GR 82334

tachykinin NK-1 receptor antagonist

Also Known As:

GR-82334; physalaemin(1-11), D-Pro(9)(spiro-gamma-lactam)Leu(10)-Trp(11)-; Physalemin, 9-deglycine-10-((5S)-6-oxo-L-alpha-(2-methylpropyl)-1,7-diazaspiro(4.4)nonane-7-acetic acid)-11-L-tryptophanamide-

Networked: 6 relevant articles (0 outcomes, 0 trials/studies)

Bio-Agent Context: Research Results

Amino Acids, Peptides, and Proteins: 1
- Proteins: 484843
  - Intercellular Signaling Peptides and Proteins: 29768
    - Kinins: 2029
      - Tachykinins: 869
        Physalaemin: 11
        GR 82334: 6
  - Nerve Tissue Proteins: 2
    - Neuropeptides: 6772
      - Tachykinins: 869
        Physalaemin: 11
        GR 82334: 6
- Peptides: 82426
Complex Mixtures: 1906
- Venoms: 4328
  - Amphibian Venoms: 77
    - Physalaemin: 11
      - GR 82334: 6
Biological Factors: 2472

Experts

1.	Ito, Hiromoto: 1 article (10/2011)
2.	Sakai, Atsushi: 1 article (10/2011)
3.	Suzuki, Hidenori: 1 article (10/2011)
4.	Uematsu, Takuya: 1 article (10/2011)
5.	Chida, Yoichi: 1 article (02/2007)
6.	Hiramoto, Tetsuya: 1 article (02/2007)
7.	Kubo, Chiharu: 1 article (02/2007)
8.	Sonoda, Junko: 1 article (02/2007)
9.	Sudo, Nobuyuki: 1 article (02/2007)
10.	Abdel-Gawad, M: 1 article (05/2001)

Related Diseases

1.	Vomiting 02/05/1999 - "A 30 min intraperitoneal pre-treatment with CP-122,721, CP-99,994, RP 67580 and FK 888 significantly (P < 0.05) antagonized nicotine-induced emesis with ID50 values of 2.1, 2.3, 13.5 and 19.2 mg/kg, respectively CP-100,263, the less active enantiomer of CP-99,994, was inactive at doses up to 10 mg/kg. Infusion of GR 82334, CP-122,721, CP-99,994 and FK 888 into the dorsal vagal complex of the hindbrain also antagonized nicotine-induced emesis yielding ID50 values of 1.1, 3.0, 3.3 and 58.0 microg/dorsal vagal complex, respectively RP 67580 and CP-100,263 were inactive. " 02/05/1999 - "The anti-emetic potential of CP-122,721 ((+)-2S,3S)-3-(2-methoxy-5-trifluoromethoxybenzyl)amino-2-phenylpi peridine), CP-99,994 ((+)-(2S,3S)-3-(2-methoxybenzylamino)-2-phenylpiperidine), CP-100,263 ((-)-(2R,3R)-3-(2-methoxybenzylamino)-2-phenylpiperidine), RP 67580 ((3R, 7aR)-7,7-diphenyl-2-[1-imino-2-(2-methoxyphenyl)ethyl] po-hydroisoindol-4-one), FK 888 (N2-[(4R)-4-hydroxy-1-(1-methyl-1H-in-dole-3-yl)carbonyl-L-propyl] -N-methyl-N-phenylmethyl-1-3-(2-naphthyl)-alaninamide) and GR 82334 ([D-Pro9[spiro-g-lactam]Leu10]-physalaemin-(1-11)) was investigated to inhibit nicotine (5 mg/kg, s.c.)-, copper sulphate pentahydrate (120 mg/kg, intragastric)- and motion (4 cm horizontal displacement at 1 Hz for 5 min)-induced emesis in Suncus murinus. "
2.	Spinal Cord Injuries (Spinal Cord Injury) 05/01/2001 - "We investigated the selective peptide tachykinin antagonists MEN 11420 and GR 82334 of NK-2 and NK-1 receptors, respectively, in a chronic rat model of detrusor hyperreflexia after suprasacral spinal cord injury. "
3.	Spasm (Spasms) 04/01/1999 - "In seven control preparations, peaks for the first and second phases of contraction reached 35.3+/-3.7% and 20+/-3.2% of maximal longitudinal spasm; the corresponding values in the presence of a combination of GR 82334, MEN 11420 and SR 142801 were 7.5+/-0.8% and 9.1+/-2.2%, respectively (n=6, P<0.001 and 0.05, respectively). " 04/01/1999 - "A combined blockade of neurokinin-1 and neurokinin-3 receptors significantly depressed the effect of capsaicin; the amplitude of the contractile response was 53.3+/-3.7% of the maximal longitudinal spasm in control preparations, whereas in the presence of GR 82334 plus SR 142801 it reached only 27.6+/-5% (P<0.001, Kruskal-Wallis test; n=9 and 10, respectively). "
4.	Abnormal Reflex (Hyperreflexia) 05/01/2001 - "We investigated the selective peptide tachykinin antagonists MEN 11420 and GR 82334 of NK-2 and NK-1 receptors, respectively, in a chronic rat model of detrusor hyperreflexia after suprasacral spinal cord injury. "
5.	Pain (Aches) 08/01/1997 - "With the exception of the response of SR 48968, which was equipotent in both models of nociception, FK 888, GR 82334 and SR 142801 were about 2-25-fold less potent at the ID50 level against the capsaicin-induced pain. "

Related Drugs and Biologics

1.	Neurokinin-1 Receptors (Neurokinin 1 Receptor)
2.	Tachykinins
3.	Capsaicin (Zostrix)
4.	MEN 11420 (Nepadutant)
5.	SR 142801 (osanetant)
6.	FK 888
7.	Neurokinin-1 Receptor Antagonists
8.	Neurokinin-3 Receptors
9.	Physalaemin
10.	Peptides (Polypeptides)