2. GPCR/G Protein Neuronal Signaling
  3. Opioid Receptor
  4. ICI 174864

ICI 174864 is a selective and brain-penetrant δ-opioid receptor antagonist with Ke values of 22.0 nM to 30.6 nM at δ-opioid receptor in mouse vas deferens. ICI 174864 selectively blocks biological effects mediated by the δ-opioid receptor agonist DPDPE (HY-P1334) after central administration. ICI 174864 reverses hypotension in rats with endotoxic shock and inhibits acetic acid-induced writhing in mice. ICI 174864 can be used for the research of opioid receptor subtypes, endotoxic hypotension and analgesic pathways.

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ICI 174864

ICI 174864 Chemical Structure

CAS No. : 89352-67-0

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Based on 1 publication(s) in Google Scholar

ICI 174864 Related Antibodies

Top Publications Citing Use of Products

View All Opioid Receptor Isoform Specific Products:

View All Isoforms
μ Opioid Receptor/MOR κ Opioid Receptor/KOR δ Opioid Receptor/DOR NOP Receptor/ORL1

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  • Purity & Documentation

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Description

ICI 174864 is a selective and brain-penetrant δ-opioid receptor antagonist with Ke values of 22.0 nM to 30.6 nM at δ-opioid receptor in mouse vas deferens. ICI 174864 selectively blocks biological effects mediated by the δ-opioid receptor agonist DPDPE (HY-P1334) after central administration. ICI 174864 reverses hypotension in rats with endotoxic shock and inhibits acetic acid-induced writhing in mice. ICI 174864 can be used for the research of opioid receptor subtypes, endotoxic hypotension and analgesic pathways[1][2][3][4][5].

IC50 & Target[2]

δ Opioid Receptor/DOR

 

In Vitro

ICI 174864 selectively antagonizes delta opioid receptors in in vitro biochemical systems[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

ICI 174864 Related Antibodies
In Vivo

ICI 174864 (1-100 μg; i.c.v.; single dose) acts as a selective, reversible central δ-opioid receptor antagonist at 3 μg with no effect on μ-opioid receptor-mediated activity, but exhibits non-Naloxone (HY-17417A)-reversible agonistic effects at doses ≥6 μg[1].
ICI 174864 (10 μg; i.c.v.; single dose; 3-10 mg/kg; s.c.; single dose) induces dose-dependent behavioral depression and ptosis via s.c. administration, and postural abnormalities, barrel rotation, and hypothermia via i.c.v. administration in naive male Sprague Dawley rats[2].
ICI 174864 (10 μg; i.c.v.; single dose) suppresses acetic acid-induced writhing in male albino mice in a Naloxone-sensitive manner, while 5 μg (i.c.v.; single dose) selectively antagonizes the writhing-suppressant effect of delta agonist DPDPE (HY-P1334) without affecting mu agonist DAGO[2].
ICI 174864 (3μg; i.c.v.; single dose) completely blocks DADL-induced hyperphagia[3].
ICI 174864 (3 mg/kg; i.v.; single dose) significantly reverses endotoxic shock hypotension in male Sprague Dawley rats, without affecting blood pressure in normotensive rats[5].
ICI 174864 (3 mg/kg; i.v.; single dose) produces only a rapid, transient pressor response with no sustained effect in normotensive male Sprague Dawley rats[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague-Dawley (adult female, 200-220 g)[1]
Dosage: 1 μg (inconsistent δ-antagonism); 3 μg (selective δ-antagonism); 6 μg (agonistic activity); 15 μg (bladder contraction inhibition); 50 μg (lethal); 100 μg (lethal)
Administration: i.c.v.; single dose
Result: Produced inconsistent δ-receptor antagonism without affecting bladder contractions.
Completely and reversibly antagonized DPDPE-mediated bladder inhibition without altering DAGO effects.
Showed naloxone-resistant agonistic activity that inhibited bladder contractions.
Caused lethal effects in rats.
Animal Model: Sprague Dawley albino rats (male, 200-220 g)[2]
Dosage: 10 μg (i.c.v.); 3 mg/kg (s.c.); 10 mg/kg (s.c.)
Administration: i.c.v.; single dose; s.c.; single dose
Result: Produced postural abnormalities, barrel rotation, prostration and behavioral depression.
Induced hypothermia in rats.
Caused dose-dependent behavioral depression and ptosis.
Animal Model: albino mice (male, 22-30 g)[2]
Dosage: 10 μg (i.c.v.); 5 μg (i.c.v.); 3 mg/kg (s.c.)
Administration: i.c.v.; single dose; s.c.; single dose
Result: Suppressed acetic acid-induced writhing significantly.
Antagonized DPDPE-induced antinociception but not DAGO-induced antinociception.
Exhibited agonist activity attenuated by high-dose naloxone only.
Animal Model: albino mice (male, 22-30 g)[2]
Dosage: 10 μg (i.c.v.); 25 μg (i.c.v.); 50 μg (i.c.v.)
Administration: i.c.v.; single dose
Result: Produced no obvious effect on tail flick latency.
Did not significantly antagonize analgesic effects of DPDPE or DAGO.
Weakly attenuated analgesic actions of DPDPE and DAGO without statistical significance.
Animal Model: Sprague Dawley (male, 250-350 g, endotoxic shock model induced by E. coli lipopolysaccharide endotoxin 22.5 mg/kg i.v.)[5]
Dosage: 3 mg/kg
Administration: i.v.; single dose
Result: Produced a significant, sustained pressor effect following the initial transient spike, which was significantly greater than the vehicle control at relevant time points.
Animal Model: Sprague Dawley (male, 250-350 g, normotensive)[5]
Dosage: 3 mg/kg
Administration: i.v.; single dose
Result: Produced a rapid, transient pressor response that disappeared within 5 minutes.
Showed no sustained pressor effect over the 60-minute period.
Molecular Weight

606.75

Formula

C34H46N4O6
CAS No.
Appearance

Solid

Color

White to off-white

Sequence

{N,N-diallyl}-Tyr-{Aib}-Phe-Leu
Sequence Shortening

{N,N-diallyl}-Y-{Aib}-FL
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (164.81 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6481 mL 8.2406 mL 16.4813 mL
5 mM 0.3296 mL 1.6481 mL 3.2963 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.6481 mL 8.2406 mL 16.4813 mL 41.2031 mL
5 mM 0.3296 mL 1.6481 mL 3.2963 mL 8.2406 mL
10 mM 0.1648 mL 0.8241 mL 1.6481 mL 4.1203 mL
15 mM 0.1099 mL 0.5494 mL 1.0988 mL 2.7469 mL
20 mM 0.0824 mL 0.4120 mL 0.8241 mL 2.0602 mL
25 mM 0.0659 mL 0.3296 mL 0.6593 mL 1.6481 mL
30 mM 0.0549 mL 0.2747 mL 0.5494 mL 1.3734 mL
40 mM 0.0412 mL 0.2060 mL 0.4120 mL 1.0301 mL
50 mM 0.0330 mL 0.1648 mL 0.3296 mL 0.8241 mL
60 mM 0.0275 mL 0.1373 mL 0.2747 mL 0.6867 mL
80 mM 0.0206 mL 0.1030 mL 0.2060 mL 0.5150 mL
100 mM 0.0165 mL 0.0824 mL 0.1648 mL 0.4120 mL
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ICI 174864 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ICI 17486489352-67-0ICI174864ICI-174864Opioid Receptormale albino micemale Wistar ratsκ-opioid receptorμ-opioid receptorδ-opioid receptorurinary bladder contractionsmale Sprague Dawley ratsendotoxic shockDPDPEDAGOInhibitorinhibitorinhibit

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