more on synephrine

July 4, 2000

Heiko

I wanted clarify that while there are no clinical studies for obesity

or weight loss, there is basic animal science on synephrine for fat and

carbo metabolism. Abstracts below.The effect of biogenic amines and their analogs on

carbohydrate metabolism in the fat body of the cockroach Blaberus discoidalis.

Park JH, Keeley LL

Department of Entomology, Texas A & M University, College Station,

Texas, 77843, USA.

Several biogenic amines and their analogs were examined for stimulatory

effects on glycogen phosphorylase activity and trehalose biosynthesis in

fat body of the cockroach, Blaberus discoidalis. Octopamine and synephrine

were the most potent activators of fat body phosphorylase; 10 muM octopamine

being nearly as effective as the hypertrehalosemic hormone (HTH). Epinephrine,

norepinephrine, and tyramine produced intermediate effects, whereas dopamine,

5-hydroxytryptamine, and melatonin had no effect. The fat body octopamine

receptors appeared to be pharmacologically related to vertebrate alpha-adrenergic

receptors and belonged to the Octopamine1 class receptor. In contrast to

previous reports, synephrine also induced both phosphorylase activation

and hypertrehalosemia as effectively as octopamine. Demethylchlordimeform,

a formamidine insecticide structurally similar to octopamine, also strongly

activated fat body phosphorylase, possibly by interaction with the octopamine

PMID: 9514848, UI: 98180977

Selective activation of beta3-adrenoceptors by octopamine:

comparative studies in mammalian fat cells.

Carpene C, Galitzky J, Fontana E, Atgie C, Lafontan M, Berlan M

Institut National de la Sante et de la Recherche Medicale (INSERM),

Unite 317, Institut Federatif de Recherches 31, CHU Rangueil, Toulouse,

France. carpene

Numerous synthetic agonists selectively stimulate beta3-adrenoceptors

(ARs). The endogenous catecholamines, noradrenaline and adrenaline, however,

stimulate all the beta-AR subtypes, and no selective physiological agonist

for beta3-ARs has been described so far. The aim of this study was to investigate

whether any naturally occurring amine can stimulate selectively beta3-ARs.

Since activation of lipolysis is a well-known beta-adrenergic function,

the efficacy and potency of various biogenic amines were compared with

those of noradrenaline, isoprenaline, and beta3-AR agonists 4-(-[2-hydroxy-(3-chlorophenyl)ethyl]-amino

propyl)phenoxyacetate (BRL 37,344) and (R,R)-5-(2-[2-(3-chlorophenyl )-2-hydroxyethyl]-amino

propyl)-1,3-benzo-dioxole-2,2-dicarboxylate (CL 316,243) by testing their

lipolytic action in white fat cells. Five mammalian species were studied:

rat, hamster and dog, in which selective beta-AR agonists act as full lipolytic

agents, and guinea-pigs and humans, in which beta3-AR agonists are less

potent activators of lipolysis. Several biogenic amines were inefficient

(e.g. dopamine, tyramine and beta-phenylethylamine) while others (synephrine,

phenylethanolamine, epinine) were partially active in stimulating lipolysis

in all species studied. Their actions were inhibited by all the beta-AR

antagonists tested, including those selective for beta1- or beta2-ARs.

Octopamine was the only amine fully stimulating lipolysis in rat, hamster

and dog fat cells, while inefficient in guinea-pig or human fat cells,

like the beta3-AR agonists. In rat white fat cells, beta-AR antagonists

inhibited the lipolytic effect of octopamine with a relative order of potency

very similar to that observed against CL 316,243. Competitive antagonism

of octopamine effect resulted in the following apparent pA2 [-log(IC50),

where IC50 is the antagonist concentration eliciting half-maximal inhibition]

values: 7.77 (bupranolol), 6.48 [3-(2-ethyl-phenoxy)-1[(1 S)-1,2,3,4-tetrahydronaphth-1-ylaminol]-(2S)2-propanol

oxalate, SR 59230A, a beta3-selective antagonist], 6.30[erythro-D,L-1(7-lethylindan-4-yloxy)-3-isopropylamino-+

++butan-2-ol, ICI 118,551, a beta2-selective antagonist] and 4.71 [(+/-)-[2-(3-carbomyl-4-hydroxyphenoxy)-ethylamino]-3-[4-(1-

methyl-4-trifluoromethyl-2-imidazolyl)-phenoxy]2-propanolmethane sulphonate,

CGP 20712A, a beta1-selective antagonist]. Octopamine had other properties

in common with beta3-AR agonists: stimulation of oxygen consumption in

rat brown fat cells and very low affinity in displacing [3H]CGP 12,177

binding to [beta1- or beta2-ARs in dog and rat adipocyte membranes. In

Chinese hamster ovary (CHO) cells expressing human beta3-ARs, octopamine

inhibited [125I]ICYP binding with only twofold less affinity than noradrenaline

while it exhibited an affinity around 200-fold lower than noradrenaline

in CHO cells expressing human beta1- or beta2-ARs. These data suggest that,

among the biogenic amines metabolically related to catecholamines, octopamine

can be considered as the most selective for beta3-ARs.

PMID: 10344530, UI: 99274327

July 4, 2000

If you prescribe based on biochemistry are you practicing TCM or western medicine?

If the answer is western medicine then what kind of qualifications are necessary?

JOE

I wanted clarify that while there are no clinical studies for obesity or weight loss, there is basic animal science on synephrine for fat and carbo metabolism. Abstracts below.

July 4, 2000

If you prescribe based on biochemistry are you practicing TCM or western medicine?

If the answer is western medicine then what kind of qualifications are necessary?

>>>>>knowledge never hurt anybody

Alon Marcus

-

Joseph Balensi

Tuesday, July 04, 2000 10:57 AM

Re: more on synephrine

If you prescribe based on biochemistry are you practicing TCM or western medicine?

If the answer is western medicine then what kind of qualifications are necessary?

JOE

I wanted clarify that while there are no clinical studies for obesity or weight loss, there is basic animal science on synephrine for fat and carbo metabolism. Abstracts below. Chinese Herbal Medicine, a voluntary organization of licensed healthcare practitioners, matriculated students and postgraduate academics specializing in Chinese Herbal Medicine, provides a variety of professional services, including board approved online continuing education.