Proglumide

Proglumide

Material name by the IUPAC glossology
IUPAC name (RS) -N2-benzoyl-N,N-dipropyl-α-glutamine
Clinical data
Drugs.com	Sale name according to the country (English) International Drug Names
Legal regulation	℞ (Prescription only)
Dosage method	Oral
Pharmacokinetics data
Half-life	~24 hours
Identification
CAS number (MeSH)	6620-60-6
ATC cord	A02BX06 (WHO)
PubChem	CID: 4922
IUPHAR/BPS	893
UNII	EPL8W5565D
ChEBI	CHEBI: 32058
ChEMBL	CHEMBL316561
Another name	4-benzamido-5-(dipropylamino) -5-oxopentanoic acid
Chemical data
Chemical formula	C18H26N2O4
Molecular weight	334.41 g/mol
SMILES O=C(NC(CCC(O)=O)C(N(CCC)CCC)=O)C1=CC=CC=C1

Proglumide (Proglumide) obstructs the exercise of stomach and intestines and is a drug decreasing the secretion from the stomach and intestines. It acts as an antagonist of the cholecystokinin [¹] and blocks both subtypes of A receptor and the B receptor [²]. I was used for the treatment of peptic ulcer mainly [³], but am replaced [⁴], a drug newer now.

Have an interesting side effect to raise a pain-killer effect of opioid [⁵], and proglumide prevents the resistant acquisition for opioid drugs, and it is possible even to let go [⁶]; [⁷]. For this property, proglumide is useful as adjuvant for the treatment of the chronic pain such as cancers which action having a long opioid drugs needs [⁸]; [⁹].

In addition, proglumide acts as an agonist of the delta-opioid receptors and contributes to a painkilling effect of itself [¹⁰].

Furthermore, I have the work to raise the placebo effect for the pain. The painkilling effect grows big more when I inject it so that a target person can see it when I give a placebo likewise. When I inject it in secret, I do not have an effect, but have an effect even if I give the normal pain-killer while the target person does not notice [¹¹]. This mechanism is regarded as the thing by increasing a nerve course of the expectation.

Allied item

• Proglumetacin

Source

1. ^ Bunney, BS; Chiodo, LA; Freeman, AS (1985). "Further studies on the specificity of proglumide as a selective cholecystokinin antagonist in the central nervous system." It is 345–51. doi: Annals of the New York Academy of Sciences 448 10.1111/j.1749-6632.1985.tb29929.x. PMID 2862828. 
2. ^ Gonzalez-Puga, Cristina; Garcia-Navarro, Ana; Escames, Germaine; Leon, Josefa; Lopez-Cantarero, Manuel; Ros, Eduardo; Acuna-Castroviejo, Dario (2005). "Selective CCK-A but not CCK-B receptor antagonists inhibit HT-29 cell proliferation: Synergism with pharmacological levels of melatonin." Journal of Pineal Research 39 (3): 243–50. doi: 10.1111/j.1600-079X.2005.00239.x. PMID 16150104. 
3. ^ Bergemann, W; Consentius, K; Braun, HE, Hirschmann, H; Marowski, B; Munck, A; Rehs, HU; Stopik, D et al. (1981). "Duodenal ulcer - multicenter double-blind study with proglumide." Medizinische Klinik 76 (8): 226–9. PMID 7231338. 
4. ^ Tariq, M; Parmar, NS; Ageel, AM (1987). "Gastric and duodenal antiulcer and cytoprotective effects of proglumide in rats." The Journal of Pharmacology and Experimental Therapeutics 241 (2): 602–7. PMID 3572816. 
5. ^ McCleane, GJ (2003). "The cholecystokinin antagonist proglumide enhances the analgesic effect of dihydrocodeine." The Clinical journal of pain 19 (3): 200–1. doi: 10.1097/00002508-200305000-00008. PMID 12792559. 
6. ^ Watkins, LR; Kinscheck, IB; Mayer, DJ (1984). "Potentiation of opiate analgesia and apparent reversal of morphine tolerance by proglumide." Science 224 (4647): 395–6. doi: 10.1126/science.6546809. PMID 6546809. 
7. ^ Tang, J; Chou, J; Iadarola, M; Yang, HY; Costa, E (1984). "Proglumide prevents and curtails acute tolerance to morphine in rats." Neuropharmacology 23 (6): 715–8. doi: 10.1016/0028-3908(84) 90,171-0. PMID 6462377. 
8. ^ Bernstein, ZP; Yucht, S; Battista, E; Lema, M; Spaulding, MB (1998). "Proglumide as a morphine adjunct in cancer pain management." Journal of pain and symptom management 15 (5): 314–20. doi: 10.1016/s0885-3924(98) 00003-7. PMID 9654837. 
9. ^ McCleane, GJ (1998). "The cholecystokinin antagonist proglumide enhances the analgesic efficacy of morphine in humans with chronic benign pain." Anesthesia and Analgesia 87 (5): 1117–20. doi: 10.1213/00000539-199811000-00025. PMID 9806692. 
10. ^ Rezvani, A; Stokes, KB; Rhoads, DL; Way, EL (1987). "Proglumide exhibits delta opioid agonist properties." Alcohol and drug research 7 (3): 135–46. PMID 3030338. 
11. ^ Benedetti, F; Amanzio, M; Maggi, G (1995). "Potentiation of placebo analgesia by proglumide." Lancet 346 (8984): 1231. doi: 10.1016/S0140-6736(95)92938-X. PMID 7475687. 

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