GR 82334
GR 82334 Basic information
- Product Name:
- GR 82334
- Synonyms:
-
- GR 82334
- PGLU-ALA-ASP-PRO-ASN-LYS-PHE-TYR-PRO(SPIRO-GAMMA-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-γ-lactam-leu-trp-nh2
- L-Tryptophanamide, 5-oxo-L-prolyl-L-alanyl-L-α-aspartyl-L-prolyl-L-asparaginyl-L-lysyl-L-phenylalanyl-L-tyrosyl-(αS,5S)-α-(2-methylpropyl)-6-oxo-1,7-diazaspiro[4.4]nonane-7-acetyl-
- CAS:
- 129623-01-4
- MF:
- C69H91N15O16
- MW:
- 1386.55
- Mol File:
- 129623-01-4.mol
GR 82334 Chemical Properties
- 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
Safety Information
- Safety Statements
- 22-24/25
- WGK Germany
- 3
MSDS
- Language:English Provider:SigmaAldrich
GR 82334 Usage And Synthesis
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
GR 82334Supplier
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