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Cholecystokinnin - Receptor Antagonists

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L4795 L-365260 ≥98% (HPLC) L-365260 is a CCK2 selective antagonist. Enhances amphetamine-induced stimulation of locomotor activity in rats (a model of drug abuse), inhibits thyroid carcinoma (TT)-cell proliferation (potential therapeutic implication for cancer treatment); bilateral injection into the medulla reverses both tactile allodynia and thermal hyperalgesia.
 
L109 Lorglumide sodium salt solid Potent and selective non-peptide cholecystokinin (CCKA) receptor antagonist; orally active.
human ... CCKAR(886)
L2545 LY225910 ≥98% (HPLC) Cholecystokinin is expressed in the gastrointestinal tract and the central nervous system. Cholecystokinin receptor type 2 (CCK2) is a GPCR that is highly expressed in brain and spinal cord. CCK2 is implicated in many brain processes, including mood, anxiety, and pain, through its modulation of GABA neurotransmission.

LY225910 is a potent, selective CCK2 antagonist. LY225910 blocks agonism of CCK2 by CCK-8S, the peptide agonist. LY225910 has been measured in multiple systems, including GABA efflux from cortical cultures, depolarization of spinal cord neurons (via potassium conductance), modulation of excitatory postsynaptic potentials (EPSPs) in nucleus accumbens slices, and enhancement of morphine analgesia.
 
M006 Proglumide sodium salt solid CCK antagonist; selectively blocks CNS effects.
Non-peptide cholecystokinin receptor antagonist that has greater selectivity for the CCKA subtype; orally active.
human ... CCK(885)
mouse ... CCK(12424)
rat ... CCK(25298)
SML0179 SR 27897 hydrate ≥98% (HPLC) SR 27897 has good brain accessibility and regulates the ileal motility through effects on peripheral nervous system.
SR 27897 is a potent, selective antagonist of the Cholecystokinin (CCK) receptor CCK1. SR-27897 blocks the elevation of leptin levels in the CNS following injection of CCK-8 peptide, and causes an increase in food intake in rats.