bremazocine

potent, log-acting opiate kappa-agonist & centrally acting analgesic; RN given refers to (2R)-isomer; structure given in first source

Also Known As:

2-(1-hydroxy-cyclopropylmethyl)-5-ethyl-9,9-dimethyl-2'-hydroxy-6,7-benzomorphan; bremazocine hydrochloride, (+-)-isomer; bremazocine hydrochloride, (2R)-isomer; bremazocine, (+-)-isomer; bremazocine, (2S)-isomer; 2,6-Methano-3-benzazocin-8-ol, 6-ethyl-1,2,3,4,5,6-hexahydro-3-((1-hydroxycyclopropyl)methyl)-11,11-dimethyl-, (2R)-

Networked: 34 relevant articles (1 outcomes, 2 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Experts

1.	Amarante, Luiz H: 2 articles (06/2004 - 11/2002)
2.	Husbands, Stephen M: 1 article (01/2009)
3.	Ko, Mei-Chuan: 1 article (01/2009)
4.	Dortch-Carnes, Juanita: 1 article (01/2005)
5.	Potter, David E: 1 article (01/2005)
6.	Alves, Daniela P: 1 article (06/2004)
7.	Duarte, Igor D G: 1 article (06/2004)
8.	Duarte, Igor Dimitri Gama: 1 article (11/2002)
9.	Potter, D E: 1 article (09/2001)
10.	Russell, K R: 1 article (09/2001)

Related Diseases

1.	Body Weight (Weight, Body) 07/01/1987 - "The urine output plateaued between 4-5 ml/100 g body weight irrespective of body weight at the higher doses of bremazocine." 07/01/1987 - "The increased urine output after injection of the kappa agonist bremazocine was determined in rats of various body weights. " 05/31/1988 - "Moreover, chronic infusion of bremazocine, (a kappa-agonist and mu-antagonist) reduced WI, FI, body weight and TC by a magnitude comparable to that of naloxone. " 01/01/2000 - "In contrast, when data were corrected for individual difference in body weight, U69,593, U50,488, (-)-bremazocine, (-)-pentazocine, and furosemide produced nearly equivalent diuresis/kg in females and males, whereas butorphanol produced slightly greater diuresis/kg, and morphine produced significantly less antidiuresis/kg, in females than males. " 01/01/2000 - "When data were not corrected for individual differences in body weight, the kappa agonists U69,593 (0.03-3.0 mg/kg), U50,488 (0.3-10 mg/kg), (-)-bremazocine (0.001-0.1 mg/kg) and (-)-pentazocine (1-10 mg/kg), as well as a nonopioid diuretic, furosemide (1-10 mg/kg) produced significantly greater diuresis in normally hydrated, age-matched males than females; however, there was no sex difference in the diuretic effect of butorphanol (0.3-3.0 mg/kg), or in the antidiuretic effect of the mu agonist morphine (1.0-5.6 mg/kg, in water-loaded rats). "
2.	Ocular Hypotension 09/01/2001 - "This study was designed to investigate mechanisms in the iris-ciliary body (ICB) that may be involved in bremazocine (BRE)-induced ocular hypotension in New Zealand White rabbits. "
3.	Contracture 03/01/1995 - "In contrast, lower bremazocine concentrations (1.4 and 7.1 x 10(-8) M) did not elicit a withdrawal contracture. " 03/01/1995 - "In tissues exposed to these bremazocine concentrations, naloxone(5 x 10-7 M) elicited a marked contracture. " 03/01/1995 - "Bremazocine (1.4-7.1 x 10(-8) M) added 1 min before naloxone (5 x 10(-7) M) inhibited the naloxone withdrawal contracture in a dose-related way whereas naloxone 5 x 10(-8) M added 1 min before naloxone 5 x 10(-7) M, did not affect the withdrawal response. " 03/01/1995 - "3. Bremazocine (5.7 x 10(-7) M) administered to guinea-pig isolated ileum, previously exposed for 5 min to morphine (10(-7) M), induced a withdrawal contracture. " 03/01/1995 - "The observation that low bremazocine concentrations inhibit the morphine-induced withdrawal contractures, indicates an interaction between the micro- and K-opioid system in guinea-pig isolated ileum, similar to that observed in the whole animal."
4.	Shock 03/01/1989 - "A 3-fold higher dose of Mr2266 produced an approximately 10-fold rightward shift in the descending portion of the dose-effect functions for U50,488 and bremazocine under the schedule of stimulus-shock termination but did not appreciably alter their rate-increasing effects. " 03/01/1989 - "Doses of bremazocine (0.001-0.003 mg/kg), U50,488 (0.03-0.1 mg/kg) and Mr2266 (1.0-3.0 mg/kg) that markedly increased overall rates of FI responding maintained by stimulus-shock termination had little effect on or only decreased overall rates of FI responding maintained by food presentation. " 03/01/1989 - "Naltrexone (0.1 mg/kg) antagonized the effects of selected doses of morphine or bremazocine on overall rates of responding under the schedule of stimulus-shock termination. " 03/01/1989 - "The behavioral effects of U50,488 [( trans]-3,4-dichloro-N-methyl-N[2-(1- pyrrolidinyl)cyclohexyl]benzeneacetamide), bremazocine, Mr2266 [(-)-5,9-diethyl-2-(3-furylmethyl)-2'-hydroxy-6,7-benzomorphan] and morphine were compared in squirrel monkeys responding under multiple fixed-ratio fixed-interval (FR FI) schedules of food presentation or stimulus-shock termination. " 12/01/1994 - "These results parallel those previously obtained with other kappa agonists, such as bremazocine and U50,488 and suggest that the antinociceptive effects of spiradoline, enadoline and U69,593 in the shock-titration procedure in squirrel monkeys relate to activity at non-mu, probably kappa, opioid receptors."
5.	Hyperalgesia 04/01/1997 - "The kappa agonists bremazocine and GR89,696 were effective at reversing the hyperalgesia associated with the inflamed hind paw but did not influence the sensitivity of the noninflamed hind paw to noxious heat. " 11/01/2002 - "Intraplantar administration of bremazocine (20, 40 and 50 microg) caused a dose-dependent peripheral antihyperalgesia against carrageenan-induced hyperalgesia. " 03/01/1985 - "Kappa receptors also appeared to mediate hyperalgesia at least in Swiss and CBA strains, as both (-)bremazocine and Mr2266 shortened the jumping latencies." 06/28/2004 - "Bremazocine (20, 40 and 50 microg) dose-dependently reversed the hyperalgesia induced in the rat paw by local injection of carrageenan (250 microg) or prostaglandin E(2) (2 microg), measured by the paw pressure test. " 04/01/1999 - "Coadministration of three kappa opioid ligands, U50,488 (3.2-100 microgram), bremazocine (0.1-3.2 microgram), and dynorphin A(1-13) (3.2-100 microgram), with capsaicin in the tail dose-dependently inhibited capsaicin-induced allodynia. "

Related Drugs and Biologics

1.	Morphine (MS Contin)
2.	Antidiuretic Agents
3.	Pentazocine (Talwin)
4.	Furosemide (Lasix)
5.	Diuretics
6.	Butorphanol (BC 2627)
7.	Opioid Analgesics (Opioids)
8.	Narcotic Antagonists (Opioid Antagonists)
9.	mu Opioid Receptors (mu Opioid Receptor)
10.	Ethylketocyclazocine

Related Therapies and Procedures

1.	Analgesia
2.	Therapeutics
3.	Intravenous Infusions
4.	Aftercare (After-Treatment)