-NH2 | [Molecular Formula]
C69H91N15O16 | [MDL Number]
MFCD00214619 | [MOL File]
129623-01-4.mol | [Molecular Weight]
1386.55 |
| Chemical Properties | Back Directory | [Boiling point ]
1788.6±65.0 °C(Predicted) | [density ]
1.42±0.1 g/cm3(Predicted) | [storage temp. ]
−20°C
| [form ]
Powder | [pka]
4.31±0.19(Predicted) | [Water Solubility ]
Soluble to 1 mg/ml in water | [Sequence]
{Glp}-Ala-Asp-Pro-Asn-Lys-Phe-Tyr-{d-Pro(spiro-γ-lactam)Leu}-Trp-NH2 |
| Hazard Information | Back Directory | [Uses]
GR 82334 is a potent and specific reversible tachykinin NK1 receptor antagonist[1]. GR 82334 inhibits substance P-induced sensitization by blocking SP NK1 receptors in naked mole-rats[1]. | [in vivo]
GR 82334 (intrathecal administration; 0.1 nmol-1 nmol) excites rats unnary bladder motihty at 1 nmol but not at 0.1 nmol, and the reflex chemonociceptive is reduced by the topical application of capsaicin (4 μg/50 ul)[1].GR 82334 (10 nM-1 μM; injected between vertebrae L4 and L5) has no effect at 10 nM in neither species, increases heat-induced foot withdrawal latency in mice at doses >100 nM, but no such increase in naked mole-rats, where doses >100 nM evoke a tendency for decreased latency[2]. | Animal Model: | 3-6 month-old, male C57BL/6 mice and 6-18 month-old naked mole-rats[2] | | Dosage: | 10 nM, 100 nM, and 1 μM | | Administration: | Lntrathecal injection between vertebrae L4 and L5? | | Result: | Increased heat-induced foot withdrawal latency in mice. |
| [References]
[1] A Lecci,et al.Effect of the NK-1 receptor antagonist GR 82,334 on reflexly-induced bladder contractions. Life Sci DOI:10.1016/0024-3205(92)90165-l
[2] Antje Brand, et al. ?Functional neurokinin and NMDA receptor activity in an animal naturally lacking substance P: the naked mole-rat.PLoS One. 2010 Dec 21;5(12):e15162. DOI:10.1371/journal.pone.0015162 |
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