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G115

Sigma-Aldrich

GR 82334

≥95%

Synonym(s):

pGlu-Ala-Asp-Pro-Asn-Lys-Phe-Tyr-Pro(spiro-γ-lactam-Leu-Trp-NH2

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About This Item

Empirical Formula (Hill Notation):
C69H91N15O16
CAS Number:
129623-01-4
Molecular Weight:
1386.55
MDL number:
MFCD00214619
UNSPSC Code:
12352200
PubChem Substance ID:
329799743

assay

≥95%

storage temp.

−20°C

SMILES string

CC(C)C[C@H](N1CC[C@@]2(CCCN2C(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]5CCCN5C(=O)[C@H](CC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H]6CCC(=O)N6)C1=O)C(=O)N[C@@H](Cc7c[nH]c8ccccc78)C(N)=O

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

InChI key

KWECNVXXONDEKG-JTCMYMKESA-N

Gene Information

human ... TACR1(6869)
mouse ... TACR1(21336)
rat ... TACR1(24807)

Amino Acid Sequence

Glp-Ala-Asp-Pro-Asn-Lys-Phe-Tyr-Pro(spiro-γ-lactam-Leu-Trp-NH2

Biochem/physiol Actions

Potent and specific reversible antagonist at the NK-1 tachykinin receptor.

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

Eyeshields, Gloves, type N95 (US)

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Certificates of Analysis (COA)

Lot/Batch Number
071M1228V
129K1328
107K1035
086K1779
066K1310

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J A Rudd et al.
European journal of pharmacology, 366(2-3), 243-252 (1999-03-19)
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
Yuan-Chang Hsu et al.
PloS one, 7(4), e32855-e32855 (2012-04-13)
The conditioned fear learning and memory occurs when a neutral conditioned stimulus (CS) is paired with an aversive unconditioned stimulus (US). This process is critically dependent on the amygdala and inevitably involves blood pressure (BP) alterations. We hypothesized that BP
R Patacchini et al.
British journal of pharmacology, 122(8), 1633-1638 (1998-01-10)
1. We studied the effect of the natural tachykinins and of synthetic agonists selective for the tachykinin NK1, NK2 and NK3 receptors, on the motility of guinea-pig isolated common bile duct longitudinally-oriented smooth muscle. 2. All the tachykinins tested (both
R Patacchini et al.
Naunyn-Schmiedeberg's archives of pharmacology, 360(3), 344-353 (1999-10-30)
In functional experiments, we have investigated the effect exerted by neurotransmitters released from capsaicin-sensitive primary afferent nerve terminals in the isolated guinea-pig common bile duct. In resting preparations, capsaicin (0.1 microM) produced a quick contraction (45.1+/-4% of KCl 80mM) which
L Barthó et al.
European journal of pharmacology, 392(3), 183-188 (2000-04-14)
The contractile effect of capsaicin in the guinea-pig small intestine involves an activation of enteric cholinergic neurons. Our present data show that the P(2) purinoceptor antagonist pyridoxal-phosphate-6-azophenyl-2',4'-disulphonic acid (PPADS, 30 microM) significantly reduces the contractile response to capsaicin (2 microM)
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