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PZ0175

Sigma-Aldrich

PD 149163 tetrahydrochloride hydrate

≥90% (HPLC)

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Synonym(s):
N2-[(2S)-2,6-Diaminohexyl]-L-lysyl-L-prolyl-L-tryptophyl-3-methyl-L-valyl-L-Leucine ethyl ester tetrahydrochloride hydrate
Empirical Formula (Hill Notation):
C42H71N9O6·4HCl · xH2O
CAS Number:
1021868-80-3
Molecular Weight:
943.91 (anhydrous basis)
MDL number:
MFCD20527308
UNSPSC Code:
12352200
PubChem Substance ID:
329823749
NACRES:
NA.77

Quality Level

100

Assay

≥90% (HPLC)

form

powder (Hygroscopic)

storage condition

desiccated

color

white to tan

solubility

H2O: ≥12 mg/mL

storage temp.

2-8°C

SMILES string

O.Cl.Cl.Cl.Cl.CCOC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]3CCCN3C(=O)[C@H](CCCCN)NC[C@@H](N)CCCCN)C(C)(C)C

InChI

1S/C42H71N9O6.4ClH.H2O/c1-7-57-41(56)34(23-27(2)3)49-39(54)36(42(4,5)6)50-37(52)33(24-28-25-46-31-17-9-8-16-30(28)31)48-38(53)35-19-14-22-51(35)40(55)32(18-11-13-21-44)47-26-29(45)15-10-12-20-43;;;;;/h8-9,16-17,25,27,29,32-36,46-47H,7,10-15,18-24,26,43-45H2,1-6H3,(H,48,53)(H,49,54)(H,50,52);4*1H;1H2/t29-,32-,33-,34-,35-,36+;;;;;/m0...../s1

InChI key

PIFVEGOSSWCHFK-AEPODNBTSA-N

Biochem/physiol Actions

PD 149163 is a Neurotensin NTR1 receptor agonist; a Neurotensin (8-13) analog. PD149163 is a selective, brain penetrating NT1 receptor agonist with pro-cognitive, antipsychotic and anxiolytic effects.

Features and Benefits

This compound is featured on the Neurotensin Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

Pictograms

Exclamation mark
GHS07

Signal Word

Warning

Hazard Statements

H302,H315,H319,H335

Hazard Classifications

Acute Tox. 4 Oral - Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3

Target Organs

Respiratory system

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Regulatory Information

监管及禁止进口产品

Certificates of Analysis (COA)

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Elizabeth N Holly et al.
European neuropsychopharmacology : the journal of the European College of Neuropsychopharmacology, 21(7), 526-531 (2011-02-01)
Agonists for neurotensin (NT)-1 receptors have produced antipsychotic-like effects in many animals, including reversal of prepulse inhibition deficits and psychostimulant-induced increases in spontaneous activity. The present study sought to provide a basic assessment of the putative antipsychotic effects of PD149163
Adam J Prus et al.
Progress in neuro-psychopharmacology & biological psychiatry, 49, 78-84 (2013-11-28)
Neurotensin is an endogenous neuropeptide that has significant interactions with monoamine neurotransmitter systems. To date, neurotensin NTS1 receptor agonists, such as PD149163, have been primarily evaluated for the treatment for schizophrenia, drug addiction, and pain. Recently, PD149163 was found to
Todd M Hillhouse et al.
Experimental and clinical psychopharmacology, 22(6), 548-556 (2014-10-07)
Major depressive disorder is the most common mood disorder in the United States and European Union; however, the limitations of clinically available antidepressant drugs have led researchers to pursue novel pharmacological treatments. Clinical studies have reported that monotherapy with the

Articles

Neurotensin Receptors

Neurotensin is a 13 amino acid regulatory peptide found mainly in gut and brain. Intestinal neurotensin is produced by a discrete population of endocrine cells (N cells) scattered throughout the jejuno-ileal mucosa.

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