PD 135158 | Peptides (Gastrointestinal) | Potent & Selective CCK2 Antagonist | CAM 1028 | PD135158

Category:

7TM Receptors

Peptides (Gastrointestinal)

CCK Receptors

Cat.No.

Product Name

2608

PD 135158

Alternative name(s):

CAM 1028

PD 135158 C35H44N4O6 4-[[(1R)-2-[[(2R)-3-(1H-Indol-3-yl)-2-methyl-1-oxo-2-[[[[(1S,2R,4S)-1,7,7-trimethylbicyclo[2.2.1]hept-2-yl]oxy]carbonyl]amino]propyl]amino]-1-phenylethyl]amino]-4-oxobutanoic acid

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PD 135158

Chemical Name: 4-[[(1R)-2-[[(2R)-3-(1H-Indol-3-yl)-2-methyl-1-oxo-2-[[ [[(1S,2R,4S)-1,7,7-trimethylbicyclo[2.2.1]hept-2-yl]oxy ]carbonyl]amino]propyl]amino]-1-phenylethyl]amino]-4-ox obutanoic acid

Biological Activity:

Potent and selective, nonpeptide CCK₂receptor antagonist (IC₅₀ values are 2.8 and 1232 nM for CCK₂and CCK₁respectively) that displays negligible affinity at GABA_A, benzodiazepine, substance P, neurotensin, opioid, bradykinin and 5-HT₃ receptors (IC₅₀ > 10 μM). Exhibits anxiolytic activity in elevated plus maze and social interaction tests and increases food intake in rats.

Technical Data:

M.Wt:	616.76
Formula:	C₃₅H₄₄N₄O₆
Storage:	Store at +4°C
Solubility:	Soluble to 100 mM in DMSO
Purity:	>98%
CAS No:	[130325-35-8]

Resources:

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References:

Hughes et al (1990) Development of a class of selective cholecystokinin type B receptor antagonists having potent anxiolytic activity. Proc.Natl.Acad.Sci.USA 87 6728. Dorre and Smith (1998) Cholecystokinin_B receptor antagonist increases food intake in rats. Physiol.Behav. 65 11. Tsutsumi et al (1999) Suppression of conditioned fear by administration of CCKB receptor antagonist PD135158. Neuropeptides 33 483.

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Keywords: PD 135158, Peptides (Gastrointestinal), Potent & Selective CCK2 Antagonist, CAM 1028, PD135158, Tocris Bioscience

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