GR 82334Tachykinin NK1 receptor antagonist CAS# 129623-01-4 |
- GPR120 modulator 1
Catalog No.:BCC1599
CAS No.:1050506-75-6
Quality Control & MSDS
3D structure
Package In Stock
Number of papers citing our products
| Cas No. | 129623-01-4 | SDF | Download SDF |
| PubChem ID | 16130972 | Appearance | Powder |
| Formula | C69H91N15O16 | M.Wt | 1386.57 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 1 mg/ml in water | ||
| Sequence | XADPNKFYPLW (Modifications: X-1 = Glp, Leu-10 = spiro-g-lactam-Leu, Trp-11 = C-terminal amide) | ||
| Chemical Name | (3S)-4-[(2S)-2-[[(2S)-4-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[(5S)-7-[(2S)-1-[[(2S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]-6-oxo-1,7-diazaspiro[4.4]nonan-1-yl]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-1-oxohexan-2-yl]amino]-1,4-dioxobutan-2-yl]carbamoyl]pyrrolidin-1-yl]-4-oxo-3-[[(2S)-2-[[(2S)-5-oxopyrrolidine-2-carbonyl]amino]propanoyl]amino]butanoic acid | ||
| SMILES | CC(C)CC(C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)N)N3CCC4(C3=O)CCCN4C(=O)C(CC5=CC=C(C=C5)O)NC(=O)C(CC6=CC=CC=C6)NC(=O)C(CCCCN)NC(=O)C(CC(=O)N)NC(=O)C7CCCN7C(=O)C(CC(=O)O)NC(=O)C(C)NC(=O)C8CCC(=O)N8 | ||
| Standard InChIKey | KWECNVXXONDEKG-JTCMYMKESA-N | ||
| Standard InChI | InChI=1S/C69H91N15O16/c1-38(2)31-54(65(97)77-48(58(72)90)34-42-37-73-45-16-8-7-15-44(42)45)83-30-26-69(68(83)100)25-12-29-84(69)67(99)51(33-41-19-21-43(85)22-20-41)81-62(94)49(32-40-13-5-4-6-14-40)78-61(93)46(17-9-10-27-70)76-63(95)50(35-55(71)86)79-64(96)53-18-11-28-82(53)66(98)52(36-57(88)89)80-59(91)39(3)74-60(92)47-23-24-56(87)75-47/h4-8,13-16,19-22,37-39,46-54,73,85H,9-12,17-18,23-36,70H2,1-3H3,(H2,71,86)(H2,72,90)(H,74,92)(H,75,87)(H,76,95)(H,77,97)(H,78,93)(H,79,96)(H,80,91)(H,81,94)(H,88,89)/t39-,46-,47-,48-,49-,50-,51-,52-,53-,54-,69-/m0/s1 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
||
| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
||
| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Tachykinin NK1 receptor antagonist. |
GR 82334 Dilution Calculator
GR 82334 Molarity Calculator
Calcutta University
University of Minnesota
University of Maryland School of Medicine
University of Illinois at Chicago
The Ohio State University
University of Zurich
Harvard University
Colorado State University
Auburn University
Yale University
Worcester Polytechnic Institute
Washington State University
Stanford University
University of Leipzig
Universidade da Beira Interior
The Institute of Cancer Research
Heidelberg University
University of Amsterdam
University of Auckland
TsingHua University
The University of Michigan
Miami University
DRURY University
Jilin University
Fudan University
Wuhan University
Sun Yat-sen University
Universite de Paris
Deemed University
Auckland University
The University of Tokyo
Korea University
- Nevirapine
Catalog No.:BCC3820
CAS No.:129618-40-2
- Satraplatin
Catalog No.:BCC5356
CAS No.:129580-63-8
- Goniopypyrone
Catalog No.:BCN3957
CAS No.:129578-07-0
- Tolfenpyrad
Catalog No.:BCC8069
CAS No.:129558-76-5
- Verteporfin
Catalog No.:BCC3690
CAS No.:129497-78-5
- 3,4-Diacetoxycinnamamide
Catalog No.:BCN6157
CAS No.:129488-34-2
- Fmoc-Asp-OtBu
Catalog No.:BCC3088
CAS No.:129460-09-9
- Fulvestrant
Catalog No.:BCC1081
CAS No.:129453-61-8
- Boc-Cysteinol(pMeBzl)
Catalog No.:BCC3044
CAS No.:129397-85-9
- Fmoc-Phenylalaninol
Catalog No.:BCC2717
CAS No.:129397-83-7
- Euphorbia factor L9
Catalog No.:BCN3786
CAS No.:129393-28-8
- Physcion 8-O-rutinoside
Catalog No.:BCN7324
CAS No.:129393-21-1
- 3-Hydroxybisabola-1,10-dien-9-one
Catalog No.:BCN7325
CAS No.:129673-86-5
- 3,4-Dihydroxybisabola-1,10-diene
Catalog No.:BCN7326
CAS No.:129673-87-6
- ZD 7114 hydrochloride
Catalog No.:BCC6852
CAS No.:129689-28-7
- Dofequidar
Catalog No.:BCC4176
CAS No.:129716-58-1
- Aripiprazole
Catalog No.:BCC5034
CAS No.:129722-12-9
- 2',4'-Dihydroxy-3',6'-dimethoxychalcone
Catalog No.:BCN6158
CAS No.:129724-43-2
- 3-Hydroxylanost-9(11)-24-dien-26-oic acid
Catalog No.:BCN1586
CAS No.:129724-83-0
- Anemoside A3
Catalog No.:BCN2328
CAS No.:129724-84-1
- Anemoside B4
Catalog No.:BCN1276
CAS No.:129741-57-7
- ODM-201
Catalog No.:BCC3796
CAS No.:1297538-32-9
- MC 976
Catalog No.:BCC1734
CAS No.:129831-99-8
- Amicarbazone
Catalog No.:BCC5464
CAS No.:129909-90-6
Effect of the NK-1 receptor antagonist GR 82,334 on reflexly-induced bladder contractions.[Pubmed:1335533]
Life Sci. 1992;51(26):PL277-80.
The effect of intrathecal administration of the novel tachykinin NK-1 receptor antagonist GR 82,334 has been tested in three reflexes which excite urinary bladder motility. GR 82,334 at 1 but not at 0.1 nmol/rat blocked the chemonociceptive micturition reflex induced by the topical application of capsaicin (4 micrograms/50 microliters) onto the urinary bladder. At the same dose proven effective in the chemonociceptive reflex, GR 82,334 did not affect either micturition reflex induced by bladder filling or the urinary bladder contraction induced by perineal pinching. These results suggest that, in urethane-anesthetized rats, specific stimuli applied in the periphery activate NK-1 receptors at spinal cord level facilitating urinary bladder reflex contractions.
Pharmacological characterization of GR82334, a tachykinin NK1 receptor antagonist, in the isolated spinal cord of the neonatal rat.[Pubmed:8566116]
Eur J Pharmacol. 1995 Jul 25;281(1):49-54.
Pharmacological characteristics of [D-Pro9,[spiro-gamma-lactam]Leu10,Trp11]physalaemin-(1-11) (GR82334), a tachykinin NK1 receptor antagonist, and its effects on slow depolarizing responses of lumbar ventral roots evoked by primary afferent stimulation were examined in isolated spinal cord preparations of neonatal rats. GR82334 (1-3 microM) caused dose-dependent rightward shifts of the concentration-response curves for substance P, substance P methyl ester, delta-aminovaleryl [Pro9,N-Me-Leu10]substance P-(7-11) (GR73632) and neurokinin A in normal artificial cerebrospinal fluid and those for substance P methyl ester, GR73632 and neurokinin A in the presence of tetrodotoxin. GR82334 (10 microM) did not evoke gamma-aminobutyric acid (GABA) release from spinal cords of neonatal rats, whereas [D-Pro9,[spiro-gamma-lactam] Leu10,Trp11]substance P (GR71251), another tachykinin NK1 receptor antagonist, induced a significant increase in GABA release. GR82334 (1-3 microM) markedly depressed the slow depolarizing response of ventral roots, referred to as slow ventral root potential, evoked by the stimulation of the contralateral dorsal root or the ipsilateral saphenous nerve. In contrast, cyclo[Gln,Trp,Phe,Gly,Leu,Met] (L-659,877, 1 microM), a selective tachykinin NK2 receptor antagonist, did not depress the saphenous nerve-evoked slow ventral root potential and did not antagonize the action of neurokinin A to induce ventral root depolarization. The present results provide further evidence for the involvement of substance P, neurokinin A and tachykinin NK1 receptors in the primary afferent-evoked slow ventral root potentials.
